Publikationen
Publikationen des Arbeitskreises Hansen.
2024
Bollmann LM, Lange F, Hamacher A, Biermann L, Schäker-Hübner L, Hansen FK, Kassack MU
Triple Combination of Entinostat, a Bromodomain Inhibitor, and Cisplatin Is a Promising Treatment Option for Bladder Cancer.
Cancers 2024; 16(19):3374. doi: 10.3390/cancers16193374.
Feller F, Honin I, Miranda M, Weber H, Henze S, Hanl M, Hansen FK
Development of the First-in-Class FEM1B-Recruiting Histone Deacetylase Degraders.
ChemRxiv 2024. doi: 10.26434/chemrxiv-2024-85zmp.
Fischle A, Lutsch M, Hübner F, Schäker-Hübner L, Schürmann L, Hansen FK, Kalinina SA
Micro-scale screening of genetically modified Fusarium fujikuroi strain extends the apicidin family.
Nat Prod Bioprospect 2024; 14(1):51. doi: 10.1007/s13659-024-00473-9.
Huber ME, Wurnig SL, Moumbock AFA, Toy L, Kostenis E, Alonso Bartolomé A, Szpakowska M, Chevigné A, Günther S, Hansen FK, Schiedel M
Development of a NanoBRET Assay Platform to Detect Intracellular Ligands for the Chemokine Receptors CCR6 and CXCR1.
ChemMedChem 2024:e202400284. doi: 10.1002/cmdc.202400284.
Jenke R, Oliinyk D, Zenz T, Körfer J, Schäker-Hübner L, Hansen FK, Lordick F, Meier-Rosar F, Aigner A, Büch T
HDAC inhibitors activate lipid peroxidation and ferroptosis in gastric cancer.
Biochem Pharmacol 2024; 225:116257. doi: 10.1016/j.bcp.2024.116257.
König B, Hansen FK
2-(Difluoromethyl)-1,3,4-oxadiazoles: The Future of Selective Histone Deacetylase 6 Modulation?
ACS Pharmacol Transl Sci 2024; 7(3):899–903. doi: 10.1021/acsptsci.4c00031.
Kraft FB, Biermann L, Schäker-Hübner L, Hanl M, Hamacher A, Kassack MU, Hansen FK
Hydrazide-Based Class I Selective HDAC Inhibitors Completely Reverse Chemoresistance Synergistically in Platinum-Resistant Solid Cancer Cells.
J. Med. Chem. 2024. doi: 10.1021/acs.jmedchem.4c01817.
Kraft FB, Enns J, Honin I, Engelhardt J, Schöler A, Smith ST, Meiler J, Schäker-Hübner L, Weindl G, Hansen FK
Groebke Blackburn Bienaymé-mediated multi-component synthesis of selective HDAC6 inhibitors with anti-inflammatory properties.
Bioorg Chem 2024; 143:107072. doi: 10.1016/j.bioorg.2023.107072.
Scheuerer S, Motlova L, Schäker-Hübner L, Sellmer A, Feller F, Ertl FJ, Koch P, Hansen FK, Barinka C, Mahboobi S
Biological and structural investigation of tetrahydro-β-carboline-based selective HDAC6 inhibitors with improved stability.
Eur J Med Chem 2024:116676. doi: 10.1016/j.ejmech.2024.116676.
Stopper D, Biermann L, Watson P, Li j, König B, Gaynes M, Carvalho LP de, Hanl M, Hamacher A, Schäker-Hübner L, Held J, Christianson D, Kassack M, Hansen FK
Exploring Alternative Zinc-Binding Groups in Histone Deacetylase (HDAC) Inhibitors Uncovers DS-103 as a Potent Ethylhydrazide-Based HDAC Inhibitor with Chemosensitizing Properties.
ChemRxiv 2024. doi: 10.26434/chemrxiv-2024-837bd.
Stopper D, Buntrock S, Tan K, Carvalho LP de, Schäker-Hübner L, Held J, Kassack MU, Hansen FK
Multicomponent syntheses enable the discovery of novel quisinostat-derived chemotypes as histone deacetylase inhibitors.
Eur J Med Chem 2024; 281:117045. doi: 10.1016/j.ejmech.2024.117045.
Stopper D, Carvalho LP de, Souza ML de, Kponomaizoun C-E, Winzeler EA, Held J, Hansen FK
Development of peptoid-based heteroaryl-decorated histone deacetylase (HDAC) inhibitors with dual-stage antiplasmodial activity.
Eur J Med Chem 2024; 277:116782. doi: 10.1016/j.ejmech.2024.116782.
Toledano-Pinedo M, Diez-Iriepa D, Porro-Pérez A, Schäker-Hübner L, Hanl M, Samadi A, Almendros P, Iriepa I, Rodríguez-Fernández MM, Griñán-Ferré C, Siwek A, Wolak M, Satała G, Bojarski AJ, Doroż-Płonka A, Handzlik J, Godyń J, Knez D, Gobec S, Więckowska A, Hansen FK, Marco-Contelles J
Contilistat, a New Multitarget Small Polyfunctionalized Indole Derivative.
Synlett 2024. doi: 10.1055/s-0043-1775419.
Toledano-Pinedo M, Porro-Pérez A, Schäker-Hübner L, Romero F, Dong M, Samadi A, Almendros P, Iriepa I, Bautista-Aguilera ÒM, Rodríguez-Fernández MM, Solana-Manrique C, Sanchis I, Mora-Morell A, Rodrìguez AC, Sànchez-Pérez AM, Knez D, Gobec S, Bellver-Sanchis A, Pérez B, Dobrydnev AV, Artetxe-Zurutuza A, Matheu A, Siwek A, Wolak M, Satała G, Bojarski AJ, Doroz-Płonka A, Handzlik J, Godyń J, Więckowska A, Paricio N, Griñán-Ferré C, Hansen FK, Marco-Contelles J
Contilisant+Tubastatin A Hybrids: Polyfunctionalized Indole Derivatives as New HDAC Inhibitor-Based Multitarget Small Molecules with In Vitro and In Vivo Activity in Neurodegenerative Diseases.
J Med Chem 2024. doi: 10.1021/acs.jmedchem.4c01367.
Tretbar M, Schliehe-Diecks J, Bredow L von, Tan K, Roatsch M, Tu J-W, Kemkes M, Sönnichsen M, Schöler A, Borkhardt A, Bhatia S, Hansen FK
Preferential HDAC6 inhibitors derived from HPOB exhibit synergistic antileukemia activity in combination with decitabine.
Eur J Med Chem 2024; 272:116447. doi: 10.1016/j.ejmech.2024.116447.
Wurnig S, Hanl M, Geiger T, Zhai S, Dressel I, Pieńkowska D, Nowak R, Hansen FK
Light-Activatable Photochemically Targeting Chimeras (PHOTACs) Enable the Optical Control of Targeted Protein Degradation of HDAC6.
ChemRxiv 2024. doi: 10.26434/chemrxiv-2024-cs18b.
Wurnig SL, Huber ME, Weiler C, Baltrukevich H, Merten N, Stoetzel I, Chang Y, Klammer R, Baumjohann D, Kiermaier E, Kolb P, Kostenis E, Schiedel M, Hansen FK
A fluorescent probe enables the discovery of improved antagonists targeting the intracellular allosteric site of the chemokine receptor CCR7.
bioRxiv 2024. doi: 10.1101/2024.08.27.607356.
Zhai S, Schäker-Hübner L, Hanl M, Jacobi L, Pieńkowska DE, Gerhartz J, Voget R, Gütschow M, Meissner F, Nowak RP, Steinebach C, Hansen FK
Development and characterization of the first selective class IIb histone deacetylase degraders.
ChemRxiv 2024. doi: 10.26434/chemrxiv-2024-ngppg-v2.
2023
Bachmann LM, Hanl M, Feller F, Sinatra L, Schöler A, Pietzsch J, Laube M, Hansen FK
Solid-Phase Parallel Synthesis of Dual Histone Deacetylase-Cyclooxygenase Inhibitors.
Molecules 2023; 28(3):1061. Verfügbar unter: https://www.mdpi.com/1420-3049/28/3/1061.
Bockstiegel J, Wurnig SL, Engelhardt J, Enns J, Hansen FK, Weindl G
Pharmacological inhibition of HDAC6 suppresses NLRP3 inflammasome-mediated IL-1β release.
Biochem Pharmacol 2023; 215:115693. doi: 10.1016/j.bcp.2023.115693.
Feller F, Hansen FK
Targeted Protein Degradation of Histone Deacetylases by Hydrophobically Tagged Inhibitors.
ACS Med. Chem. Lett. 2023. doi: 10.1021/acsmedchemlett.3c00468.
Huber ME, Wurnig S, Toy L, Weiler C, Merten N, Kostenis E, Hansen FK, Schiedel M
Fluorescent Ligands Enable Target Engagement Studies for the Intracellular Allosteric Binding Site of the Chemokine Receptor CXCR2.
Journal of Medicinal Chemistry 2023. doi: 10.1021/acs.jmedchem.3c00769.
König B, Watson PR, Reßing N, Cragin AD, Schäker-Hübner L, Christianson DW, Hansen FK
Difluoromethyl-1,3,4-oxadiazoles Are Selective, Mechanism-Based, and Essentially Irreversible Inhibitors of Histone Deacetylase 6.
Journal of Medicinal Chemistry 2023; 66(19):13821–37. doi: 10.1021/acs.jmedchem.3c01345.
Kraft FB, Hanl M, Feller F, Schäker-Hübner L, Hansen FK
Photocaged Histone Deacetylase Inhibitors as Prodrugs in Targeted Cancer Therapy.
Pharmaceuticals 2023; 16(3):356. Verfügbar unter: https://www.mdpi.com/1424-8247/16/3/356.
Marquardt V, Theruvath J, Pauck D, Picard D, Qin N, Blümel L, Maue M, Bartl J, Ahmadov U, Langini M, Meyer F-D, Cole A, Cruz-Cruz J, Graef CM, Wölfl M, Milde T, Witt O, Erdreich-Epstein A, Leprivier G, Kahlert U, Stefanski A, Stühler K, Keir ST, Bigner DD, Hauer J, Beez T, Knobbe-Thomsen CB, Fischer U, Felsberg J, Hansen FK, Vibhakar R, Venkatraman S, Cheshier SH, Reifenberger G, Borkhardt A, Kurz T, Remke M, Mitra S
Tacedinaline (CI-994), a class I HDAC inhibitor, targets intrinsic tumor growth and leptomeningeal dissemination in MYC-driven medulloblastoma while making them susceptible to anti-CD47-induced macrophage phagocytosis via NF-kB-TGM2 driven tumor inflammation.
Journal for ImmunoTherapy of Cancer 2023; 11(1):e005871. Verfügbar unter: https://jitc.bmj.com/lookup/doi/10.1136/jitc-2022-005871.
Sinatra L, Vogelmann A, Friedrich F, Tararina MA, Neuwirt E, Colcerasa A, König P, Toy L, Yesiloglu TZ, Hilscher S, Gaitzsch L, Papenkordt N, Zhai S, Zhang L, Romier C, Einsle O, Sippl W, Schutkowski M, Gross O, Bendas G, Christianson DW, Hansen FK, Jung M, Schiedel M
Development of First-in-Class Dual Sirt2/HDAC6 Inhibitors as Molecular Tools for Dual Inhibition of Tubulin Deacetylation.
Journal of Medicinal Chemistry 2023; 66(21):14787–814. doi: 10.1021/acs.jmedchem.3c01385.
Steinebach C, Bricelj A, Murgai A, Sosič I, Bischof L, Ng YLD, Heim C, Maiwald S, Proj M, Voget R, Feller F, Košmrlj J, Sapozhnikova V, Schmidt A, Zuleeg MR, Lemnitzer P, Mertins P, Hansen FK, Gütschow M, Krönke J, Hartmann MD
Leveraging Ligand Affinity and Properties: Discovery of Novel Benzamide-Type Cereblon Binders for the Design of PROTACs.
Journal of Medicinal Chemistry 2023; 66(21):14513–43. doi: 10.1021/acs.jmedchem.3c00851.
Wurnig S, Vogt M, Hogenkamp J, Dienstbier N, Borkhardt A, Bhatia S, Hansen FK
Development of the first geldanamycin-based HSP90 degraders.
Frontiers in Chemistry 2023; 11:1219883. doi: 10.3389/fchem.2023.1219883.
2022
Bhatia S, Spanier L, Bickel D, Dienstbier N, Woloschin V, Vogt M, Pols H, Lungerich B, Reiners J, Aghaallaei N, Diedrich D, Frieg B, Schliehe-Diecks J, Bopp B, Lang F, Gopalswamy M, Loschwitz J, Bajohgli B, Skokowa J, Borkhardt A, Hauer J, Hansen FK, Smits SHJ, Jose J, Gohlke H, Kurz T.
Development of a First-in-Class Small-Molecule Inhibitor of the C-Terminal Hsp90 Dimerization.
ACS Central Science 2022; 8(5):636–55. Verfügbar unter: https://pubs.acs.org/doi/10.1021/acscentsci.2c00013.
Bredow L von, Schäfer TM, Hogenkamp J, Tretbar M, Stopper D, Kraft FB, Schliehe-Diecks J, Schöler A, Borkhardt A, Bhatia S, Held J, Hansen F. K
Synthesis, Antiplasmodial, and Antileukemia Activity of Dihydroartemisinin-HDAC Inhibitor Hybrids as Multitarget Drugs.
Pharmaceuticals 2022; 15(3):333. Verfügbar unter: https://www.mdpi.com/1424-8247/15/3/333.
Chu K-B, Lee H-A, Pflieger M, Fischer F, Asfaha Y, Alves Avelar LA, Skerhut A, Kassack MU, Hansen FK, Schöler A, Kurz T, Kim M-J, Moon E-K, Quan F.-S.
Antiproliferation and Antiencystation Effect of Class II Histone Deacetylase Inhibitors on Acanthamoeba castellanii.
ACS Infectious Diseases 2022; 8(2):271–9. Verfügbar unter: https://pubs.acs.org/doi/10.1021/acsinfecdis.1c00390.
Clauß O, Schäker-Hübner L, Wenzel B, Toussaint M, Deuther-Conrad W, Gündel D, Teodoro R, Dukić-Stefanović S, Ludwig F, Kopka K, Brust P, Hansen FK, Scheunemann M.
Development and Biological Evaluation of the First Highly Potent and Specific Benzamide-Based Radiotracer 18FBA3 for Imaging of Histone Deacetylases 1 and 2 in Brain.
Pharmaceuticals 2022; 15(3):324. Verfügbar unter: https://www.mdpi.com/1424-8247/15/3/324.
Keuler T, König B, Bückreiß N, Kraft FB, König P, Schäker-Hübner L, Steinebach C, Bendas G, Gütschow M, Hansen F. K
Development of the first non-hydroxamate selective HDAC6 degraders.
Chem Commun (Camb) 2022; 58(79):11087–90. Verfügbar unter: http://xlink.rsc.org/?DOI=D2CC03712B.
Reßing N, Schliehe-Diecks J, Watson PR, Sönnichsen M, Cragin AD, Schöler A, Yang J, Schäker-Hübner L, Borkhardt A, Christianson DW, Bhatia S, Hansen F. K
Development of Fluorinated Peptoid-Based Histone Deacetylase (HDAC) Inhibitors for Therapy-Resistant Acute Leukemia.
Journal of Medicinal Chemistry 2022; 65(22):15457–72. doi: 10.1021/acs.jmedchem.2c01418.
Schäker‐Hübner L, Haschemi R, Büch T, Kraft FB, Brumme B, Schöler A, Jenke R, Meiler J, Aigner A, Bendas G, Hansen F. K
Balancing Histone Deacetylase (HDAC) Inhibition and Drug‐likeness: Biological and Physicochemical Evaluation of Class I Selective HDAC Inhibitors.
ChemMedChem 2022; 17(9):e202100755. Verfügbar unter: https://onlinelibrary.wiley.com/doi/10.1002/cmdc.202100755.
Sinatra L, Yang J, Schliehe-Diecks J, Dienstbier N, Vogt M, Gebing P, Bachmann LM, Sönnichsen M, Lenz T, Stühler K, Schöler A, Borkhardt A, Bhatia S, Hansen F. K
Solid-Phase Synthesis of Cereblon-Recruiting Selective Histone Deacetylase 6 Degraders (HDAC6 PROTACs) with Antileukemic Activity.
Journal of Medicinal Chemistry 2022; 65(24):16860–78. doi: 10.1021/acs.jmedchem.2c01659.
Vogelmann A, Jung M, Hansen FK, Schiedel M.
Comparison of Cellular Target Engagement Methods for the Tubulin Deacetylases Sirt2 and HDAC6: NanoBRET, CETSA, Tubulin Acetylation, and PROTACs.
ACS Pharmacology & Translational Science 2022; 5(2):138–40. Verfügbar unter: https://pubs.acs.org/doi/10.1021/acsptsci.2c00004.
2021
Alves Avelar LA, Schrenk C, Sönnichsen M, Hamacher A, Hansen FK, Schliehe-Diecks J, Borkhardt A, Bhatia S, Kassack MU, Kurz T.
Synergistic induction of apoptosis in resistant head and neck carcinoma and leukemia by alkoxyamide-based histone deacetylase inhibitors.
European Journal of Medicinal Chemistry 2021; 211:113095. Verfügbar unter: https://linkinghub.elsevier.com/retrieve/pii/S0223523420310679.
Bhatia S, Hansen FK, Schiedel M.
Call for Papers: “Epigenetics 2.0”—A Joint Virtual Special Issue on Epigenetics.
ACS Pharmacology & Translational Science 2021; 4(4):1262–3. Verfügbar unter: https://pubs.acs.org/doi/10.1021/acsptsci.1c00156.
Jenke R, Reßing N, Hansen FK, Aigner A, Büch T.
Anticancer Therapy with HDAC Inhibitors: Mechanism-Based Combination Strategies and Future Perspectives.
Cancers 2021; 13(4):634. Verfügbar unter: https://www.mdpi.com/2072-6694/13/4/634.
Mackwitz MKW, Hesping E, Eribez K, Schöler A, Antonova-Koch Y, Held J, Winzeler EA, Andrews KT, Hansen F. K
Investigation of the in vitro and in vivo efficacy of peptoid-based HDAC inhibitors with dual-stage antiplasmodial activity.
European Journal of Medicinal Chemistry 2021; 211:113065. Verfügbar unter: https://linkinghub.elsevier.com/retrieve/pii/S0223523420310370.
Müller CE, Hansen FK, Gütschow M, Lindsley CW, Liotta D.
New Drug Modalities in Medicinal Chemistry, Pharmacology, and Translational Science: Joint Virtual Special Issue by Journal of Medicinal Chemistry, ACS Medicinal Chemistry Letters, and ACS Pharmacology & Translational Science.
Journal of Medicinal Chemistry 2021; 64(19):13935–6. Verfügbar unter: https://pubs.acs.org/doi/10.1021/acs.jmedchem.1c01548.
Okubo K, Isono M, Asano T, Reßing N, Schulz WA, Hansen FK, Sato A.
Ubiquitin-proteasome System Is a Promising Target for Killing Cisplatin-resistant Bladder Cancer Cells.
Anticancer Research 2021; 41(6):2901–12. Verfügbar unter: http://ar.iiarjournals.org/lookup/doi/10.21873/anticanres.15072.
Okubo K, Reßing N, Schulz WA, Hansen FK, Asano T, Sato A.
The Dual Histone Deacetylase-Proteasome Inhibitor RTS-V5 Acts Synergistically With Ritonavir to Induce Endoplasmic Reticulum Stress in Bladder Cancer Cells.
Anticancer Research 2021; 41(12):5987–96. Verfügbar unter: http://ar.iiarjournals.org/lookup/doi/10.21873/anticanres.15417.
Pflieger M, Sönnichsen M, Horstick-Muche N, Yang J, Schliehe-Diecks J, Schöler A, Borkhardt A, Hamacher A, Kassack MU, Hansen FK, Bhatia S, Kurz T.
Oxa Analogues of Nexturastat A Demonstrate Improved HDAC6 Selectivity and Superior Antileukaemia Activity.
ChemMedChem 2021; 16(11):1798–803. Verfügbar unter: https://onlinelibrary.wiley.com/doi/10.1002/cmdc.202001011.
Schäker-Hübner L, Warstat R, Ahlert H, Mishra P, Kraft FB, Schliehe-Diecks J, Schöler A, Borkhardt A, Breit B, Bhatia S, Hügle M, Günther S, Hansen F. K
4-Acyl Pyrrole Capped HDAC Inhibitors: A New Scaffold for Hybrid Inhibitors of BET Proteins and Histone Deacetylases as Antileukemia Drug Leads.
Journal of Medicinal Chemistry 2021; 64(19):14620–46. Verfügbar unter: https://pubs.acs.org/doi/10.1021/acs.jmedchem.1c01119.
Selg C, Schöler A, Schliehe-Diecks J, Hanl M, Sinatra L, Borkhardt A, Sárosi MB, Bhatia S, Hey-Hawkins E, Hansen F. K
Borinostats: solid-phase synthesis of carborane-capped histone deacetylase inhibitors with a tailor-made selectivity profile.
Chemical Science 2021; 12(35):11873–81. Verfügbar unter: http://xlink.rsc.org/?DOI=D1SC02268G.
Sinatra L, Kolano L, Icker M, Fritzsche SR, Volke D, Gockel I, Thieme R, Hoffmann R, Hansen F. K
Hybrid Peptides Based on α-Aminoxy Acids as Antimicrobial and Anticancer Foldamers.
ChemPlusChem 2021; 86(6):827–35. Verfügbar unter: https://onlinelibrary.wiley.com/doi/10.1002/cplu.202000812 .
2020
Benedetti R, Conte M, Dell'Aversana C, Hansen FK, Zwergel C.
Editorial: Chemical Innovative Approaches in Cancer Molecular Medicine and Translational Clinical Research.
Frontiers in Chemistry 2020; 8(September):820. doi: 10.3389/fchem.2020.00820.
Friedrich A, Assmann A-S, Schumacher L, Stuijvenberg JV, Kassack MU, Schulz WA, Roos WP, Hansen FK, Pflieger M, Kurz T, Fritz G.
In Vitro Assessment of the Genotoxic Hazard of Novel Hydroxamic Acid- and Benzamide-Type Histone Deacetylase Inhibitors (HDACi).
International Journal of Molecular Sciences 2020; 21(13):1–21. doi: 10.3390/ijms21134747.
Reßing N, Sönnichsen M, Osko JD, Schöler A, Schliehe-Diecks J, Skerhut A, Borkhardt A, Hauer J, Kassack MU, Christianson DW, Bhatia S, Hansen F. K
Multicomponent Synthesis, Binding Mode, and Structure-Activity Relationship of Selective Histone Deacetylase 6 (HDAC6) Inhibitors with Bifurcated Capping Groups.
Journal of Medicinal Chemistry 2020; 63(18):10339–51. Verfügbar unter: https://pubs.acs.org/doi/10.1021/acs.jmedchem.9b01888.
Rodrigues Moita AJ, Bandolik JJ, Hansen FK, Kurz T, Hamacher A, Kassack M. U
Priming with HDAC Inhibitors Sensitizes Ovarian Cancer Cells to Treatment with Cisplatin and HSP90 Inhibitors.
International Journal of Molecular Sciences 2020; 21(21):1–22. doi: 10.3390/ijms21218300.
Sinatra L, Bandolik JJ, Roatsch M, Sönnichsen M, Schoeder CT, Hamacher A, Schöler A, Borkhardt A, Meiler J, Bhatia S, Kassack MU, Hansen F. K
Hydroxamic Acids Immobilized on Resins (HAIRs): Synthesis of Dual-Targeting HDAC Inhibitors and HDAC Degraders (PROTACs).
Angew Chem Int Ed Engl 2020; 59(50):22494–9. Verfügbar unter: https://onlinelibrary.wiley.com/doi/10.1002/anie.202006725 .
2019
Erdeljac N, Bussmann K, Schöler A, Hansen FK, Gilmour R.
Fluorinated Analogues of the Histone Deacetylase Inhibitor Vorinostat (Zolinza): Validation of a Chiral Hybrid Bioisostere, BITE.
ACS Medicinal Chemistry Letters 2019; 10(9):1336–40. Verfügbar unter: https://pubs.acs.org/doi/10.1021/acsmedchemlett.9b00287.
Koehne E, Kreidenweiss A, Zoleko Manego R, McCall M, Mombo-Ngoma G, Mackwitz MKW, Hansen FK, Held J.
Histone deacetylase inhibitors with high in vitro activities against Plasmodium falciparum isolates collected from Gabonese children and adults.
Scientific Reports 2019; 9(1):17336. doi: 10.1038/s41598-019-53912-w.
Krieger V, Hamacher A, Cao F, Stenzel K, Gertzen CGW, Schäker-Hübner L, Kurz T, Gohlke H, Dekker FJ, Kassack MU, Hansen F. K
Synthesis of Peptoid-Based Class I-Selective Histone Deacetylase Inhibitors with Chemosensitizing Properties.
Journal of Medicinal Chemistry 2019; 62(24):11260–79. Verfügbar unter: https://pubs.acs.org/doi/10.1021/acs.jmedchem.9b01489.
Mackwitz MKW, Hesping E, Antonova-Koch Y, Diedrich D, Woldearegai TG, Skinner-Adams T, Clarke M, Schöler A, Limbach L, Kurz T, Winzeler EA, Held J, Andrews KT, Hansen F. K
Structure-Activity and Structure-Toxicity Relationships of Peptoid-Based Histone Deacetylase Inhibitors with Dual-Stage Antiplasmodial Activity.
ChemMedChem 2019; 14(9):912–26. Verfügbar unter: https://onlinelibrary.wiley.com/doi/10.1002/cmdc.201800808.
Raudszus R, Nowotny R, Gertzen CGW, Schöler A, Krizsan A, Gockel I, Kalwa H, Gohlke H, Thieme R, Hansen F. K
Fluorescent analogs of peptoid-based HDAC inhibitors: Synthesis, biological activity and cellular uptake kinetics.
Bioorganic & Medicinal Chemistry 2019; 27(19):115039. Verfügbar unter: https://linkinghub.elsevier.com/retrieve/pii/S0968089619304778.
Reßing N, Marquardt V, Gertzen CGW, Schöler A, Schramm A, Kurz T, Gohlke H, Aigner A, Remke M, Hansen F. K
Design, synthesis and biological evaluation of β-peptoid-capped HDAC inhibitors with anti-neuroblastoma and anti-glioblastoma activity.
MedChemComm 2019; 10(7):1109–15. Verfügbar unter: http://xlink.rsc.org/?DOI=C8MD00454D.
2018
Bhatia S, Diedrich D, Frieg B, Ahlert H, Stein S, Bopp B, Lang F, Zang T, Kröger T, Ernst T, Kögler G, Krieg A, Lüdeke S, Kunkel H, Rodrigues Moita AJ, Kassack MU, Marquardt V, Opitz FV, Oldenburg M, Remke M, Babor F, Grez M, Hochhaus A, Borkhardt A, Groth G, Nagel-Steger L, Jose J, Kurz T, Gohlke H, Hansen FK, Hauer J.
Targeting HSP90 dimerization via the C terminus is effective in imatinib-resistant CML and lacks the heat shock response.
Blood 2018; 132(3):307–20. Verfügbar unter: http://www.bloodjournal.org/lookup/doi/10.1182/blood-2017-10-810986 https://ashpublications.org/blood/article/132/3/307/39262/Targeting-HSP90-dimerization-via-the-C-terminus-is.
Bhatia S, Krieger V, Groll M, Osko JD, Reßing N, Ahlert H, Borkhardt A, Kurz T, Christianson DW, Hauer J, Hansen F. K
Discovery of the First-in-Class Dual Histone Deacetylase-Proteasome Inhibitor.
Journal of Medicinal Chemistry 2018; 61(22):10299–309. doi: 10.1021/acs.jmedchem.8b01487.
Diedrich D, Stenzel K, Hesping E, Antonova-Koch Y, Gebru T, Duffy S, Fisher G, Schöler A, Meister S, Kurz T, Avery VM, Winzeler EA, Held J, Andrews KT, Hansen F. K
One-pot, multi-component synthesis and structure-activity relationships of peptoid-based histone deacetylase (HDAC) inhibitors targeting malaria parasites.
European Journal of Medicinal Chemistry 2018; 158:801–13. Verfügbar unter: https://linkinghub.elsevier.com/retrieve/pii/S0223523418307906.
Kaletsch A, Pinkerneil M, Hoffmann MJ, Jaguva Vasudevan AA, Wang C, Hansen FK, Wiek C, Hanenberg H, Gertzen C, Gohlke H, Kassack MU, Kurz T, Schulz WA, Niegisch G.
Effects of novel HDAC inhibitors on urothelial carcinoma cells.
Clinical Epigenetics 2018; 10(1):100. doi: 10.1186/s13148-018-0531-y.
Mackwitz MKW, Hamacher A, Osko JD, Held J, Schöler A, Christianson DW, Kassack MU, Hansen F. K
Multicomponent Synthesis and Binding Mode of Imidazo1,2- apyridine-Capped Selective HDAC6 Inhibitors.
Organic Letters 2018; 20(11):3255–8. Verfügbar unter: https://pubs.acs.org/doi/10.1021/acs.orglett.8b01118.
Porter NJ, Osko JD, Diedrich D, Kurz T, Hooker JM, Hansen FK, Christianson D. W
Histone Deacetylase 6-Selective Inhibitors and the Influence of Capping Groups on Hydroxamate-Zinc Denticity.
Journal of Medicinal Chemistry 2018; 61(17):8054–60. Verfügbar unter: https://pubs.acs.org/doi/10.1021/acs.jmedchem.8b01013.
2017
Alves Avelar LA, Held J, Engel JA, Sureechatchaiyan P, Hansen FK, Hamacher A, Kassack MU, Mordmüller B, Andrews KT, Kurz T.
Design and Synthesis of Novel Anti-Plasmodial Histone Deacetylase Inhibitors Containing an Alkoxyamide Connecting Unit.
Archiv der Pharmazie 2017; 350(3-4):1–11. doi: 10.1002/ardp.201600347.
Krieger V, Ciglia E, Thoma R, Vasylyeva V, Frieg B, Sousa Amadeu N de, Kurz T, Janiak C, Gohlke H, Hansen F. K
α-Aminoxy Peptoids: A Unique Peptoid Backbone with a Preference for cis-Amide Bonds.
Chemistry - A European Journal 2017; 23(15):3699–707. doi: 10.1002/chem.201605100.
Krieger V, Hamacher A, Gertzen CGW, Senger J, Zwinderman MRH, Marek M, Romier C, Dekker FJ, Kurz T, Jung M, Gohlke H, Kassack MU, Hansen F. K
Design, Multicomponent Synthesis, and Anticancer Activity of a Focused Histone Deacetylase (HDAC) Inhibitor Library with Peptoid-Based Cap Groups.
Journal of Medicinal Chemistry 2017; 60(13):5493–506. Verfügbar unter: http://pubs.acs.org/doi/10.1021/acs.jmedchem.7b00197 https://pubs.acs.org/doi/10.1021/acs.jmedchem.7b00197.
Kroeger T, Frieg B, Zhang T, Hansen FK, Marmann A, Proksch P, Nagel-Steger L, Groth G, Smits SHJ, Gohlke H.
EDTA aggregates induce SYPRO orange-based fluorescence in thermal shift assay.
PLoS ONE 2017; 12(5):e0177024. doi: 10.1371/journal.pone.0177024.
Stenzel K, Chakrabarti A, Melesina J, Hansen FK, Lancelot J, Herkenhöhner S, Lungerich B, Marek M, Romier C, Pierce RJ, Sippl W, Jung M, Kurz T.
Isophthalic Acid-Based HDAC Inhibitors as Potent Inhibitors of HDAC8 from Schistosoma mansoni.
Archiv der Pharmazie 2017; 350(8):1700096. Verfügbar unter: http://doi.wiley.com/10.1002/ardp.201700096.
Stenzel K, Chua MJ, Duffy S, Antonova-Koch Y, Meister S, Hamacher A, Kassack MU, Winzeler E, Avery VM, Kurz T, Andrews KT, Hansen F. K
Design and Synthesis of Terephthalic Acid-Based Histone Deacetylase Inhibitors with Dual-Stage Anti-Plasmodium Activity.
ChemMedChem 2017; 12(19):1627–36. Verfügbar unter: http://www.ncbi.nlm.nih.gov/pubmed/28812327%0Ahttp://doi.wiley.com/10.1002/cmdc.201700360.
Stenzel K, Hamacher A, Hansen FK, Gertzen CGW, Senger J, Marquardt V, Marek L, Marek M, Romier C, Remke M, Jung M, Gohlke H, Kassack MU, Kurz T.
Alkoxyurea-Based Histone Deacetylase Inhibitors Increase Cisplatin Potency in Chemoresistant Cancer Cell Lines.
Journal of Medicinal Chemistry 2017; 60(13):5334–48. doi: 10.1021/acs.jmedchem.6b01538.
2016
Choi SY, Kee HJ, Kurz T, Hansen FK, Ryu Y, Kim GR, Lin MQ, Jin L, Piao ZH, Jeong M. H
Class I HDACs specifically regulate E-cadherin expression in human renal epithelial cells.
Journal of Cellular and Molecular Medicine 2016; 20(12):2289–98. doi: 10.1111/jcmm.12919.
Diedrich D, Hamacher A, Gertzen CGW, Alves Avelar LA, Reiss GJ, Kurz T, Gohlke H, Kassack MU, Hansen F. K
Rational design and diversity-oriented synthesis of peptoid-based selective HDAC6 inhibitors.
Chem Commun (Camb) 2016; 52(15):3219–22. Verfügbar unter: http://xlink.rsc.org/?DOI=C5CC10301K.
Diedrich D, Moita AJR, Rüther A, Frieg B, Reiss GJ, Hoeppner A, Kurz T, Gohlke H, Lüdeke S, Kassack MU, Hansen F. K
α-Aminoxy Oligopeptides: Synthesis, Secondary Structure, and Cytotoxicity of a New Class of Anticancer Foldamers.
Chemistry - A European Journal 2016; 22(49):17600–11. doi: 10.1002/chem.20160252.
Trazzi S, Fuchs C, Viggiano R, Franceschi M de, Valli E, Jedynak P, Hansen FK, Perini G, Rimondini R, Kurz T, Bartesaghi R, Ciani E.
HDAC4: a key factor underlying brain developmental alterations in CDKL5 disorder.
Human Molecular Genetics 2016; 25(18):3887–907. Verfügbar unter: https://academic.oup.com/hmg/article-lookup/doi/10.1093/hmg/ddw231.
Xiao H, Jiao J, Wang L, O'Brien S, Newick K, Wang L-CS, Falkensammer E, Liu Y, Han R, Kapoor V, Hansen FK, Kurz T, Hancock WW, Beier U. H
HDAC5 controls the functions of Foxp3(+) T-regulatory and CD8(+) T cells.
International Journal of Cancer 2016; 138(10):2477–86. Verfügbar unter: http://doi.wiley.com/10.1002/ijc.29979.
2014
Hansen FK, Skinner-Adams TS, Duffy S, Marek L, Sumanadasa SDM, Kuna K, Held J, Avery VM, Andrews KT, Kurz T.
Synthesis, antimalarial properties, and SAR studies of alkoxyurea-based HDAC inhibitors.
ChemMedChem 2014; 9(3):665–70. doi: 10.1002/cmdc.201300469.
Hansen FK, Sumanadasa SDM, Stenzel K, Duffy S, Meister S, Marek L, Schmetter R, Kuna K, Hamacher A, Mordmüller B, Kassack MU, Winzeler EA, Avery VM, Andrews KT, Kurz T.
Discovery of HDAC inhibitors with potent activity against multiple malaria parasite life cycle stages.
European Journal of Medicinal Chemistry 2014; 82:204–13. Verfügbar unter: http://www.ncbi.nlm.nih.gov/pubmed/24904967 https://linkinghub.elsevier.com/retrieve/pii/S0223523414004747.
Spanier L, Ciglia E, Hansen FK, Kuna K, Frank W, Gohlke H, Kurz T.
Design, synthesis, and conformational analysis of trispyrimidonamides as α-helix mimetics.
J Org Chem 2014; 79(4):1582–93. doi: 10.1021/jo402353z.
Trenholme K, Marek L, Duffy S, Pradel G, Fisher G, Hansen FK, Skinner-Adams TS, Butterworth A, Ngwa CJ, Moecking J, Goodman CD, McFadden GI, Sumanadasa SDM, Fairlie DP, Avery VM, Kurz T, Andrews K. T
Lysine acetylation in sexual stage malaria parasites is a target for antimalarial small molecules.
Antimicrobial Agents and Chemotherapy 2014; 58(7):3666–78. doi: 10.1128/AAC.02721-13.
2013
Marek L, Hamacher A, Hansen FK, Kuna K, Gohlke H, Kassack MU, Kurz T.
Histone deacetylase (HDAC) inhibitors with a novel connecting unit linker region reveal a selectivity profile for HDAC4 and HDAC5 with improved activity against chemoresistant cancer cells.
Journal of Medicinal Chemistry 2013; 56(2):427–36. doi: 10.1021/jm301254q.
Monbaliu J-CM, Beagle LK, Hansen FK, Stevens CV, McArdle C, Katritzky A. R
Capture of benzotriazole-based Mannich electrophiles by CH-acidic compounds.
RSC Advances 2013; 3(13):4152. Verfügbar unter: http://xlink.rsc.org/?DOI=c3ra22826f.
2012
Beagle L, Hansen F, Monbaliu J-C, DesRosiers M, Phillips A, Stevens C, Katritzky A.
Efficient Synthesis of 2,5-Diketopiperazines by Staudinger-Mediated Cyclization.
Synlett 2012; 23(16):2337–40. Verfügbar unter: http://www.thieme-connect.de/DOI/DOI?10.1055/s-0031-1290446.
Geffken D, Hansen F, Khankischpur M, Mauz T, Meurer R.
Expedient Microwave-Assisted Synthesis of Novel 6-Substituted 5-Alkoxy(benzyloxy)-3,6-dihydro-2H-1,3,4-oxadiazin-2-ones.
Synlett 2012; 23(04):637–9. Verfügbar unter: http://www.thieme-connect.de/DOI/DOI?10.1055/s-0031-1290160.
Ha K, Chahar M, Monbaliu J-CM, Todadze E, Hansen FK, Oliferenko AA, Ocampo CE, Leino D, Lillicotch A, Stevens CV, Katritzky A. R
Long-range intramolecular S → N acyl migration: a study of the formation of native peptide analogues via 13-, 15-, and 16-membered cyclic transition states.
J Org Chem 2012; 77(6):2637–48. doi: 10.1021/jo2023125.
Hansen FK, Geffken D.
Efficient synthesis of flupirtine analogues derived from pyrimidine.
Journal of Heterocyclic Chemistry 2012; 49(2):321–8. Verfügbar unter: https://onlinelibrary.wiley.com/doi/10.1002/jhet.725.
Hansen FK, Khankischpur M, Tolaymat I, Mesaros R, Dannhardt G, Geffken D.
Efficient synthesis and 5-LOX/COX-inhibitory activity of some 3-hydroxybenzobthiophene-2-carboxylic acid derivatives.
Bioorg Med Chem Lett 2012; 22(15):5031–4. doi: 10.1016/j.bmcl.2012.06.012.
Monbaliu J-CM, Hansen FK, Beagle LK, Panzner MJ, Steel PJ, Todadze E, Stevens CV, Katritzky A. R
A new benzotriazole-mediated stereoflexible gateway to hetero-2,5-diketopiperazines.
Chemistry - A European Journal 2012; 18(9):2632–8. doi: 10.1002/chem.201103143.
Katritzky A, K. Hansen F, K. Beagle L, Todadze E.
Efficient Microwave-Assisted Synthesis of 1,2,4-Triazole-Based Peptidomimetics Using Benzotriazole Methodology.
Heterocycles 2012; 84(1):515. doi: 10.3987/COM-11-S(P)13.
2011
Draghici B, Hansen FK, Buciumas A-M, El-Gendy BE-DM, Todadze E, Katritzky A. R
Efficient microwave-assisted synthesis of aminoxy acid conjugates.
RSC Advances 2011; 1(4):602. Verfügbar unter: http://xlink.rsc.org/?DOI=c1ra00413a.
Hansen FK, Ha K, Todadze E, Lillicotch A, Frey A, Katritzky A. R
Microwave-assisted chemical ligation of S-acyl peptides containing non-terminal cysteine residues.
Org Biomol Chem 2011; 9(20):7162–7. doi: 10.1039/c1ob05740e.
Khankischpur M, Hansen FK, Meurer R, Mauz T, Bergmann B, Walter RD, Geffken D.
Facile synthesis and in-vitro antimalarial activity of novel α-hydroxy hydrazonates.
Archiv der Pharmazie 2011; 344(11):755–64. doi: 10.1002/ardp.201000346.
2010
Hansen F, Geffken D.
Expedient Microwave-Assisted Synthesis of 5-Benzoylamino-2-(aralkylsulfanyl)pyrimidin-4(3H)-ones.
Synthesis 2010; 2010(15):2583–7. Verfügbar unter: http://www.thieme-connect.de/DOI/DOI?10.1055/s-0029-1218841.
Hansen F, Geffken D.
Synthesis of Novel N,3-Substituted 3H-[1,2,3]Triazolo[4,5-d]pyrimidin-5-amines.
Synthesis 2010; 2010(04):689–93. Verfügbar unter: http://www.thieme-connect.de/DOI/DOI?10.1055/s-0029-1218597.
Khankischpur M, Hansen F, Geffken D.
Convenient Synthesis of 5-Substituted 2-Amino[1,2,4]triazolo[1,5- a][1,3,5]triazin-7(6H)-ones from N-Triazolide Imidates and 1,2,4-Triazole-3,5-diamine.
Synthesis 2010; 2010(10):1645–8. Verfügbar unter: http://www.thieme-connect.de/DOI/DOI?10.1055/s-0029-1218718.