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One-pot, multi-component synthesis and structure-activity relationships of peptoid-based histone deacetylase (HDAC) inhibitors targeting malaria parasites.
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 FK. Diedrich D, et al. Eur J Med Chem. 2018 Oct 5;158:801-813. doi: 10.1016/j.ejmech.2018.09.018. Epub 2018 Sep 7. Eur J Med Chem. 2018. PMID: 30245402 Free PMC article.
Structure-Activity and Structure-Toxicity Relationships of Peptoid-Based Histone Deacetylase Inhibitors with Dual-Stage Antiplasmodial Activity.
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 FK. Mackwitz MKW, et al. Among authors: diedrich d. ChemMedChem. 2019 May 6;14(9):912-926. doi: 10.1002/cmdc.201800808. Epub 2019 Feb 19. ChemMedChem. 2019. PMID: 30664827 Free PMC article.
Development of a First-in-Class Small-Molecule Inhibitor of the C-Terminal Hsp90 Dimerization.
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. Bhatia S, et al. Among authors: diedrich d. ACS Cent Sci. 2022 May 25;8(5):636-655. doi: 10.1021/acscentsci.2c00013. Epub 2022 Apr 27. ACS Cent Sci. 2022. PMID: 35647282 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: diedrich d. 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.
127 results