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Unusual binding mode of an HIV-1 protease inhibitor explains its potency against multi-drug-resistant virus strains.
Weber J, Mesters JR, Lepsík M, Prejdová J, Svec M, Sponarová J, Mlcochová P, Skalická K, Strísovský K, Uhlíková T, Soucek M, Machala L, Stanková M, Vondrásek J, Klimkait T, Kraeusslich HG, Hilgenfeld R, Konvalinka J. Weber J, et al. Among authors: lepsik m. J Mol Biol. 2002 Dec 6;324(4):739-54. doi: 10.1016/s0022-2836(02)01139-7. J Mol Biol. 2002. PMID: 12460574
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: lepsik m. 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.
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: lepsik m. 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.
83 results