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Development of the first geldanamycin-based HSP90 degraders.
Wurnig S, Vogt M, Hogenkamp J, Dienstbier N, Borkhardt A, Bhatia S, Hansen FK. Wurnig S, et al. Among authors: hansen fk. Front Chem. 2023 Jun 28;11:1219883. doi: 10.3389/fchem.2023.1219883. eCollection 2023. Front Chem. 2023. PMID: 37448856 Free PMC article.
Targeting HSP90 dimerization via the C terminus is effective in imatinib-resistant CML and lacks the heat shock response.
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. Bhatia S, et al. Among authors: hansen fk. Blood. 2018 Jul 19;132(3):307-320. doi: 10.1182/blood-2017-10-810986. Epub 2018 May 3. Blood. 2018. PMID: 29724897 Free PMC article.
Discovery of the First-in-Class Dual Histone Deacetylase-Proteasome Inhibitor.
Bhatia S, Krieger V, Groll M, Osko JD, Reßing N, Ahlert H, Borkhardt A, Kurz T, Christianson DW, Hauer J, Hansen FK. Bhatia S, et al. Among authors: hansen fk. J Med Chem. 2018 Nov 21;61(22):10299-10309. doi: 10.1021/acs.jmedchem.8b01487. Epub 2018 Nov 8. J Med Chem. 2018. PMID: 30365892 Free PMC article.
Hydroxamic Acids Immobilized on Resins (HAIRs): Synthesis of Dual-Targeting HDAC Inhibitors and HDAC Degraders (PROTACs).
Sinatra L, Bandolik JJ, Roatsch M, Sönnichsen M, Schoeder CT, Hamacher A, Schöler A, Borkhardt A, Meiler J, Bhatia S, Kassack MU, Hansen FK. Sinatra L, et al. Among authors: hansen fk. Angew Chem Int Ed Engl. 2020 Dec 7;59(50):22494-22499. doi: 10.1002/anie.202006725. Epub 2020 Oct 9. Angew Chem Int Ed Engl. 2020. PMID: 32780485 Free PMC article.
Multicomponent Synthesis, Binding Mode, and Structure-Activity Relationship of Selective Histone Deacetylase 6 (HDAC6) Inhibitors with Bifurcated Capping Groups.
Reßing N, Sönnichsen M, Osko JD, Schöler A, Schliehe-Diecks J, Skerhut A, Borkhardt A, Hauer J, Kassack MU, Christianson DW, Bhatia S, Hansen FK. Reßing N, et al. Among authors: hansen fk. J Med Chem. 2020 Sep 24;63(18):10339-10351. doi: 10.1021/acs.jmedchem.9b01888. Epub 2020 Sep 1. J Med Chem. 2020. PMID: 32803970 Free PMC article.
4-Acyl Pyrrole Capped HDAC Inhibitors: A New Scaffold for Hybrid Inhibitors of BET Proteins and Histone Deacetylases as Antileukemia Drug Leads.
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 FK. Schäker-Hübner L, et al. Among authors: hansen fk. J Med Chem. 2021 Oct 14;64(19):14620-14646. doi: 10.1021/acs.jmedchem.1c01119. Epub 2021 Sep 28. J Med Chem. 2021. PMID: 34582215
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