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4-Oxo-β-lactams as Covalent Inhibitors of the Mitochondrial Intramembrane Protease PARL.
Ji S, Bach K, Miriyala VM, Dohnálek J, Riopedre-Fernandez M, Lepšík M, van de Plassche M, Vanhoutte R, Barniol-Xicota M, Moreira R, Strisovsky K, Verhelst SHL. Ji S, et al. Among authors: strisovsky k. ACS Med Chem Lett. 2024 Nov 14;15(12):2101-2106. doi: 10.1021/acsmedchemlett.4c00384. eCollection 2024 Dec 12. ACS Med Chem Lett. 2024. PMID: 39691509
Extensive targeting of chemical space at the prime side of ketoamide inhibitors of rhomboid proteases by branched substituents empowers their selectivity and potency.
Bach K, Dohnálek J, Škerlová J, Kuzmík J, Poláchová E, Stanchev S, Majer P, Fanfrlík J, Pecina A, Řezáč J, Lepšík M, Borshchevskiy V, Polovinkin V, Strisovsky K. Bach K, et al. Among authors: strisovsky k. Eur J Med Chem. 2024 Sep 5;275:116606. doi: 10.1016/j.ejmech.2024.116606. Epub 2024 Jun 17. Eur J Med Chem. 2024. PMID: 38901105 Free article.
General and Modular Strategy for Designing Potent, Selective, and Pharmacologically Compliant Inhibitors of Rhomboid Proteases.
Tichá A, Stanchev S, Vinothkumar KR, Mikles DC, Pachl P, Began J, Škerle J, Švehlová K, Nguyen MTN, Verhelst SHL, Johnson DC, Bachovchin DA, Lepšík M, Majer P, Strisovsky K. Tichá A, et al. Among authors: strisovsky k. Cell Chem Biol. 2017 Dec 21;24(12):1523-1536.e4. doi: 10.1016/j.chembiol.2017.09.007. Epub 2017 Oct 26. Cell Chem Biol. 2017. PMID: 29107700 Free PMC article.
Discovery and Biological Evaluation of Potent and Selective N-Methylene Saccharin-Derived Inhibitors for Rhomboid Intramembrane Proteases.
Goel P, Jumpertz T, Mikles DC, Tichá A, Nguyen MTN, Verhelst S, Hubalek M, Johnson DC, Bachovchin DA, Ogorek I, Pietrzik CU, Strisovsky K, Schmidt B, Weggen S. Goel P, et al. Among authors: strisovsky k. Biochemistry. 2017 Dec 26;56(51):6713-6725. doi: 10.1021/acs.biochem.7b01066. Epub 2017 Dec 12. Biochemistry. 2017. PMID: 29185711 Free PMC article.
The zymogenic form of SARS-CoV-2 main protease: A discrete target for drug discovery.
Novotný P, Humpolíčková J, Nováková V, Stanchev S, Stříšovský K, Zgarbová M, Weber J, Kryštůfek R, Starková J, Hradilek M, Moravcová A, Günterová J, Bach K, Majer P, Konvalinka J, Majerová T. Novotný P, et al. Among authors: strisovsky k. J Biol Chem. 2024 Dec 14;301(1):108079. doi: 10.1016/j.jbc.2024.108079. Online ahead of print. J Biol Chem. 2024. PMID: 39675720 Free article.
48 results