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Potent HIV-1 protease inhibitors incorporating meso-bicyclic urethanes as P2-ligands: structure-based design, synthesis, biological evaluation and protein-ligand X-ray studies.
Ghosh AK, Gemma S, Takayama J, Baldridge A, Leshchenko-Yashchuk S, Miller HB, Wang YF, Kovalevsky AY, Koh Y, Weber IT, Mitsuya H. Ghosh AK, et al. Among authors: mitsuya h. Org Biomol Chem. 2008 Oct 21;6(20):3703-13. doi: 10.1039/b809178a. Epub 2008 Aug 11. Org Biomol Chem. 2008. PMID: 18843400 Free PMC article.
Novel bis-tetrahydrofuranylurethane-containing nonpeptidic protease inhibitor (PI) UIC-94017 (TMC114) with potent activity against multi-PI-resistant human immunodeficiency virus in vitro.
Koh Y, Nakata H, Maeda K, Ogata H, Bilcer G, Devasamudram T, Kincaid JF, Boross P, Wang YF, Tie Y, Volarath P, Gaddis L, Harrison RW, Weber IT, Ghosh AK, Mitsuya H. Koh Y, et al. Among authors: mitsuya h. Antimicrob Agents Chemother. 2003 Oct;47(10):3123-9. doi: 10.1128/AAC.47.10.3123-3129.2003. Antimicrob Agents Chemother. 2003. PMID: 14506019 Free PMC article.
Altered HIV-1 Gag protein interactions with cyclophilin A (CypA) on the acquisition of H219Q and H219P substitutions in the CypA binding loop.
Gatanaga H, Das D, Suzuki Y, Yeh DD, Hussain KA, Ghosh AK, Mitsuya H. Gatanaga H, et al. Among authors: mitsuya h. J Biol Chem. 2006 Jan 13;281(2):1241-50. doi: 10.1074/jbc.M505920200. Epub 2005 Nov 7. J Biol Chem. 2006. PMID: 16275650 Free article.
Among the amino acid substitutions identified in Gag noncleavage sites in HIV-1 variants resistant to protease inhibitors, H219Q (Gatanaga, H., Suzuki, Y., Tsang, H., Yoshimura, K., Kavlick, M. F., Nagashima, K., Gorelick, R. J., Mardy, S., Tang, C., Summers, M. F., …
Among the amino acid substitutions identified in Gag noncleavage sites in HIV-1 variants resistant to protease inhibitors, H219Q (Gatanaga, …
Structure-based design of novel HIV-1 protease inhibitors to combat drug resistance.
Ghosh AK, Sridhar PR, Leshchenko S, Hussain AK, Li J, Kovalevsky AY, Walters DE, Wedekind JE, Grum-Tokars V, Das D, Koh Y, Maeda K, Gatanaga H, Weber IT, Mitsuya H. Ghosh AK, et al. Among authors: mitsuya h. J Med Chem. 2006 Aug 24;49(17):5252-61. doi: 10.1021/jm060561m. J Med Chem. 2006. PMID: 16913714
716 results