Publications and Patents
Publications
- A. Oneto, G. A. Hamwi, L. Schäkel, N. Krüger, K. Sylvester, M. Petry, R. A. Shamleh, T. Pillaiyar, T. Claff, A. C. Schiedel, N. Sträter, M. Gütschow, C. E. Müller;
Nonpeptidic Irreversible Inhibitors of SARS-CoV-2 Main Protease with Potent Antiviral Activity;
J. Med. Chem. 2024, accepted.
- J. Sievers, R. Voget, F. Lu, K. M. Garchitorena, Y. L. D. Ng, C. H. Chau, C. Steinebach, W. D. Figg, J. Krönke, M. Gütschow;
Revisiting the Antiangiogenic Mechanisms of Fluorinated Thalidomide Derivatives;
Bioorg. Med. Chem. Lett. 2024, 110, 129858.
- B. E. Barton, M. K. Collins, C. H. Chau, H. Choo-Wosoba, D. J. Venzon, C. Steinebach, K. M. Garchitorena, B. Shah, E. L. Sarin, M. Gütschow, W. D. Figg;
Preclinical Evaluation of a Novel Series of Polyfluorinated Thalidomide Analogs in Drug Resistant Multiple Myeloma;Biomolecules, 2024, 14, 725.
- A. Bricelj, Y. L. D. Ng, M. Gobec, R. Kuchta, W. Hu, Š. Javornik, M. Rožič, M. Gütschow, G. Zheng, J. Krönke, C. Steinebach,* I. Sosič;*
Design, Synthesis, and Evaluation of BCL-2 Targeting PROTACs;Chem. Eur. J. 2024, e202400430.
- J. Breidenbach, R. Voget, Y. Si, A. Hingst, T. Claff, K. Sylvester, V. Wolf, V. Krasniqi, A. Useini, N. Sträter, Y. Ogura, A. Kawaguchi, C. E. Müller, M. Gütschow;
Macrocyclic Azapeptide Nitriles: Structure-Based Discovery of Potent SARS-CoV-2 Main Protease Inhibitors as Antiviral Drugs;J. Med. Chem. 2024, 67, 8757-8790.
- Y. Yamauchi, S. Konno, N. Noriko, N. Yoshioka, A. Hingst, M. Gütschow, C. E. Müller, A. Taguchi, A. Taniguchi, A. Kawaguchi, Y. Hayashi;
Detection of Active SARS-CoV-2 3CL Protease in Infected Cells using Activity-based Probes with a 2,6-Dichlorobenzoyloxymethyl Ketone Reactive Warhead;ACS Chem. Biol. 2024, 19, 1028-1034.
- R. Voget, J. Breidenbach,§ T. Claff,§ A. Hingst,§ K. Sylvester, C. Steinebach, L. P. Vu, R. H. Weiße, U. Bartz, N. Sträter, C. E. Müller, M. Gütschow;
Development of an Active-site Titrant for SARS-CoV-2 Main Protease as an Indispensable Tool for Evaluating Enzyme Kinetics;
§J.B., T.C. and A.H. contributed equally to this work.Acta Pharm. Sin. B 2024, 14, 2349-2357.
- I. Pachòn-Angona, P. J. Bernard, A. Simakov, M. Maj, K. Jozwiak, A. Novotna, C. Lemke, M. Gütschow, H. Martin, M. J. Oset-Gasque, J. Marco-Contelles,* L. Ismaili;*
Design and Synthesis of Multi-Functional Ligands through Hantzsch Reaction: Targeting Ca2+ Channels, Activating Nrf2 and Possessing Cathepsin S Inhibitory and Antioxidant Properties;Pharmaceutics 2024, 16, 121.
- P. Flury,§ J. Breidenbach,§ N. Krüger,§ R. Voget, L. Schäkel, Y. Si, V. Krasniqi, S. Calistri, M. Olfert, K. Sylvester, C. Rocha, R. Ditzinger, A. Rasch, S. Pöhlmann, T. Kronenberger, A. Poso, K. Rox, S. A. Laufer, C. E. Müller, M. Gütschow,* T. Pillaiyar;*
Cathepsin-Targeting SARS-CoV-2 Inhibitors: Design, Synthesis, and Biological Activity;
§P.F., J.B. and N.K. contributed equally to this work.
ACS Pharmacol. Trans. Sci. 2024, 7, 493-514.
- C. Steinebach,§ A. Bricelj,§ A. Murgai,§ I. Sosič, L. Bischof, Y. L. D. Ng, C. Heim, S. Maiwald, M. Proj, R. Voget, F. Feller, J. Košmrlj, V. Sapozhnikova, A. Schmidt, M. R. Zuleeg, P. Lemnitzer, P. Mertins, F. K. Hansen, M. Gütschow, J. Krönke,* M. D. Hartmann;*
Leveraging Ligand Affinity and Properties: Discovery of Novel Benzamide-Type Cereblon Binders for the Design of PROTACs;
§C.S., A.B. and A.M. contributed equally to this work.J. Med. Chem. 2023, 66, 14513-14543.
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L. P. Vu, C. J. Diehl,§ R. Casement,§ A. G. Bond,§ C. Steinebach, N. Strašek, A. Bricelj, A. Perdih, G. Schnakenburg, I. Sosič, A. Ciulli,* M. Gütschow;*
Expanding the Structural Diversity at the Phenylene Core of Ligands for the von Hippel-Lindau (VHL) E3 Ubiquitin Ligase: Development of Highly Potent Hypoxia-Inducible Factor-1α (HIF-1α) Stabilizers;
§C.J.D., R.C. and A.G.B. contributed equally to this work.
J. Med. Chem. 2023, 66, 12776-12811. -
M. Abdoli, V. Krasniqi, A. Bonardi, M. Gütschow,* C. T. Supuran,* R. Žalubovskis;*
4-Cyanamido-substituted Benzenesulfonamides Act as Dual Carbonic Anhydrase and Cathepsin Inhibitors;
Bioorg. Chem. 2023, 139, 106725. -
S. J. Hammerschmidt, H. Maus, A. C. Weldert, M. Gütschow, C. Kersten;
Improving Binding Entropy by Higher Ligand Symmetry? – A Case Study with Human Matriptase;
RSC Med. Chem. 2023, 14, 969-982. -
T. Keuler, V. Wolf, C. Lemke, R. Voget, A. Braune,* M. Gütschow;*
Fluorogenic Substrates and Pre‐column Derivatization for Monitoring the Activity of Bile Salt Hydrolase from Clostridium perfringens;
Bioorg. Chem. 2023, 138, 106574. -
Y. L. D. Ng,§ A. Bricelj,§ J. A. Jansen, A. Murgai, K. Peter, K. A. Donovan, M. Gütschow, J. Krönke, C. Steinebach,* I. Sosič;*
Heterobifunctional Ligase Recruiters Enable Pan-Degradation of Inhibitor of Apoptosis Proteins;
§Y.L.D.N. and A.B. contributed equally to this work.
J. Med. Chem. 2023, 66, 4703-4733. -
N. Geiger, V. Diesendorf, V. Roll, E. M. König, H. Obernolte, K. Sewald, J. Breidenbach, T. Pillaiyar, M. Gütschow, C. E. Müller, J. Bodem;Cell Type-specific Anti-viral Effects of Novel SARS-CoV-2 Main Protease Inhibitors;
Int. J. Mol. Sci. 2023, 24, 3972. -
R. Kuchta, C. Heim, A. Herrmann, S. Maiwald, Y. L. D. Ng, I. Sosič, T. Keuler, J. Krönke, M. Gütschow, M. D. Hartmann,* C. Steinebach;*
Accessing Three-Branched High-Affinity Cereblon Ligands for Molecular Glue and Protein Degrader Design;
RSC Chem. Biol. 2023, 4, 229-234. -
F. Pöstges, K. Kayser, J. Appelhaus, M. Monschke, M. Gütschow, C. Steinebach,* K. G. Wagner;*
Solubility Enhanced Formulation Approaches to Overcome Oral Delivery Obstacles of PROTACs;
Pharmaceutics 2023, 15, 156.
- A. Bricelj,§ Y. L. D. Ng,§ D. Ferber, R. Kuchta, S. Müller, M. Monschke, K. G. Wagner, J. Krönke, I. Sosič, M. Gütschow, C. Steinebach;
Influence of Linker Attachment Points on Stability and Neosubstrate Degradation of Cereblon Ligands;
§A.B. and Y.L.D.N. contributed equally to this work.
ACS Med. Chem. Lett. 2021, 12, 1733-1738. -
L. Schäkel, S. Mirza, M. Pietsch, S. Y. Lee, T. Keuler, K. Sylvester, J. Pelletier, J. Sévigny, T. Pillaiyar, M. Gütschow, C. E. Müller;
2-Substituted Thienotetrahydropyridine Derivatives – Allosteric Ectonucleotidase Inhibitors;
Arch. Pharm. 2021, 354, e2100300. -
C. Lemke, J. Benýšek, D. Brajtenbach, C. Breuer, A. Jílková, M. Horn, M. Buša, L. Ulrychová, A. Illies, K. F. Kubatzky, U. Bartz, M. Mareš,* M. Gütschow;*
An Activity-Based Probe for Cathepsin K Imaging with Excellent Potency and Selectivity;
J. Med. Chem. 2021, 64, 13793-13806. -
I. Sosič,* M. Gobec, C. Steinebach, M. Schlesinger, G. Bendas, M. Gütschow;*
Another Structural Correction for 1-Oxo-1H-phenalene-2,3-dicarbonitriles: Synthesis of a Potent BCL-2 Inhibiting 7-Phenoxy Derivative;
Arch. Pharm. 2021, 354, e2100151. -
A. Bricelj, C. Steinebach, R. Kuchta, M. Gütschow,* I. Sosič;*
E3 Ligase Ligands in Successful PROTACs: An Overview of Syntheses and Linker Attachment Points;
Front. Chem. 2021, 9, 707317. -
W. Tonnus, C. Meyer, C. Steinebach, A. Belavgeni, A. von Mässenhausen, N. Zamora Gonzalez, F. Maremonti, F. Gembardt, N. Himmerkus, M. Latk, S. Locke, J. Marschner, W. Li, S. Short, S. Doll, I. Ingold, B. Proneth, C. Daniel, N. Kabgani, R. Kramann, S. Motika, P. Hergenrother, S. R. Bornstein, C. Hugo, J. U. Becker, K. Amann, H. J. Anders, D. Kreisel, D. Pratt, M. Gütschow, M. Conrad, A. Linkermann;
Dysfunction of the Key Ferroptosis-surveilling Systems Hypersensitizes Mice to Massive Tubular Necrosis During Acute Kidney Injury;
Nat. Commun. 2021, 12, 4402. -
W. Deuther-Conrad,* D. Diez-Iriepa, I. Iriepa, F. López-Muñoz, M. A. Martínez-Grau, M. Gütschow,* J. Marco-Contelles;*
Studies on the Affinity of 6-[(n-(Cyclo)aminoalkyl)oxy]-4H-chromen-4-ones for Sigma 1/2 Receptors;
RSC Med. Chem. 2021, 12, 1000-1004. -
T. Keuler, K. Gatterdam, A. Akbal, M. Lovotti, M. Marleaux, M. Geyer, E. Latz, M. Gütschow;
Development of Fluorescent and Biotin Probes Targeting NLRP3;
Front. Chem. 2021, 9, 642273. -
J. Breidenbach,§ C. Lemke,§ T. Pillaiyar,§ L. Schäkel,§ G. Al Hamwi, M. Diett, R. Gedschold, N. Geiger, V. Lopez, S. Mirza, V. Namasivayam, A. C. Schiedel, K. Sylvester, D. Thimm, C. Vielmuth, L. P. Vu, M. Zyulina, J. Bodem, M. Gütschow,* C. E. Müller;*
Targeting the Main Protease of SARS-CoV-2: From the Establishment of High Throughput Screening to the Design of Tailored Inhibitors;
§J.B., C.L., T.P. and L.S. contributed equally to this work.
Angew. Chem. Int. Ed. 2021, 60, 10423-10429. -
J. Breidenbach,§ C. Lemke,§ T. Pillaiyar,§ L. Schäkel,§ G. Al Hamwi, M. Diett, R. Gedschold, N. Geiger, V. Lopez, S. Mirza, V. Namasivayam, A. C. Schiedel, K. Sylvester, D. Thimm, C. Vielmuth, L. P. Vu, M. Zyulina, J. Bodem, M. Gütschow,* C. E. Müller;*
Die Hauptprotease von SARS-CoV-2 als Zielstruktur: Von der Etablierung eines Hochdurchsatz-Screenings zum Design maßgeschneiderter Inhibitoren;
§J.B., C.L., T.P. und L.S. haben gleichermaßen zu dieser Arbeit beigetragen.
Angew. Chem. 2021, 133, 10515-10521. -
A. Jílková, M. Horn, J. Fanfrlík, J. Küppers, P. Pachl, P. Řezáčová, M. Lepšík, P. Fajtová, P. Rubešová, M. Chanová, C. R. Caffrey, M. Gütschow,* M. Mareš;*
Azanitrile Inhibitors of the SmCB1 Protease Target are Lethal to Schistosoma mansoni: Structural and Mechanistic Insights into Chemotype Reactivity;
ACS Infect. Dis. 2021, 7, 189-201. -
N. Kirchner, C. Cano-Prieto, A. C. Schulz-Fincke, M. Gütschow, N. Ortlieb, J. Moschny, T. H. Niedermeyer, J. Horak, M. Lämmerhofer, M. van der Voort, J. M. Raaijmakers, H. Gross;
Discovery of Thanafactin A, a Linear, Proline-Containing Octalipopeptide from Pseudomonas sp. SH-C52, Motivated by Genome Mining;
J. Nat. Prod. 2021, 84, 101-109. -
C. Heim, S. Maiwald, C. Steinebach, M. K. Collins, J. Strope, C. H. Chau, W. D. Figg, M. Gütschow, M. D. Hartmann;
On the Correlation of Cereblon Binding, Fluorination and Antiangiogenic Properties of Immunomodulatory Drugs;
Biochem. Biophys. Res. Commun. 2021, 534, 67-72. -
C. Hermes, R. Richarz, D. Wirtz, J. Patt, W. Hanke, S. Kehraus, J. Voss, J. Küppers, T. Ohbayashi, V. Namasivayam, J. Alenfelder, A. Inoue, P. Mergaert, M. Gütschow, C. Müller, E. Kostenis, G. König, M. Crüsemann;
Thioesterase-mediated Side Chain Transesterification Generates Potent Gq Signaling Inhibitor FR900359;
Nat. Commun. 2021, 12, 144.
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M. L. Peach, S. L. Beedie, C. H. Chau, M. K. Collins, S. Markolovic, W. Luo, D. Tweedie, C. Steinebach, N. H. Greig, M. Gütschow, N. Vargesson, M. C. Nicklaus, W. D. Figg;
In Silico Cereblon Binding Analysis of Novel Thalidomide Analogs;
Molecules 2020, 25, 5683. -
A. K. Krome, T. G. Becker, S. Kehraus, A. Schiefer, C. Steinebach, T. Aden, S. J. Frohberger, Á. López Mármol, D. Kapote, R. Jansen, L. Chaverra-Muñoz, M. P. Hübner, K. Pfarr, T. Hesterkamp, M. Stadler, M. Gütschow, G. M. König, A. Hoerauf, K. G. Wagner;
Solubility and Stability Enhanced Oral Formulations for the Anti-Infective Corallopyronin A;
Pharmaceutics 2020, 12, E1105. -
C. Lemke, L. Cianni, C. Feldmann, E. Gilberg, J. Yin, F. dos Reis Rocho, D. de Vita, U. Bartz, J. Bajorath,* C. A. Montanari,* M. Gütschow;*
N-Sulfonyl Dipeptide Nitriles as Inhibitors of Human Cathepsin S: In silico Design, Synthesis and Biochemical Characterization;
Bioorg. Med. Chem. Lett. 2020, 30, 127420. -
M. Gütschow et al.;
Breakthroughs in Medicinal Chemistry: New Targets and Mechanisms, New Drugs, New Hopes–7;
Molecules 2020, 25, 2968. -
S. Kuwahara-Ota, Y. Shimura, C. Steinebach, R. Isa, J. Yamaguchi, D. Nishiyama, Y. Fujibayashi, T. Takimoto-Shimomura, Y. Mizuno, Y. Matsumura-Kimoto, T. Tsukamoto, Y. Chinen, T. Kobayashi, S. Horiike, M. Taniwaki, M. Gütschow, J. Kuroda;
Lenalidomide and Pomalidomide Potently Interfere with Induction of Myeloid-derived Suppressor Cells in Multiple Myeloma;
Br. J. Haematol. 2020, 191, 784-795. -
L. P. Vu, M. Gütschow;
Synthesis and Biological Activities of 4H-3,1-Benzothiazin-4-ones;
Chem. Heterocycl. Compd. 2020, 56, 708-714. -
S. Rivière, C. Vielmuth, C. Ennenbach, A. Abdelrahman, C. Lemke, M. Gütschow, C. E. Müller, D. Menche;
Design, Synthesis and Biological Evaluation of Highly Potent Simplified Archazolids;
ChemMedChem 2020, 15, 1348-1363. -
J. Küppers, T. Benkel, S. Annala, K. Kimura, L. Reinelt, B. K. Fleischmann, E. Kostenis,* M. Gütschow;*
Tetrahydroimidazo[1,2-a]pyrazine Derivatives: Synthesis and Evaluation As Gαq-Protein Ligands;
Chem. Eur. J. 2020, 26, 12615-12623. -
J. Breidenbach, U. Bartz, M. Gütschow;
Coumarin as a Structural Component of Substrates and Probes for Serine and Cysteine Proteases;
Biochim. Biophys. Acta Proteins Proteom. 2020, 1868, 140445. -
C. Steinebach, S. A. Voell, L. P. Vu, A. Bricelj, I. Sosič, G. Schnakenburg, M. Gütschow;
A Facile Synthesis of Ligands for the von Hippel-Lindau E3 Ligase;
Synthesis 2020, 52, 2521-2527. -
C. Steinebach,§ Y. L. D. Ng,§ I. Sosič, C.-S. Lee, S. Chen, S. Lindner, L. P. Vu, A. Bricelj, R. Haschemi, M. Monschke, E. Steinwarz, K. G. Wagner, G. Bendas, J. Luo, M. Gütschow,* J. Krönke;*
Systematic Exploration of Different E3 Ubiquitin Ligases: An Approach Towards Potent and Selective CDK6 Degraders;
§C.S. and Y.L.D.N. contributed equally to this work.
Chem. Sci. 2020, 11, 3474-3486. -
A. Gitlin-Domagalska, D. Dębowski, K. Gucwa, D. Starego, N. Ptaszyńska, A. Sieradzan, A. Karczyńska, S. Samsonov, M. Mangold, M. Gütschow, A. Łęgowska, K. Rolka;
Truncation of Huia versabilis Bowman-Birk inhibitor increases its selectivity, matriptase-1 inhibitory activity and proteolytic stability;
Biochimie 2020, 171-172, 178-186. -
L. Cianni, C. Lemke, E. Gilberg, C. Feldmann, F. Rosini, F. D. R. Rocho, J. F. R. Ribeiro, D. Y. Tezuka, C. D. Lopes, S. de Albuquerque, J. Bajorath, S. Laufer, A. Leitão, M. Gütschow,* C. A. Montanari;*
Mapping the S1 and S1’ Subsites of Cysteine Proteases with New Dipeptidyl Nitrile Inhibitors as Trypanocidal Agents;
PLoS Negl. Trop. Dis. 2020, 14, e0007755. -
S. Scheeff, S. Rivière, J. Ruiz, A. Abdelrahman, A. C. Schulz-Fincke, M. Köse, F. Tiburcy, H. Wieczorek, M. Gütschow, C. E. Müller, D. Menche;
Synthesis of Novel Potent Archazolids: Pharmacology of an Emerging Class of Anticancer Drugs;
J. Med. Chem. 2020, 63, 1684-1698. -
T. Nakamura, K. Harada, T. Kamiya, M. Takizawa, J. Küppers, K. Nakajima, M. Gütschow, T. Kitaguchi, K. Ohta, T. Kato, T. Tsuboi;
Glutamine-induced Signaling Pathways via Amino Acid Receptors in Enteroendocrine L Cell Lines;
J. Mol. Endocrinol. 2020, 64, 133-143. -
E. Pászti-Gere, G. Szombath, M. Gütschow, T. Steinmetzer, A. Székács;
3-Amidinophenylalanine-Derived Matriptase Inhibitors Can Modulate Hepcidin Production in vitro;
Naunyn Schmiedebergs Arch. Pharmacol. 2020, 393, 511-520. -
F. M. Dato, J. M. Neudörfl, M. Gütschow, B. Goldfuss, M. Pietsch;
ω-Quinazolinonylalkyl Aryl Ureas as Reversible Inhibitors of Monoacylglycerol Lipase;
Bioorg. Chem. 2020, 94, 103352. -
J. J. Vanden Eynde, A. A. Mangoni, J. Rautio, J. Leprince, Y. T. Azuma, A. T. García-Sosa, C. Hulme, J. Jampilek, R. Karaman, W. Li, P. A. C. Gomes, D. Hadjipavlou-Litina, R. Capasso, A. Geronikaki, L. Cerchia, J. M. Sabatier, R. Ragno, T. Tuccinardi, A. Trabocchi, J. Y. Winum, F. J. Luque, K. Prokai-Tatrai, M. Spetea, M. Gütschow, I. Kosalec, C. Guillou, M. H. Vasconcelos, G. Kokotos, G. Rastelli, M. E. de Sousa, C. Manera, S. Gemma, S. Mangani, C. Siciliano, S. Galdiero, H. Liu, P. J. H. Scott, C. de los Ríos, L. A. Agrofoglio, S. Collina, R. C. Guedes, D. Muñoz-Torrero;
Breakthroughs in Medicinal Chemistry: New Targets and Mechanisms, New Drugs, New Hopes–6;
Molecules 2020, 25, 119. -
M. Kuschak, V. Namasivayam, M. Rafehi, J. H. Voss, J. Garg, J. G. Schlegel, A. Abdelrahman, S. Kehraus, R. Reher, J. Küppers, K. Sylvester, S. Hinz, M. Matthey, D. Wenzel, B. K. Fleischmann, A. Pfeifer, A. Inoue, M. Gütschow, G. M. König, C. E. Müller;
Cell-permeable High-affinity Tracers for Gq Proteins Provide Structural Insights, Reveal Distinct Binding Kinetics, and Identify Small Molecule Inhibitors;
Br. J. Pharmacol. 2020, 177, 1898-1916.
- C. Lemke, J. Christmann, J. Yin, J. M. Alonso, E. Serrano, M. Chioua, L. Ismaili, M. A. Martínez-Grau, C. D. Beadle, T. Vetman, F. M. Dato, U. Bartz, P. W. Elsinghorst, M. Pietsch, C. E. Müller, I. Iriepa, T. Wille, J. Marco-Contelles,* M. Gütschow;*
Chromenones as Multi-Neurotargeting Inhibitors of Human Enzymes;
ACS Omega 2019, 4, 22161-22168. -
J. Küppers, T. Benkel, S. Annala, G. Schnakenburg, E. Kostenis, M. Gütschow;
BIM-46174 Fragments as Potential Ligands of G Proteins;
Med. Chem. Commun. 2019, 10, 1838-1843. -
A. Braune, M. Gütschow, M. Blaut;
An NADH-dependent Reductase from Eubacterium ramulus Catalyzes the Stereospecific Heteroring Cleavage of Flavanones and Flavanonols;
Appl. Environ. Microbiol. 2019, 85, e1233-19. -
L. Cianni, C. W. Feldmann, E. Gilberg, M. Gütschow, L. Juliano, A. Leitão, J. Bajorath, C. A. Montanari;
Can Cysteine Protease Cross-Class Inhibitors Achieve Selectivity?
J. Med. Chem. 2019, 62, 10497-10525. -
A. A. Mangoni, J. J. Vanden Eynde, J. Jampilek, D. Hadjipavlou-Litina, H. Liu, J. Reynisson, M. E. Sousa, P. A. Gomes, K. Prokai-Tatrai, T. Tuccinardi, J. M. Sabatier, F. J. Luque, J. Rautio, R. Karaman, M. H. Vasconcelos, S. Gemma, S. Galdiero, C. Hulme, S. Collina, M. Gütschow, G. Kokotos, C. Siciliano, R. Capasso, L. A. Agrofoglio, R. Ragno, D. Muñoz-Torrero;
Breakthroughs in Medicinal Chemistry: New Targets and Mechanisms, New Drugs, New Hopes–5;
Molecules 2019, 24, 2415. -
C. Steinebach, I. Sosič, S. Lindner, A. Bricelj, F. Kohl, Y. L. D. Ng, M. Monschke, K. G. Wagner, J. Krönke, M. Gütschow;
A MedChem Toolbox for Cereblon-directed PROTACs;
Med. Chem. Comm. 2019, 10, 1034-1041. -
J. Schwenck, A. Maurer, B. Fehrenbacher, R. Mehling, P. Knopf, N. Mucha, D. Haupt, K. Fuchs, C. M. Griessinger, D. Bukala, J. Holstein, M. Schaller, I. Gonzalez Menendez, K. Ghoreschi, L. Quintanilla-Martinez, M. Gütschow, S. Laufer, T. Reinheckel, M. Röcken, H. Kalbacher, B. J. Pichler, M. Kneilling;
Cysteine-type Cathepsins Promote the Effector Phase of Acute Cutaneous Delayed-type Hypersensitivity Reactions;
Theranostics 2019, 9, 3903-3917. -
S. Lindner,§ C. Steinebach,§ H. Kehm, M. Mangold, M. Gütschow, J. Krönke;
Chemical Inactivation of the E3 Ubiquitin Ligase Cereblon by Pomalidomide-based Homo-PROTACs;
§S.L. and C.S. contributed equally to this work.
J. Vis. Exp. 2019, 147, e59472. -
M. Laube, M. Frizler, R. Wodtke, C. Neuber, B. Belter, T. Kniess, M. Bachmann, M. Gütschow, J. Pietzsch, R. Löser;
Synthesis and Preliminary Radiopharmacological Characterisation of an 11C-Labelled Azadipeptide nitrile as Potential PET Tracer for Imaging of Cysteine Cathepsins;
J. Labelled Comp. Radiopharm. 2019, 62, 448-459. -
C. Steinebach,§ H. Kehm,§ S. Lindner, L. P. Vu, S. Köpff, Á. López Mármol, C. Weiler, K. G. Wagner, M. Reichenzeller, J. Krönke,* M. Gütschow;*
PROTAC-mediated Crosstalk Between E3 Ligases;
§C.S. and H.K. contributed equally to this work.
Chem. Commun. 2019, 55, 1821-1824. -
E. Gilberg, M. Gütschow, J. Bajorath;
Promiscuous Ligands from Experimentally Determined Structures, Binding Conformations, and Protein Family Dependent Interaction Hotspots;
ACS Omega 2019, 4, 1729-1737. -
A. A. Mangoni, C. Guillou, J. J. Vanden Eynde, C. Hulme, J. Jampilek, W. Li, K. Prokai-Tatrai, J. Rautio, S. Collina, T. Tuccinardi, M. E. Sousa, J. M. Sabatier, S. Galdiero, R. Karaman, G. Kokotos, G. Torri, F. J. Luque, M. H. Vasconcelos, D. Hadjipavlou-Litina, C. Siciliano, M. Gütschow, R. Ragno, P. A. Gomes, L. A. Agrofoglio, D. Muñoz-Torrero;
Breakthroughs in Medicinal Chemistry: New Targets and Mechanisms, New Drugs, New Hopes–4;
Molecules 2019, 24, 130. -
J. Küppers, M. Hympánová, T. Keuler, A. J. Schneider, G. Schnakenburg, M. Gütschow;
Transformation of the Carboxyl Group of an Amino Acid to Variously Substituted Imidazoles through a Davidson-type Heterocyclization;
Synthesis 2019, 51, 1961-1068. -
J. Schmitz,§ E. Gilberg,§ R. Löser, J. Bajorath, U. Bartz, M. Gütschow;
Cathepsin B: Active Site Mapping with Peptidic Substrates and Inhibitors;
§J.S. and E.G. contributed equally to this work.
Bioorg. Med. Chem. 2019, 27, 1-15.
- A. Gitlin-Domagalska, M. Mangold, D. Dębowski, A. Łęgowska, M. Gütschow, K. Rolka;
Matriptase-2: Monitoring and Inhibiting its Proteolytic Activity;
Future Med. Chem. 2018, 10, 2745-2761. -
K. Krebs, E. Pfeil, K. Simon, M. Grundmann, F. Häberlein, O. Bautista-Aguilera, M. Gütschow, C. David Weaver, B. Fleischmann, E. Kostenis;
Label-free Whole Cell Biosensing for High-throughput Discovery of Activators and Inhibitors Targeting GIRK Channels;
ACS Omega 2018, 3, 14814-14823. -
C. Steinebach,§ S. Lindner,§ N. D. Udeshi, D. C. Mani, H. Kehm, S. Köpff, S. A. Carr, M. Gütschow,* J. Krönke;*
Homo-PROTACs for the Chemical Knockdown of Cereblon;
§C.S. and S.L. contributed equally to this work.
ACS Chem. Biol. 2018, 13, 2771-2782. -
C. Steinebach, A. Ambrożak, S. Dosa, S. L. Beedie, J. D. Strope, G. Schnakenburg, W. D. Figg, M. Gütschow;
Synthesis, Structural Characterization and Antiangiogenic Activity of Polyfluorinated Benzamides;
ChemMedChem 2018, 13, 2010-2089. -
F. M. Dato, M. Sheikh, R. Z. Uhl, A. W. Schüller, M. Steinkrüger, P. Koch, J. M. Neudörfl, M. Gütschow, B. Goldfuss, M. Pietsch;
ω-Phthalimidoalkyl Aryl Ureas as Potent and Selective Inhibitors of Cholesterol Esterase;
ChemMedChem 2018, 13, 1833-1847. -
A. A. Mangoni, T. Tuccinardi, S. Collina, J. J. Vanden Eynde, D. Muñoz-Torrero, R. Karaman, C. Siciliano, M. E. de Sousa, K. Prokai-Tatrai, J. Rautio, C. Guillou, M. Gütschow, S. Galdiero, H. Liu, L. A. Agrofoglio, J. M. Sabatier, C. Hulme, G. Kokotos, Q. You, P. A. C. Gomes;
Breakthroughs in Medicinal Chemistry: New Targets and Mechanisms, New Drugs, New Hopes–3;
Molecules 2018, 23, 1596. -
M. Mangold, M. Gütschow, M. Stirnberg;
A Short Peptide Inhibitor as an Activity-Based Probe for Matriptase-2;
Pharmaceuticals 2018, 11, 49. -
C. Breuer,§ C. Lemke,§ J. Schmitz, U. Bartz, M. Gütschow;
Synthesis and Kinetic Evaluation of Ethyl Acrylate and Vinyl Sulfone Derived Inhibitors for Human Cysteine Cathepsins;
§C.B. and C.L. contributed equally to this work.
Bioorg. Med. Chem. Lett. 2018, 28, 2008-2012. -
J. Hochscherf, M. Pietsch, W. Tieu, K. Kuan, A. D. Abell, M. Gütschow, K. Niefind;
Crystal Structure of Highly Glycosylated Human Leukocyte Elastase in Complex with an S2'-site Binding Inhibitor;
Acta Crystallogr. Sect. F, Struct. Biol. Cryst. Commun. 2018, 74, 480-489. -
A. C. Schulz-Fincke, M. Blaut, A. Braune,* M. Gütschow;*
A BODIPY-tagged Phosphono Peptide as Activity-Based Probe for Human Leukocyte Elastase;
ACS Med. Chem. Lett. 2018, 9, 345-350. -
A. C. Schulz-Fincke, A. S. Tikhomirov, A. Braune, T. Girbl, E. Gilberg, J. Bajorath, M. Blaut, S. Nourshargh, M. Gütschow;
Design of an Activity-Based Probe for Human Neutrophil Elastase: Implementation of the Lossen Rearrangement to Induce Förster Resonance Energy Transfers;
Biochemistry 2018, 57, 742-752. -
E. Gilberg, M. Gütschow, J. Bajorath;
X-ray Structures of Target-Ligand Complexes Containing Compounds with Assay Interference Potential;
J. Med. Chem. 2018, 61, 1276-1284. -
D. Muñoz-Torrero, A. A. Mangoni, H. Liu, C. Hulme, J. Rautio, R. Karaman, M. E. de Sousa, K. Prokai-Tatrai, J. M. Sabatier, C. Siciliano, F. J. Luque, G. Kokotos, R. Ragno, S. Collina, C. Guillou, M. Gütschow, L. A. Agrofoglio;
Breakthroughs in Medicinal Chemistry: New Targets and Mechanisms, New Drugs, New Hopes–2;
Molecules 2018, 23, 65. -
A. Kranawetvogl, J. Küppers, M. Siegert, M. Gütschow, F. Worek, H. Thiermann, P. W. Elsinghorst, H. John;
Bioanalytical Verification of V-type Nerve Agent Exposure: Simultaneous Detection of Phosphonylated Tyrosines and Cysteine-containing Disulfide-adducts Derived from Human Albumin;
Anal. Bioanal. Chem. 2018, 410, 1463-1474. -
D. S. Redka, M. Gütschow, S. Grinstein, J. Canton;
Differential Ability of Pro-inflammatory and Anti-inflammatory Macrophages to Perform Macropinocytosis;
Mol. Biol. Cell 2018, 29, 53-65. -
C. Mahony, S. McMenemy, A. J. Rafipay, S. L. Beedie, L. R. Fraga, M. Gütschow, W. D. Figg, L. Erskine, N. Vargesson;
CPS49-Induced Neurotoxicity does not Cause Limb Patterning Anomalies in Developing Chicken Embryos;
J. Anat. 2018, 232, 568-574.
- A. Gitlin-Domagalska, D. Dębowski, A. Łęgowska, M. Stirnberg, J. Okońska, M. Gütschow, K. Rolka;
Design and Chemical Syntheses of Potent Matriptase-2 Inhibitors Based on Trypsin Inhibitor SFTI-1 Isolated from Sunflower Seeds;
Biopolymers 2017, 108(6). doi: 10.1002/bip.23031. -
D. Muñoz-Torrero, A. A. Mangoni, C. Guillou, S. Collina, J. J. Vanden Eynde, J. Rautio, G. M. Keserű, C. Hulme, K. Chibale, F. J. Luque, R. Karaman, M. Gütschow, H. Liu;
Breakthroughs in Medicinal Chemistry: New Targets and Mechanisms, New Drugs, New Hopes;
Molecules 2017, 22, 743. -
S. Kayastha, D. Horvath, E. Gilberg, M. Gütschow, J. Bajorath, A. Varnek;
Privileged Structural Motif Detection and Analysis using Generative Topographic Maps;
J. Chem. Inf. Model. 2017, 57, 1218-1232. -
D. Häußler,§ A.-C. Schulz-Fincke,§ A.-M. Beckmann, A. Keils, E. Gilberg, M. Mangold, J. Bajorath, M. Stirnberg, T. Steinmetzer, M. Gütschow;
A Fluorescent-labeled Phosphono Bisbenzguanidine as Activity-based Probe for Matriptase;
§D.H. and A.C.S.F. contributed equally to this work.
Chem. Eur. J. 2017, 23, 5205-5209. -
A. M. Kanarek, A. Wagner, J. Küppers, M. Gütschow, R. Postina, E. Kojro;
Crosstalk between Angiotensin and the Non-Amyloidogenic Pathway of Alzheimer's Amyloid Precursor Protein;
FEBS J. 2017, 284, 742-753. -
A. Kranawetvogl, J. Küppers, M. Gütschow, F. Worek, H. Thiermann, P. W. Elsinghorst, H. John;
Identification of Novel Disulfide Adducts Between the Thiol Containing Leaving Group of the Nerve Agent VX and Cysteine Containing Tripeptides Derived from Human Serum Albumin;
Drug Test. Anal. 2017, 9, 1192-1203. -
D. Lorendeau, L. Dury, R. Nasr, A. Boumendjel, E. Teodori, M. Gütschow, P. Falson, A. Di Pietro, H. Baubichon-Cortay;
MRP1-Dependent Collateral Sensitivity of Multidrug-Resistant Cancer Cells: Identifying Selective Modulators Inducing Cellular Glutathione Depletion;
Curr. Med. Chem. 2017, 24, 1186-1213. -
P. Hufendiek, S. S. M. Stölben, S. Kehraus, N. Merten, H. Harms, M. Crüsemann, I. Arslan, M. Gütschow, T. Schneider, G. M. König;
Biosynthetic Studies on Acetosellin and Structure Elucidation of a New Acetosellin Derivative;
Planta Med. 2017, 83, 1044-1052. -
T. Schirmeister, J. Schmitz, S. Jung, T. Schmenger, R. L. Krauth-Siegel, M. Gütschow;
Evaluation of Dipeptide Nitriles as Inhibitors of Rhodesain, a Major Cysteine Protease of Trypanosoma brucei;
Bioorg. Med. Chem. Lett. 2017, 27, 45-50. -
N. Böhringer, M. Gütschow, G. M. König, T. F. Schäberle;
Phileucin - A Cyclic Dipeptide Similar to Phevalin (Aureusimine B) from Streptomyces coelicolor M1146;
Nat. Prod. Commun. 2017, 12, 107-109.
- A. Ambrozak, C. Steinebach, E. R. Gardner, S. L. Beedie, G. Schnakenburg, W. D. Figg, M. Gütschow;
Synthesis and Antiangiogenic Properties of Tetrafluorophthalimido and Tetrafluorobenzamido Barbituric Acids;
ChemMedChem 2016, 11, 2621-2629. -
A. Braune, W. Engst, P. W. Elsinghorst, N. Furtmann, J. Bajorath, M. Gütschow, M. Blaut;
Chalcone Isomerase from Eubacterium ramulus Catalyzes the Ring Contraction of Flavanonols;
J. Bacteriol. 2016, 198, 2965-2974. -
S. Thiede, P. Wosniok, D. Herkommer, A. C. Schulz-Fincke, M. Gütschow, D. Menche;
Total Synthesis of Leupyrrin B1: a Potent Inhibitor of Human Leukocyte Elastase;
Org. Lett. 2016, 18, 3964-3967. -
J. Küppers, A. C. Schulz-Fincke, J. Palus, M. Giurg, J. Skarżewski, M. Gütschow;
Convergent Synthesis of two Fluorescent Ebselen-Coumarin Heterodimers;
Pharmaceuticals 2016, 9, 43. -
A.-M. Beckmann, E. Gilberg, S. Gattner, T. L. Huang, J. J. Vanden Eynde, A. Mayence, J. Bajorath, M. Stirnberg, M. Gütschow;
Evaluation of Bisbenzamidines as Inhibitors for Matriptase-2;
Bioorg. Med. Chem. Lett. 2016, 26, 3741-3745. -
A.-M. Beckmann, K. Glebov, J. Walter, O. Merkel, M. Mangold, F. Schmidt, C. Becker-Pauly, M. Gütschow, M. Stirnberg;
The intact Kunitz Domain Protects the Amyloid Precursor Protein from Being Processed by Matriptase-2;
Biol. Chem. 2016, 397, 777-790. -
J. Canton, D. Schlam, C. Breuer, M. Gütschow, M. Glogauer, S. Grinstein;
Calcium-sensing Receptors Signal Constitutive Macropinocytosis and Facilitate the Uptake of NOD2 Ligands in Macrophages;
Nat. Commun. 2016, 7, 11284. -
D. Häußler, M. Mangold, N. Furtmann, A. Braune, M. Blaut, J. Bajorath, M. Stirnberg, M. Gütschow;
Phosphono Bisbenzguanidines as Irreversible Dipeptidomimetic Inhibitors and Activity-based Probes of Matriptase-2;
Chem. Eur. J. 2016, 22, 8525-8535. -
C. Steinebach, A. C. Schulz-Fincke, G. Schnakenburg, M. Gütschow;
In Situ Generation and Trapping of Thioimidates: An Intermolecular Tandem Reaction to 4-Acylimino-4H-3,1-benzothiazines;
RSC Adv. 2016, 6, 15430-15440. -
P. G. Roydeva,§ A.-M. Beckmann,§ M. Stirnberg, J. Cesar, D. Kikelj, J. Ilaš, M. Gütschow;
3,1-Benzothiazines, 1,4-Benzodioxines and 1,4-Benzoxazines as Inhibitors of Matriptase-2: Outcome of a Focused Screening Approach;
§P.G.R. and A.M.B. contributed equally to this work.
Pharmaceuticals 2016, 9, 2. -
J. Schmitz, T. Li, U. Bartz, M. Gütschow;
Cathepsin B Inhibitors: Combining Dipeptide Nitriles with an Occluding Loop Recognition Element by Click Chemistry;
ACS Med. Chem. Lett. 2016, 7, 211-216 (Featured Letter). -
A.-M. Beckmann, E. Maurer, V. Lülsdorff, A. Wilms, N. Furtmann, J. Bajorath, M. Gütschow, M. Stirnberg;
En Route to New Therapeutic Options for Iron Overload Diseases: Matriptase-2 as a target for Kunitz-type inhibitors;
ChemBioChem 2016, 17, 595-604. -
D. Häußler, M. Gütschow;
Fluorescently Labeled Amino Acids as Building Blocks for Bioactive Molecules;
Synthesis 2016, 48, 245-255.
ref. https://www.thieme.de/de/thieme-chemistry/neue-fluoreszenzmarkierte-aminosaeuren-91222.htm. -
N. Furtmann, D. Häußler, T. Scheidt, M. Stirnberg, T. Steinmetzer, J. Bajorath, M. Gütschow;
Limiting the Number of Potential Binding Modes by Introducing Symmetry into Ligands: Structure-Based Design of Inhibitors for Trypsin-Like Serine Proteases;
Chem. Eur. J. 2016, 22, 610-625. -
M. D. Mertens, A. Bierwisch, T. Li, M. Gütschow, H. Thiermann, T. Wille, P. W. Elsinghorst;
A Novel Fluorogenic Probe for the Investigation of Free Thiols: Application to Kinetic Measurements of Acetylcholinesterase Activity;
Toxicol. Lett. 2016, 244, 161-166.
- F. Kohl, J. Schmitz, N. Furtmann, A. C. Schulz-Fincke, M. D. Mertens, J. Küppers, M. Benkhoff, E. Tobiasch, U. Bartz, J. Bajorath, M. Stirnberg, M. Gütschow;
Design, Characterization and Cellular Uptake Studies of Fluorescence-labeled Prototypic Cathepsin Inhibitors;
Org. Biomol. Chem. 2015, 13, 10310-10323. -
S. L. Beedie, C. J. Peer, S. T. Pisle, E. R. Gardner, C. Mahony, S. Barnett, A. Ambrozak, M. Gütschow, C. H. Chau, N. Vargesson, W. D. Figg;
Anti-Cancer Properties of a Novel Class of Tetrafluorinated Thalidomide Analogs;
Mol. Cancer Ther. 2015, 14, 2228-2237. -
D. Häußler, T. Scheidt, M. Stirnberg, T. Steinmetzer, M. Gütschow;
A Bisbenzamidine Phosphonate as a Janus-faced Inhibitor for Trypsin-like Serine Proteases;
ChemMedChem 2015, 10, 1641-1646. -
P. A. Ottersbach, G. Schnakenburg, M. Gütschow;
Atropisomerism in Azadipeptides: Evaluation of N1-Methylation and Thioamide Introduction;
Tetrahedron Lett. 2015, 56, 4889-4891. -
F. Jäckle, F. Schmidt, R. Wichert, P. Arnold, J. Prox, M. Mangold, A. Ohler, C. U. Pietrzik, T. Koudelka, A. Tholey, M. Gütschow, M. Stirnberg, C. Becker-Pauly;
Metalloprotease Meprin β is Activated by Transmembrane Serine Protease Matriptase-2 at the Cell Surface thereby Enhancing APP Shedding;
Biochem. J. 2015, 470, 91-103. -
A. Gitlin, D. Dębowski, N. Karna, A. Łęgowska, M. Stirnberg, M. Gütschow, K. Rolka;
Inhibitors of Matriptase-2 Based on Trypsin Inhibitor SFTI-1;
ChemBioChem 2015, 16, 1601-1607. -
N. Furtmann, Y. Hu, M. Gütschow, J. Bajorath;
Identification of Interaction Hotspots in Structures of Drug Targets on the Basis of Three-Dimensional Activity Cliff Information;
Chem. Biol. Drug Des. 2015, 86, 1458-1465. -
J. Schmitz, N. Furtmann, M. Ponert, M. Frizler, R. Löser, U. Bartz, J. Bajorath, M. Gütschow;
Active Site Mapping of Human Cathepsin F with Dipeptide Nitrile Inhibitors;
ChemMedChem 2015, 10, 1365-1377. -
N. Furtmann, Y. Hu, M. Gütschow, J. Bajorath;
Identification and Analysis of Currently Available High-Confidence Three-Dimensional Activity Cliffs;
RSC Adv. 2015, 5, 43660-43668. -
D. Häußler, M. Gütschow;
Synthesis of a Fluorescent-labeled Bisbenzamidine Containing the Central (6,7-Dimethoxy-4-coumaryl)alanine Building Block;
Heteroatom Chem. 2015, 26, 367-373. -
N. Furtmann, E. Gilberg, N. Spütz, M. Gütschow;
Oxidation of Disulfides to Taurine and Sulfanilic Acid Derivatives;
Synthesis 2015, 47, 2609-2616. -
M. Stirnberg, E. Maurer, K. Arenz, A. Babler, W. Jahnen-Dechent, M. Gütschow;
Cell Surface Serine Protease Matriptase-2 Suppresses Fetuin-A/AHSG-Mediated Induction of Hepcidin;
Biol. Chem. 2015, 396, 81-93. -
J. Schmitz,§ A.-M. Beckmann,§ A. Dudic, T. Li, R. Sellier, U. Bartz, M. Gütschow;
3-Cyano-3-aza-beta-amino Acid Derivatives as Inhibitors of Human Cysteine Cathepsins;
§J.S. and A.M.B contributed equally to this work.
ACS Med. Chem. Lett. 2014, 5, 1076-1081 (Featured Letter). -
A. L. Schmitz, R. Schrage, E. Gaffal, T. H. Charpentier, J. Wiest, G. Hiltensperger, J. Morschel, S. Hennen, D. Häußler, V. Horn, D. Wenzel, M. Grundmann, K. Büllesbach, R. Schröder, H. H. Brewitz, J. Schmidt, J. Gomeza, C. Galé, B. K. Fleischmann, T. Tüting, D. Imhof, D. Tietze, M. Gütschow, U. Holzgrabe, J. Sondek, T. K. Harden, K. Mohr, E. Kostenis;
A Cell-Permeable Inhibitor to Trap Gaq Proteins in the Empty Pocket Conformation;
Chem. Biol. 2014, 21, 890-902. -
K. C. Chua, M. Pietsch, X. Zhang, S. Hautmann, H. Y. Chan, J. B. Bruning, M. Gütschow, A. D. Abell;
Macrocyclic Protease Inhibitors with Reduced Peptide Character;
Angew. Chem. Int. Ed. 2014, 53, 7828-7831. -
K. C. Chua, M. Pietsch, X. Zhang, S. Hautmann, H. Y. Chan, J. B. Bruning, M. Gütschow, A. D. Abell;
Macrocyclic Protease Inhibitors with Reduced Peptide Character;
Angew. Chem. 2014, 126, 7962-7965. -
M. D. Mertens, M. Gütschow;
Clickable Coumarins as Fluorescent Labels for Amino Acids;
Synthesis 2014, 2191-2200. -
V. Konya, S. Blättermann, K. Jandl, W. Platzer, P. A. Ottersbach, G. Marsche, M. Gütschow, E. Kostenis, A. Heineman;
A Biased Non-Gαi OXE-R Antagonist Demonstrates that Gαi Protein Subunit is not Directly Involved in Neutrophil, Eosinophil and Monocyte Activation by 5-oxo-ETE;
J. Immunol. 2014, 192, 4774-4782. -
S. Aslam, S. Zaib, M. Ahmad, J. M. Gardiner, A. Ahmad, A. Hameed, N. Furtmann, M. Gütschow, J. Bajorath, J. Iqbal;
Novel Structural Hybrids of Pyrazolobenzothiazines with Benzimidazoles as Cholinesterase Inhibitors;
Eur. J. Med. Chem. 2014, 78, 106-117. -
M. D. Mertens, J. Schmitz, M. Horn, N. Furtmann, J. Bajorath, M. Mareš, M. Gütschow;
A Coumarin-Labeled Vinyl Sulfone as Tripeptidomimetic Activity-Based Probe for Cysteine Cathepsins;
ChemBioChem 2014, 15, 955-959. -
G. C. Muscia, S. Hautmann, G. Y. Buldain, S. E. Asís, M. Gütschow;
Synthesis and Evaluation of 2-(1H-Indol-3-yl)-4-phenylquinolines as Inhibitors of Cholesterol Esterase;
Bioorg. Med. Chem. Lett. 2014, 24, 1545-1549. -
M. D. Mertens, S. Hinz, C. E. Müller, M. Gütschow;
Alkynyl-Coumarinyl Ethers as MAO-B Inhibitors;
Bioorg. Med. Chem. 2014, 22, 1916-1928. -
M. Wysocka, N. Gruba N, A. Miecznikowska, J. Popow-Stellmaszyk, M. Gütschow, M. Stirnberg, N. Furtmann, J. Bajorath, A. Lesner, K. Rolka;
Substrate Specificity of Human Matriptase-2;
Biochimie 2014, 97, 121-127. -
A. K. Orlovius, S. Guddat, M. Gütschow, M. Thevis, W. Schänzer;
In Vitro Synthesis and Characterisation of three Fenoterol Sulfoconjugates Detected in Fenoterol Post-Administration Urine Samples;
Anal. Bioanal. Chem. 2013, 405, 9477-9487. -
M. D. Mertens, M. Pietsch, G. Schnakenburg, M. Gütschow;
Regioselective Sulfonylation and N- to O-Sulfonyl Migration of Quinazolin-4(3H)-ones and Analogous Thienopyrimidin-4(3H)-ones;
J. Org. Chem. 2013, 78, 8966-8979. -
F. Lohr, I. Jenniches, M. Frizler, M. Meehan, M. Sylvester, A. Schmitz, M. Gütschow, P. C. Dorrestein, G. M. König, T. F. Schäberle;
α,β -> β,γ Double Bond Migration in Corallopyronin A Biosynthesis;
Chem. Sci. 2013, 4, 4175-4180. -
M. D. Mertens, M. Gütschow;
Synthesis and Evaluation of Two Coumarin-Type Derivatization Reagents for Fluorescence Detection of Chiral Amines and Chiral Carboxylic Acids;
Chirality 2013, 25, 957-964. -
M. Frizler, I. V. Yampolsky, M. S. Baranov, M. Stirnberg, M. Gütschow;
Chemical Introduction of the Green Fluorescence: Imaging of Cysteine Cathepsins by an Irreversibly Locked GFP Fluorophore;
Org. Biomol. Chem. 2013, 11, 5913-5921. -
M. Hussein, M. Bettio, A. Schmitz, J. S. Hannam, J. Theis, G. Mayer, S. Dosa, M. Gütschow, M. Famulok;
Cyplecksins Are Covalent Inhibitors of the Pleckstrin Homology Domain of Cytohesin;
Angew. Chem. Int. Ed. 2013, 52, 9529-9533. -
M. Hussein, M. Bettio, A. Schmitz, J. S. Hannam, J. Theis, G. Mayer, S. Dosa, M. Gütschow, M. Famulok;
Kovalente Inhibition der Pleckstrin-Homologiedomäne von Cytohesinen durch Cyplecksine;
Angew. Chem. 2013, 125, 9707-9712. -
A. Stößel, M. Schlenk, S. Hinz, P. Küppers, J. Heer, M. Gütschow,* C. E. Müller;*
Dual Targeting of Adenosine A2A Receptors and Monoamine Oxidase B by 4H-3,1-Benzothiazin-4-ones;
J. Med. Chem. 2013, 56, 4580-4596. -
R. Löser, R. Bergmann, M. Frizler, B. Mosch, L. Dombrowski, M. Kuchar, J. Steinbach, M. Gütschow, J. Pietzsch;
Synthesis and Radiopharmacological Characterisation of a Fluorine-18 Labelled Azadipeptide Nitrile as Potential PET Tracer for in vivo Imaging of Cysteine Cathepsins;
ChemMedChem 2013, 8, 1330-1344. -
A. D. Pehere, M. Pietsch, M. Gütschow, P. M. Neilsen, D. F. Callen, D. S. Pedersen, S. Nguyen, M. J. Sykes, O. Zvarec, A. D. Abell;
Synthesis and Extended Activity of Triazole-Containing Macrocyclic Protease Inhibitors;
Chem. Eur. J. 2013, 19, 7975-7981. -
C. Mohn, H.-G. Häcker, R. Hilger, M. Gütschow, U. Jaehde;
Defining the Role of MRP-Mediated Efflux and Glutathione in Detoxification of Oxaliplatin;
Pharmazie 2013, 68, 622-627. -
P. A. Ottersbach, J. Schmitz, G. Schnakenburg, M. Gütschow;
An Access to Aza-Freidinger Lactams and E-Locked Analogs;
Org. Lett. 2013, 15, 448-451. -
E. Maurer, M. Gütschow, M. Stirnberg;
Hepatocyte Growth Factor Activator Inhibitor Type 2 (HAI-2) Modulates Hepcidin Expression by Inhibiting Cell Surface Protease Matriptase-2;
Biochem. J. 2013, 450, 583-593. -
M. Stirnberg, M. Gütschow;
Matriptase-2, a Regulatory Protease of Iron Homeostasis: Possible Substrates, Cleavage Sites and Inhibitors;
Curr. Pharm. Des. 2013, 19, 1052-1061. -
M. Frizler, M. D. Mertens, M. Gütschow;
Fluorescent Nitrile-Based Inhibitors of Cysteine Cathepsins;
Bioorg. Med. Chem. Lett. 2012, 22, 7715-7718. -
S. Dosa, M. Stirnberg, V. Lülsdorff, D. Häußler, E. Maurer, M. Gütschow;
Active Site Mapping of Trypsin, Thrombin and Matriptase-2 by Sulfamoyl Benzamidines;
Bioorg. Med. Chem. 2012, 20, 6489-6505. -
M. F. Elsebai, M. Nazir, S. Kehraus, E. Egereva, K. N. Ioset, L. Marcourt, D. Jeannerat, M. Gütschow, J. L. Wolfender, G. M. König;
Novel Polyketide Skeletons from the Marine Alga-Derived Fungus Coniothyrium cereale;
Eur. J. Org. Chem. 2012, 6197-6203. -
R. Löser, M. Nieger, M. Gütschow;
Synthesis and Crystal Structure of Benzyl [(1S)-1-(5-amino-1,3,4-oxadiazol-2-yl)-2-phenylethyl]carbamate;
Crystals 2012, 2, 1201-1209. -
M. Frizler, J. Schmitz, A. C. Schulz-Fincke, M. Gütschow;
Selective Nitrile Inhibitors to Modulate the Proteolytic Synergism of Cathepsins S and F;
J. Med. Chem. 2012, 55, 5982-5986. -
P. A. Ottersbach, G. Schnakenburg, M. Gütschow;
Induction of Chirality: Experimental Evidence of Atropisomerism in Azapeptides;
Chem. Commun. 2012, 48, 5772-5774. -
Y. Hu, N. Furtmann, M. Gütschow, J. Bajorath;
Systematic Identification and Classification of Three-Dimensional Activity Cliffs;
J. Chem. Inf. Model. 2012, 52, 1490-1498. -
M. Hammami, E. Rühmann, E. Maurer, A. Heine, M. Gütschow, G. Klebe, T. Steinmetzer;
New 3-Amidinophenylalanine Derived Inhibitors of Matriptase;
Med. Chem. Commun. 2012, 3, 807-813. -
L. Hroch, M. Hrušková, J. Schmitz, G. Schnakenburg, M. Gütschow;
3,5,5-Trisubstituted Hydantoins From Activated (Benzyloxycarbonylamino)malonic Acids;
Synthesis 2012, 1907-1914. -
C. Almeida, Y. Hemberger, S. M. Schmitt, S. Bouhired, L. Natesan, S. Kehraus, K. Dimas, M. Gütschow, G. Bringmann, G. M. König;
Marilines A-C, Novel Phthalimidines from the Sponge-Derived Fungus Stachylidium sp.;
Chem. Eur. J. 2012, 18, 8827-8834. -
S. Blättermann, L. Peters, P. A. Ottersbach, A. Bock, V. Konya, C. D. Weaver, A. Gonzalez, R. Schröder, R. Tyagi, P. Luschnig, J. Gäb, S. Hennen, T. Ulven, L. Pardo, K. Mohr, M. Gütschow, A. Heinemann, E. Kostenis;
A biased ligand for OXE-R uncouples Galpha and Gbetagamma signaling within a heterotrimer;
Nat. Chem. Biol. 2012, 8, 631-638. -
M. Gütschow,* M. Schlenk, J. Gäb, M. Paskaleva, W. Alnouri, S. Scolari, J. Iqbal, C. E. Müller;*
Benzothiazinones – A Novel Class of Adenosine Receptor Antagonists Structurally Unrelated to Xanthine and Adenine Derivatives;
J. Med. Chem. 2012, 55, 3331-3341. -
E. Maurer, M. Gütschow, M. Stirnberg;
Matriptase-2 (TMPRSS6) is Directly Up-regulated by Hypoxia Inducible Factor-1: Identification of a Hypoxia Responsive Element in the TMPRSS6 Promoter Region;
Biol. Chem. 2012, 393, 535-540. -
E. Maurer, M. T. Sisay, M. Stirnberg, T. Steinmetzer, J. Bajorath, M. Gütschow;
Insights into Matriptase-2 Substrate Binding and Inhibition Mechanisms by Analyzing Active Site-Mutated Variants;
ChemMedChem 2012, 7, 68-72. -
P. W. Elsinghorst, T. Cavlar, A. Müller, A. Braune, M. Blaut, M. Gütschow;
The Thermal and Enzymatic Taxifolin–Alphitonin Rearrangement;
J. Nat. Prod. 2011, 74, 2243-2249. -
S. Heng, W. Tieu, S. Hautmann, K. Kuan, D. S. Pedersen, M. Pietsch, M. Gütschow, A. D. Abell;
New cholesterol esterase inhibitors based on rhodanine and thiazolidinedione scaffolds;
Bioorg. Med. Chem. 2011, 19, 7453-7463. -
M. K. Parr, C. Blatt, O. Zierau, C. Hess, M. Gütschow, G. Fußhöller, G. Opfermann, W. Schänzer, P. Diel;
Endocrine Characterization of the Designer Steroid Methyl-1-Testosterone - Investigations on Tissue-Specific Anabolic-Androgenic Potency, Side Effects and Metabolism;
Endocrinology 2011, 152, 4718-4728. -
S. Fustero, A. C. Cuñat, S. Flores, C. Báez, J. Oliver, M. Cynamon, M. Gütschow, M. D. Mertens, O. Delgado, G. Tresadern, A. Trabanco;
Design, Synthesis and Biological Evaluation of Novel Fluorinated Ethanolamines;
Chem. Eur. J. 2011, 17, 14772-14784. -
M. F. Elsebai, L. Natesan, S. Kehraus, I. E. Mohamed, G. Schnakenburg, F. Sasse, S. Shaaban, M. Gütschow, G. M. König;
HLE-Inhibitory Alkaloids with a Polyketide Skeleton from the Marine-Derived Fungus Coniothyrium cereale;
J. Nat. Prod. 2011, 74, 2282-2285. -
M. Frizler, F. Lohr, M. Lülsdorff, M. Gütschow;
Facing the gem-Dialkyl Effect in Enzyme Inhibitor Design: Preparation of Homocycloleucine-Based Azadipeptide Nitriles;
Chem. Eur. J. 2011, 17, 11419-11423. -
H.-G. Häcker, M. T. Sisay, M. Gütschow;
Allosteric Modulation of Caspases;
Pharmacol. Ther. 2011, 132, 180-195. -
D. Meynard, V. Vaja, C. C. Sub, E. Corradini, S. Chen, C. López-Otin, L. Grgurevic, C. C. Hong, M. Stirnberg, M. Gütschow, S. Vukicevic, J. L. Babitt, H. Y. Lin;
Regulation of TMPRSS6 by BMP6 an Iron in Human Cells and Mice;
Blood 2011, 118, 747-756. -
S. Fustero, V. Rodrigo, M. Sánchez-Roselló, C. del Pozo, J. Timoneda, M. Frizler, M. T. Sisay, J. Bajorath, L. P. Calle, F. Javier Cañada, J. Jiménez-Barbero, M. Gütschow;
New Cathepsin Inhibitors to Explore the Fluorophilic Properties of the S2 Pocket of Cathepsin B: Design, Synthesis and Biological Evaluation;
Chem. Eur. J.. 2011, 17, 5256-5260. -
C. M. González Tanarro, M. Gütschow;
Hyperbolic Mixed-Type Inhibition of Acetylcholinesterase by Tetracyclic Thienopyrimidines;
J. Enz. Inhib. Med. Chem. 2011, 26, 350-358. -
P. W. Elsinghorst, W. Härtig, D. Gündisch, K. Mohr, C. Tränkle, M. Gütschow;
A Hydrazide Linker Strategy for Heterobivalent Compounds as Ortho- and Allosteric Ligands of Acetylcholine-Binding Proteins;
Curr. Top. Med. Chem. 2011, 11, 2731-2748. -
S. Dosa, J. Daniels, M. Gütschow;
Biaryl Sulfonamides from O-Acetyl Amidoximes: 1,2,4-Oxadiazole Cyclization under Acidic Conditions;
J. Heterocyclic Chem. 2011, 48, 407-413. -
M. Frizler, F. Lohr, N. Furtmann, J. Kläs, M. Gütschow;
Structural Optimization of Azadipeptide Nitriles Strongly Increases Association Rates and Allows the Development of Selective Cathepsin Inhibitors;
J. Med. Chem. 2011, 54, 396-400. -
M. F. Elsebai, S. Kehraus, U. Lindequist, F. Sasse, S. Shaaban, M. Gütschow, M. Josten, H.-G. Sahl, G. M. König;
Antimicrobial Phenalenone Derivatives From the Marine-Derived Fungus Coniothyrium cereale;
Org. Biomol. Chem. 2011, 9, 802-808. -
H.-G. Häcker, M. Meusel, M. Aschfalk, M. Gütschow;
Solid-Phase Synthesis of Disubstituted N-Acylureas from Resin-Bound Ureas and Acyl Chlorides;
ACS Comb. Sci. 2011, 13, 59-46. -
M. Rodamer, P. W. Elsinghorst, M. Kinzig, M. Gütschow, F. Sörgel;
Development and Validation of a Liquid Chromatography/Tandem Mass Spectrometry Procedure for the Quantification of Sunitinib (SU11248) and Its Active Metabolite, N-Desethyl Sunitinib (SU12662), in Human Plasma: Application to an Explorative Study;
J. Chromatogr. B 2011, 879, 695-706.
-
P. A. Ottersbach, P. W. Elsinghorst, H.-G. Häcker, M. Gütschow;
Direct Formation of Ring-Fused 1,3-Thiazine-2,4-dithiones From Aromatic o-Amino Carboxylic Acids: Observation of a Carbon Disulfide-Mediated Thionation;
Org. Lett. 2010, 12, 3662-3665. -
M. T. Sisay, T. Steinmetzer, M. Stirnberg, E. Maurer, M. Hammami, J. Bajorath, M. Gütschow;
Identification of the First Low Molecular Weight Inhibitors of Matriptase-2;
J. Med. Chem. 2010, 53, 5523-5535. -
M. Stirnberg, E. Maurer, A. Horstmeyer, S. Kolp, S. Frank, T. Bald, K. Arenz, A. Janzer, K. Prager, P. Wunderlich, J. Walter, M. Gütschow;
The Proteolytic Processing of the Serine Protease Matriptase-2: Identification of the Cleavage Sites Required for its Autocatalytic Release from the Cell Surface;
Biochem. J. 2010, 430, 87-95. -
M. F. Elsebai, S. Kehraus, M. Gütschow, G. M. König;
Spartinoxide, a New Enantiomer of A82775C with Inhibitory Activity toward HLE from the Marine-derived Fungus Phaeosphaeria spartinae;
Nat. Prod. Commun. 2010, 5, 1071-1076. -
P. A. Ottersbach, H.-G. Häcker, P. W. Elsinghorst, G. Schnakenburg, M. Gütschow;
1,2-Dihydro-2-thioxo-4H-3,1-benzothiazin-4-one: Formation from Carbon Disulfide and Isatoic Anhydride;
Tetrahedron Lett. 2010, 51, 2727-2729. -
M. Frizler, M. Stirnberg, M. T. Sisay, M. Gütschow;
Development of Nitrile-Based Peptidic Inhibitors of Cysteine Cathepsins;
Curr. Top. Med. Chem. 2010, 10, 294-322. -
W. Härtig, J. Kacza, B.-R. Paulke, J. Grosche, U. Bauer, A. Hoffmann, P. W. Elsinghorst, M. Gütschow;
In Vivo Labelling of Hippocampal beta-Amyloid in Triple-Transgenic Mice with a Fluorescent Acetylcholinesterase Inhibitor Released from Nanoparticles;
Eur. J. Neurosci. 2010, 31, 99-109. -
D. Briel, A. Rybak, C. Kronbach, K. Unverferth,C. M. González Tanarro, M. Gütschow;
Thieno[2,3-d]pyrimidines and –[1,3]Oxazines as Glutamate Antagonists and Investigations on the Inhibitory Potency towards Human Leukocyte Elastase;
J. Heterocyclic Chem. 2010, 47, 634-639. -
D. Stumpfe, M. T. Sisay, M. Frizler, I. Vogt, M. Gütschow, J. Bajorath;
Inhibitors of Cathepsin K and S Identified Using the DynaMAD Virtual Screening Algorithm;
ChemMedChem 2010, 5, 61-64. -
R. Löser, J. Gut, P. J. Rosenthal, M. Frizler, M. Gütschow, K. T. Andrews;
Antimalarial Activity of Azadipeptide Nitriles;
Bioorg. Med. Chem. Lett. 2010, 20, 252-255. -
V. M. Zakharova, O. Brede, M. Gütschow, M. A. Kuznetsov, M. Zibinsky, J. Sieler, B. Schulze;
N,N'-Linked 1,2-Benzisothiazol-3(2H)-one 1,1-Dioxides: Synthesis, Biological Activity and Derived Radicals;
Tetrahedron 2009, 66, 379-384. -
A. K. Orlovius, S. Guddat, M. K. Parr, M. Kohler, M. Gütschow, M. Thevis, W. Schänzer;
Terbutaline Sulfoconjugate: Characterisation and Urinary Excretion Monitored by LC/ESI-MS/MS;
Drug Testing Anal. 2009, 1, 568-575. -
H.-G. Häcker, A. de la Haye, K. Sterz, G. Schnakenburg, M. Wiese, M. Gütschow;
Analogs of a 4-Aminothieno[2,3-d]pyrimidine lead (QB13) As Modulators of P-Glycoprotein Substrate Specificity;
Bioorg. Med. Chem. Lett. 2009, 19, 6102-6105. -
P. W. Elsinghorst, W. Härtig, S. Goldhammer, J. Grosche, M. Gütschow;
A Gorge-Spanning, High-Affinity Cholinesterase Inhibitor to Explore beta-Amyloid Plaques;
Org. Biomol. Chem. 2009, 7, 3940-3946. -
M. F. Elsebai, S. Kehraus, M. Gütschow, G. M. König;
New Polyketides from the Marine-derived Fungus Phaeosphaeria spartinae;
Nat. Prod. Commun. 2009, 4, 1463-1468. -
H.-G. Häcker, S. Leyers, J. Wiendlocha, M. Gütschow, M. Wiese;
Aromatic 2-(Thio)ureidocarboxylic Acids As a New Family of Modulators of Multidrug Resistance-Associated Protein 1: Synthesis, Biological Evaluation, and Structure-Activity Relationships;
J. Med. Chem. 2009, 52, 4586-4595. -
M. T. Sisay, S. Hautmann, C. Mehner, G. M. König, J. Bajorath, M. Gütschow;
Inhibition of Human Leukocyte Elastase by Brunsvicamides A−C, Cyanobacterial Cyclic Peptides;
ChemMedChem 2009, 4, 1425-1429. -
H.-G. Häcker, G. Schnakenburg, W. Hoffbauer, J. Daniels, M. Pietsch, M. Gütschow;
Isopropylammonium Tetrafluorohydrogenphthalate: Structural Characterization and Comparison to Two Related Salts with Different Stoichiometric Ratios;
J. Mol. Struct. 2009, 934, 23-27. -
P. W. Elsinghorst, M. Gütschow;
Synthesis of 2H- and 13C-Labelled Sunitinib and its Primary Metabolite;
J. Labelled Compd. Radiopharm. 2009, 52, 360-365. -
M. Pietsch, L. Christian, T. Inhester, S. Petzold, M. Gütschow;
Kinetics of Inhibition of Acetylcholinesterase in the Presence of Acetonitrile;
FEBS J. 2009, 276, 2292-2307. -
Z. Yunt, K. Reinhardt, M. Engeser, H. M. Dahse, M. Gütschow, T. Bruhn, G. Bringmann, J. Piel;
Cleavage of Four Carbon-Carbon Bonds during Biosynthesis of the Griseorhodin A Spiroketal Pharmacophore;
J. Am. Chem. Soc. 2009, 131, 2297-2305. -
K. Neumann, S. Kehraus, M. Gütschow, G. M. König;
Cytotoxic and HLE-inhibitory Tetramic Acid Derivatives from Marine-derived Fungi;
Nat. Prod. Commun. 2009, 4, 347-354. -
R. Löser, M. Gütschow;
Dipeptide-Derived Nitriles Containing Additional Electrophilic Sites - Potentially Irreversible Inhibitors of Cysteine Proteases;
J. Enz. Inhib. Med. Chem. 2009, 24, 1245-1252. -
H.-G. Häcker, P. W. Elsinghorst, S. Michels, J. Daniels, G. Schnakenburg, M. Gütschow;
2-(Benzoylimino)thiazolidin-4-ones: Formation by an Alternative Ring Closure and Analysis of Rotational Barriers;
Synthesis 2009, 1195-1203. -
H.-G. Häcker, F. Grundmann, F. Lohr, P. A. Ottersbach, J. Zhou, G. Schnakenburg, M. Gütschow;
2-Amino- and 2-Alkylthio-4H-3,1-benzothiazin-4-ones: Synthesis, Interconversion and Enzyme Inhibitory Activities;
Molecules 2009, 14, 378-402. -
M. K. Parr, M. Gütschow, J. Daniels, G. Opfermann, M. Thevis, W. Schänzer;
Identification of Steroid Isoxazole Isomers Marketed as Designer Supplement;
Steroids 2009, 74, 322-328. -
D. Stumpfe, M. Frizler, M. T. Sisay, J. Batista, I. Vogt, M. Gütschow, J. Bajorath;
Hit Expansion through Computational Selectivity Searching;
ChemMedChem 2009, 4, 52-54. -
A. Eilfeld, C. M. González Tanarro, M. Frizler, J. Sieler, B. Schulze, M. Gütschow;
Synthesis and Elastase-Inhibiting Activity of 2-Pyridinyl-isothiazol-3(2H)-one 1,1-Dioxides;
Bioorg. Med. Chem. 2008, 16, 8127-8135. -
C. Mehner, D. Müller, S. Kehraus, S. Hautmann, M. Gütschow, G. M. König;
New Insulapeptolides from the Cyanobacterium Nostoc insulare as Selective and Potent Inhibitors of Human Leukocyte Elastase;
ChemBioChem 2008, 9, 2692-2703. -
S. Leyers, H.-G. Häcker, J. Wiendlocha, M. Gütschow, M. Wiese;
A 4-Aminobenzoic Acid Derivative as Novel Lead for Selective Inhibitors of Multidrug Resistance Associated Proteins;
Bioorg. Med. Chem. Lett. 2008, 18, 4761-4763. -
L. Tan, H. Geppert, M. Sisay, M. Gütschow, J. Bajorath;
Integrating Structure- and Ligand-based Virtual Screening: Comparison of Individual, Parallel, and Fused Molecular Docking and Similarity Search Calculations on Multiple Targets;
ChemMedChem 2008, 3, 1566-1571. -
A. Matthies, T. Clavel, M. Gütschow, W. Engst, D. Haller, M. Blaut, A. Braune;
Conversion of Daidzein and Genistein by a Newly Isolated Anaerobic Bacterium from Mouse Intestine;
Appl. Environ. Microbiol. 2008, 74, 4847-4852. -
R. Löser, M. Frizler, K. Schilling, M. Gütschow;
Azadipeptide Nitriles - Highly Potent and Proteolytically Stable Inhibitors of Papain-Like Cysteine Proteases;
Angew. Chem. Int. Ed. 2008, 47, 4331-4334. -
R. Löser, M. Frizler, K. Schilling, M. Gütschow;
Azadipeptidnitrile - hochpotente und proteolysestabile Inhibitoren Papain-ähnlicher Cysteinproteasen;
Angew. Chem. 2008, 120, 4403-4406. -
P. A. Ottersbach, D. Bolek, E. Lepičová, M. Nieger, M. Gütschow;
Darzens Reaction of 2-Bromo-4,6-dimethoxy-3(2H)-benzofuranone with Aromatic Aldehydes to Form Flavonoids;
J. Heterocyclic Chem. 2008, 45, 1149-1153. -
C. Mehner, D. Müller, A. Krick, S. Kehraus, R. Löser, M. Gütschow, A. Maier, H. H. Fiebig, R. Brun, G. M. König;
A Novel beta-Amino Acid in a Cytotoxic Peptides from the Cyanobacterium Tychonema sp.;
Eur. J. Org. Chem. 2008, 1732-1739. -
V. M. Zakharova, C. M. González Tanarro, M. Gütschow, L. Hennig, J. Sieler, B. Schulze;
Synthesis of N,N'-Linked Bisazaheterocycles with Sulfonamide Structure via Oxidation of S,N-Heteroaromatic cations;
Synthesis 2008, 1133-1141. -
J. Wolf, C. M. González Tanarro, M. Gütschow, J. Sieler, B. Schulze;
Synthesis of 4-(Isothiazol-3-yl)morpholines and 1-(Isothiazol-3-yl)piperazines and their Inhibitory Activity towards Acetylcholinesterase;
Helv. Chim. Acta 2008, 90, 35-45. -
M. Pietsch, H.-G. Häcker, G. Schnakenburg, W. Hoffbauer, M. Nieger, M. Gütschow;
Structural Characterization of Two Salts Derived from Tetrafluorophthalic Acid and Isopropylamine;
J. Mol. Struct. 2008, 878, 131-138. -
P. W. Elsinghorst, J. S. Cieslik, K. Mohr, C. Tränkle, M. Gütschow;
The First Gallamine-Tacrine Hybrid: Design and Characterization at Cholinesterases and the M2 Muscarinic Receptor;
J. Med. Chem. 2007, 50, 5685-5695. -
A. Ambrozak, M. Gütschow;
Preparation of Phthalamic Acid Derivatives and Ring Closure to Phthalimidobarbituric Acids;
J. Heterocyclic Chem. 2007, 44, 1259-1263. -
P. W. Elsinghorst, M. Nieger, M. Gütschow;
6,9-Dichloro-1,2,3,4-tetrahydroacridine;
Acta Crystallogr. E 2007, 63, 1818-1820. -
T. Librowski, M. Kubacka, M. Meusel, S. Scolari, C. E. Müller, M. Gütschow;
Evaluation of Anticonvulsant and Analgesic Effects of Benzyl- and Benzhydryl Ureides;
Eur. J. Pharmacol. 2007, 559, 138-149. -
M. Pietsch, M. Nieger, M. Gütschow;
N-Benzyl-tetrahydropyrido-anellated Thiophene Derivatives - New Anticholinesterases;
Acta Crystallogr. C 2007, 63, 147-151. -
M. Meusel, M. Frizler, P. Ottersbach, L. Peters, M. Gütschow;
The Use of Visible Absorption Spectra to Evaluate Different Color Reactions for the Detection of Cyclic Ureides;
Pharmazie 2007, 62, 416-418. -
P. W. Elsinghorst, C. M. Gonzalez Tanarro, M. Gütschow;
Novel Heterobivalent Tacrine Derivatives As Cholinesterase Inhibitors With Notable Selectivity Towards Butyrylcholinesterase;
J. Med. Chem. 2006, 49, 7540-7544. -
A. Rüttger, J. Mollenhauer, R. Löser, M. Gütschow, B. Wiederanders;
Microplate Assay for Quantitative Determination of Cathepsin Activities in Viable Cells Using Derivatives of 4-Methoxy-beta-naphthylamide;
BioTechniques 2006, 41, 469-473. -
M. Gütschow, M. Meusel;
Enzyminhibitoren in der Parkinson-Therapie;
Pharm. Unserer Zeit 2006, 35, 218-225. -
S. Kolp, M. Pietsch, E. A. Galinski; M. Gütschow;
Compatible Solutes As Protectants for Zymogens Against Proteolysis;
Biochim. Biophys. Acta 2006, 1764, 1234-1242. -
A. Ambrozak, M. Gütschow;
Transformation of a Spirobarbituric Acid via Aminobarbituric Acid-Hydantoin Rearrangement;
J. Heterocyclic Chem. 2006, 43, 807-811.
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M. Pietsch, M. Gütschow;
Synthesis of Tricyclic 1,3-Oxazin-4-ones and Kinetic Analysis of Cholesterol Esterase and Acetylcholinesterase Inhibition;
J. Med. Chem. 2005, 48, 8270-8288. -
R. Löser, K. Schilling, E. Dimmig, M. Gütschow;
Interaction of Papain-Like Cysteine Proteases with Dipeptide-Derived Nitriles;
J. Med. Chem. 2005, 48, 7688-7707. -
M. Meusel, M. Frizler; M. Gütschow;
A New Objective Method to Compare Different Color Reactions for the Detection of Cyclic Ureides;
Anal. Sci. 2005, 21, 1561-1564. -
H. Euler, A. Kirfel, M. Meusel, M. Gütschow;
Crystal Structure of N-Benzyl-N-1,3,4-tetramethyl-2,5-dioxo-4-imidazolidinecarboxamide, C15H19N3O3;
Z. Kristallogr. NCS 2005, 220, 369-370. -
D. Bolek, M. Gütschow;
Preparation of 4,6,3',4'-Tetrasubstituted Aurones via Aluminium Oxide-Catalyzed Condensation;
J. Heterocyclic Chem. 2005, 42, 1399-1404. -
M. Gütschow, M. Pietsch, A. Themann, J. Fahrig, B. Schulze;
2,4,5-Triphenylisothiazol-3(2H)-one 1,1-Dioxides As Inhibitors of Human Leukocyte Elastase;
J. Enz. Inhib. Med. Chem. 2005, 20, 341-347. -
M. Meusel, M. Gütschow;
Preparation of a Polystyrene-Based Urea Resin;
Tetrahedron Lett. 2005, 46, 2231-2233. -
O. Zschörnig, M. Pietsch, R. Süß, J. Schiller, M. Gütschow;
Cholesterol Esterase Action on Human High-Density Lipoproteins and Inhibition Studies Detected by MALDI-TOF MS;
J. Lipid Res. 2005, 46, 803-811 . -
M. Meusel, M. Gütschow;
Recent Developments in Hydantoin Chemistry. A Review;
Org. Prep. Proced. Int. 2004, 36, 391-443. -
R. Löser, M. Chlupacova, A. Marecek, V. Opletalova, M. Gütschow;
Synthetic Studies Towards the Preparation of 2-Benzyl-2-hydroxybenzofuran-3-(2H)-one, the Prototype of Naturally Occurring Auronols;
Helv. Chim. Acta 2004, 87, 2597-2601. -
S. S. Ng, G. R. Mac Pherson, M. Gütschow, K. Eger, W. D. Figg;
Antitumor Effects of Thalidomide Analogues in Human Prostate Cancer Xenografts Implanted in Immunodeficient Mice;
Clin. Cancer Res. 2004, 10, 4192-4197. -
E. R. Lepper, S. S. Ng, M. Gütschow, M. Weiss, S. Hauschildt, T. H. Hecker, F. A. Luzzio, K. Eger, W. D. Figg;
Comparative Molecular Field Analysis and Comparative Molecular Similarity Indices Analysis of Thalidomide Analogs as Angiogenesis Inhibitors;
J. Med. Chem. 2004, 47, 2219-2227. -
S. S. Ng, M. Gütschow, M. Weiss, S. Hauschildt, U. Teubert, T. K. Hecker, F. A. Luzzio, E. A. Kruger, K. Eger, W. D. Figg;
Antiangiogenic Activity of N-Substituted and Tetrafluorinated Thalidomide Analogues;
Cancer Res. 2003, 63, 3189-3194. -
M. Meusel, A. Ambrozak, T. K. Hecker, M. Gütschow;
The Aminobarbituric Acid-Hydantoin Rearrangement;
J. Org. Chem. 2003, 68, 4684-4692. -
M. Gütschow, M. Pietsch, K. Taubert, T. H. E. Freysoldt, B. Schulze;
Synthesis of 2-Phenylisothiazol-3(2H)-one 1,1-Dioxides: Inhibitors of Human Leukocyte Elastase;
Z. Naturforsch. 2003, 58b, 111-120. -
A. Thiele, R. Bang, M. Gütschow, M. Rossol, S. Loos, K. Eger, G. Tiegs, S. Hauschildt;
Cytokine Modulation and Suppression of Liver Injury by a Novel Analogue of Thalidomide;
Eur. J. Pharmacol. 2002, 453, 325-334. -
M. Gütschow, S. Hauschildt, S. Benard, S. Reichl, U. G. Witt, K. Eger, J. Arnhold;
Michael Adducts of fPalmitoylascorbic Acid: Effects on the Oxidative Burst of Neutrophils and the Production of TNF-alpha in Monocytes;
Pharmacology 2002, 66, 162-168. -
M. Pietsch, M. Gütschow;
Alternate Substrate Inhibition of Cholesterol Esterase by Thieno[2,3-d][1,3]oxazin-4-ones;
J. Biol. Chem. 2002, 277, 24006-24013. -
M. Gütschow, L. Kuerschner, M. Pietsch, A. Ambrozak, U. Neumann, R. Günther, H.-J. Hofmann;
Inhibition of Cathepsin G by 2-Amino-3,1-benzoxazin-4-ones: Kinetic Investigations and Docking Studies;
Arch. Biochem. Biophys. 2002, 402, 180-191. -
A. Braune, M. Gütschow, W. Engst, M. Blaut;
Degradation of Quercetin and Luteolin by Eubacterium ramulus;
Appl. Environ. Microbiol. 2001, 67, 5558-5567. -
M. Gütschow, J. C. Powers;
2-Alkylthio-4-oxo-3-quinazolineacetonitriles and Analogous Thieno[3,2-d]pyrimidineacetonitriles: Reaction with Thiols via Trapped Thioimidates;
J. Org. Chem. 2001, 66, 4723-4727. -
M. Gütschow, J. C. Powers;
A New Dimerization Reaction Producing 2-Amino-9-oxopyrrolo[2,1-b]quinazoline-1-carbonitriles and Analogous Pyrrolo[1,2-a]thieno[3,2-d]pyrimidinecarbonitriles;
J. Heterocyclic Chem. 2001, 38, 419-424. -
M. Gütschow, T. Hecker, A. Thiele, S. Hauschildt, K. Eger;
Aza Analogues of Thalidomide: Synthesis and Evaluation as Inhibitors of Tumor Necrosis Factor-alpha Production In Vitro;
Bioorg. Med. Chem. 2001, 9, 1059-1065. -
U. Neumann, N. M. Schechter, M. Gütschow;
Inhibition of Human Chymase by 2-Amino-3,1-benzoxazin-4-ones;
Bioorg. Med. Chem. 2001, 9, 947-954.
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P. Wippich, M. Gütschow, S. Leistner;
Regioselective Preparation of 1-(Bromomethyl)-5H-thiazolo[3,2-a]quinazolin-5-ones and Analogous 5H-Thieno[3,2-e]thiazolo[3,2-a]pyrimidin-5-ones from Fused 2-(Alkenylthio)pyrimidin-4-ones;
Synthesis 2000, 714-720. -
F. Wormstädt, U. Brinckmann, M. Gütschow, K. Eger;
Synthesis of Acyclic Nucleoside Phosphonates as Antiviral Compounds;
J. Heterocyclic Chem. 2000, 37, 1187-1191. -
M. Gütschow, L. Kuerschner, U. Neumann, M. Pietsch, R. Löser, N. Koglin, K. Eger;
2-Diethylaminothieno[1,3]oxazin-4-ones as Stable Inhibitors of Human Leukocyte Elastase;
J. Med. Chem. 1999, 42, 5437-5447. -
M. Gütschow;
One-Pot Reactions of N-(Mesyloxy)phthalimides with Secondary Amines to 2-Ureidobenzamides, 2-Ureidobenzoic Acids, Ethyl 2-Ureidobenzoates, or Isatoic Anhydrides;
J. Org. Chem. 1999, 64, 5109-5115. -
M. Gütschow, T. Hecker, K. Eger;
A New One-Pot Synthesis of 5,5-Disubstituted Hydantoins from Diethyl Acetamidomalonates and Ureas;
Synthesis 1999, 410-414. -
M. Gütschow, U. Neumann, J. Sieler, K. Eger;
Studies on 2-Benzyloxy-4H-3,1-benzoxazin-4-ones as Serine Protease Inhibitors;
Pharm. Acta Helv. 1998, 73, 95-103. -
M. Gütschow, U. Neumann;
Novel Thieno[2,3-d][1,3]oxazin-4-ones as Inhibitors of Human Leukocyte Elastase;
J. Med. Chem. 1998, 41, 1729-1740. -
M. Gütschow, U. Neumann;
Inhibition of Cathepsin G by 4H-3,1-Benzoxazin-4-ones;
Bioorg. Med. Chem. 1997, 5, 1935-1942. -
M. Gütschow;
Novel Heterocycles Derived from Substituted Aroylthioureas: Synthesis of 3,1-Benzothiazin-4-ones, Thieno[3,2-d][1,3]thiazin-4-ones and 1,2,4-Thiadiazolo[2,3-a][3,1]benzothiazin-5-ones;
J. Heterocyclic Chem. 1996, 33, 355-360. -
P. Wippich, C. Hendreich, M. Gütschow, S. Leistner;
Regioselektive Darstellung von 4-Methyl-3,4-dihydro-2H-6H-[1,3]thiazino[2,3-b]chinazolin-6-onen und 2,3-Dihydro-3-methyl-5H-[2,3-b]chinazolin-5-onen sowie analogen mehrcyclischen Pyrimidinon-Derivaten aus kondensierten 2-Alkenylthiopyrimidin-4(3H)-onen;
Synthesis 1996, 741-747. -
M. Gütschow, H. Schröter, G. Kuhnle, K. Eger;
Synthesis of 4-Isobutyl Substituted Thiophenes by Gewald Reaction;
Monatsh. Chem. 1996, 127, 297-303.
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M. Gütschow, S. Leistner;
A Simple Conversion of Thiazolo- and [1,3]Thiazino[2,3-b]-quinazolinones and Analogous Fused Thieno[2,3-d]pyrimidinones into Heterocyclic Substituted Alkyl Disulfides;
Synthesis 1995, 1488-1490. -
M. Gütschow, E. Tonew, S. Leistner;
Bis[(2,4-dioxo-1,2,3,4-tetrahydrochinazolin-3-yl)alkyl]-disulfane und 3-(Mercaptoalkyl)chinazolin-2,4(1H,3H)-dione: Synthese durch Ringtransformationen und antivirale Aktivität;
Pharmazie 1995, 50, 672-675. -
M. Gütschow, U. Neumann;
2-Benzoylamino-6,7-dimethoxy-4H-3,1-benzoxazin-4-one: Synthesis and Investigation of Serine Protease Inactivation;
Monatsh. Chem. 1995, 126, 1145-1149. -
U. Neumann, M. Gütschow;
3,1-Benzothiazin-4-ones and 3,1-Benzoxazin-4-ones: Highly Different Activities in Chymotrypsin Inactivation;
Bioorg. Chem. 1995, 23, 72-88. -
M. Gütschow, K. Drößler, S. Leistner;
Darstellung von N-1-substituierten 3-(2-Mercaptoethyl)chinazolin-2,4(1H,3H)-dionen über Bis[2-(2-amino-benzoylaminoethyl]-disulfane und Prüfung auf immunstimulatorische Wirksamkeit;
Arch. Pharm. (Weinheim) 1995, 328, 277-281. -
M. Gütschow, K. Drößler, S. Leistner;
3-Mercaptoalkylthieno[2,3-d]pyrimidin-2,4(1H,3H)-dione: Synthese und Prüfung auf immunstimulatorische Wirksamkeit;
Arch. Pharm. (Weinheim) 1995, 328, 231-234. -
M. Gütschow, S. Leistner;
Synthesis of 2-Acetonyl-, 2-Phenacyl-, and 2-(Dioxocycloalkyl)-Substituted Thieno[2,3-d][1,3]thiazin-4-ones;
Liebigs Ann. Chem. 1995, 445-448. -
U. Neumann, M. Gütschow;
N-(Sulfonyloxy)phthalimides and Analogues are Potent Inactivators of Serine Proteases;
J. Biol. Chem. 1994, 269, 21561-21567. -
M. Gütschow;
2H-Thieno[2,3-d][1,3]thiazine-2,4(1H)-diones from Ethyl 2-(Alkoxythio-carbonyl)thiophene-3-carboxylates;
Sulfur Lett. 1993, 16, 71-76. -
M. Pink, J. Sieler, M. Gütschow;
Crystal Structure of 2-(Morpholin-4-yl)-4H-3,1-benzoxazin-4-one;
Z. Krist. 1993, 207, 319-321. -
M. Pink, J. Sieler, M. Gütschow;
Crystal Structure of 3-Benzoyl-1-ethyl-2,3-dihydro-2-thioxo-quinazolin-4(1H)-one;
Z. Krist. 1993, 207, 316-318. -
M. Gütschow, S. Leistner, M. Pink;
One-Pot Synthesis of 4-Acylimino-2-aminothieno[2,3-d][1,3]thiazines;
J. Heterocyclic Chem. 1992, 29, 279-282. -
M. Gütschow, K. Heinecke, W. Thiel, S. Leistner;
Zur Synthese 6,7-dimethoxy-substituierter 3,1-Benzothiazin-4-one;
Arch. Pharm. (Weinheim) 1991, 324, 464-466. -
S. Leistner, M. Gütschow;
Einfache Darstellung N,N-dimethyl-N'-heterocyclylsubstituierter Formamidine aus [2,3-d]thieno-anellierten 1,3-Thiazin-4-on- bzw. Pyrimidin-Derivaten und Vilsmeyer-Reagens;
Pharmazie 1991, 46, 457-458.
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M. Gütschow, S. Leistner;
Zur Bildung von 2-Amino-3,1-benzothiazin-4-on aus 2-(3-Benzoyl-thioureido)benzonitril;
Z. Chem. 1990, 30, 440-441. -
S. Leistner, M. Gütschow, J. Stach;
2-Amino-4-oxo-4H-3,1-benzothiazine: Darstellung, Dimroth-Umlagerung zu 4-Oxo-2-thioxo-1,2,3,4-tetrahydrochinazolinen und MS/MS-Fragmentierung;
Arch. Pharm. (Weinheim) 1990, 323, 857-861. -
M. Gütschow, S. Leistner;
Darstellung von 2-Amino-4-imino-thieno[2,3-d][1,3]-thiazinium-Salzen und deren Retro-Cycloadditions-Reaktion zu 2-Thioureido-thiophen-3-carbonitrilen;
Z. Chem. 1990, 30, 23-24. -
A.O. Gukassyan, L.H. Galstyan, M. Gütschow, A.A. Avetysyan;
Synthesis of Functionally Substituted 3- and 4-Penten-4-olides;
Z. Org. Chim. 1989, 25, 1716-1722. -
S. Leistner, M. Gütschow, G. Wagner;
Eine einfache Synthese von 2-Alkylthio-4-amino-thieno[2,3-d]pyrimidinen;
Arch. Pharm. (Weinheim) 1989, 322, 227-230. -
S. Leistner, M. Gütschow, G. Wagner;
Darstellung von Thiazolo[3,2-d]thieno[2,3-d]-pyrimidinen und strukturanalogen 1,3-Thiazino-Verbindungen aus 2-Hydroxyalkyl-thioureido-thiophen-3-carbonsäure-ethylestern;
Pharmazie 1989, 44, 153-154. -
S. Leistner, M. Gütschow, H. Vieweg, G. Wagner, T. Strohscheidt, R. Grupe;
Verschiedene Darstellungswege zu gegebenenfalls anellierten Imidazo[1,2-c]thieno[3,2-e]pyrimidinen bzw. Pyrimido[1,2-c]thieno[3,2-e]pyrimidinen;
Pharmazie 1988, 43, 756-760. -
S. Leistner, M. Gütschow, G. Wagner, F. Grupe, B. Böhme;
Einstufige Darstellung von zum Teil anellierten 2-Amino-thieno[2,3-d][1,3]thiazin-4-onen aus 2-Benzoyl-thioureido-thiophen-3-carbonsäureethylestern und deren Prüfung auf antiallergische Wirksamkeit;
Pharmazie 1988, 43, 466-470. -
S. Leistner, M. Gütschow, G. Wagner;
Einfache Synthese von zum Teil in 5,6-Stellung anellierten 2-Amino-thieno[2,3-d][1,3]thiazin-4-onen;
Synthesis 1987, 466-470. -
S. Leistner, M. Gütschow, G. Wagner;
Darstellung substituierter Thieno[2,3-d]pyrimidin-4(3H)-thione aus Thieno[2,3-d]1,3-thiazin-4-thionen und N-Nucleophilen durch Ringtransformationsreaktionen;
Pharmazie 1986, 41, 96-98. -
S. Leistner, G. Wagner, M. Gütschow, E. Glusa;
Darstellung von 7-Benzyl-5,6,7,8-tetrahydropyrido[4',3':4,5]thieno[2,3-d]pyrimidin-4(3H)-onen mit Alkylthioethergruppen in 2-Stellung und deren Prüfung auf blutplättchenaggregierende Wirkung;
Pharmazie 1986, 41, 54-55.
Patents
- A. Linkermann, M. Gütschow, C. Steinebach; Dual-Inhibitors of Cellular Necroptosis and Ferroptosis for Use in the Treatment of Organ Transplant Patients; EPC (2020), 20160943.5 - 1112.
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W.D. Figg, E. Lepper, M. Gütschow, A. Ambrozak; Tetrahalogenated Compounds Useful as Inhibitors; PCT Int. Appl. (2007), WO2007120669.
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W.D. Figg, K. Eger, U. Teubert, M. Weiss, M. Gütschow, T. Hecker, S. Hauschildt; Analogs of Thalidomide as Potential Angiogenesis Inhibitors; PCT Int. Appl. (2002), WO 2002068414.
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S. Leistner, M. Gütschow, K. Drößler, H. Vieweg, G. Wagner, T. Strohscheidt, D. Lohmann, G. Laban, H. Ambrosius, A. Siegling; 2-(Mercaptoalkyl)chinazolin-2,4(1H,3H)-dione, Verfahren zu ihrer Herstellung und pharmazeutische Zubereitungen; EP 454 060.
Book Chapters
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20 Monographien in "Hagers Handbuch der Pharmazeutischen Praxis, 5. Auflage, Stoffe A-Z, Springer-Verlag 1993 und 1994".
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11 Monographien in "Hagers Handbuch der Pharmazeutischen Praxis, 5. Auflage, Folgeband 4 und 5, Stoffe A-Z, Springer-Verlag 1999".