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The stereoselective targeting of a specific enzyme-substrate complex is the molecular mechanism for the synergic inhibition of HIV-1 reverse transcriptase by (R)-(-)-PPO464: a novel generation of nonnucleoside inhibitors.
Maga G, Ramunno A, Nacci V, Locatelli GA, Spadari S, Fiorini I, Baldanti F, Paolucci S, Zavattoni M, Bergamini A, Galletti B, Muck S, Hubscher U, Giorgi G, Guiso G, Caccia S, Campiani G. Maga G, et al. Among authors: hubscher u. J Biol Chem. 2001 Nov 30;276(48):44653-62. doi: 10.1074/jbc.M106702200. Epub 2001 Sep 25. J Biol Chem. 2001. PMID: 11572864 Free article.
Nevirapine resistance mutation at codon 181 of the HIV-1 reverse transcriptase confers stavudine resistance by increasing nucleotide substrate discrimination and phosphorolytic activity.
Blanca G, Baldanti F, Paolucci S, Skoblov AY, Victorova L, Hübscher U, Gerna G, Spadari S, Maga G. Blanca G, et al. Among authors: hubscher u. J Biol Chem. 2003 May 2;278(18):15469-72. doi: 10.1074/jbc.C300022200. Epub 2003 Feb 24. J Biol Chem. 2003. PMID: 12601008 Free article.
Effects of drug resistance mutations L100I and V106A on the binding of pyrrolobenzoxazepinone nonnucleoside inhibitors to the human immunodeficiency virus type 1 reverse transcriptase catalytic complex.
Locatelli GA, Campiani G, Cancio R, Morelli E, Ramunno A, Gemma S, Hübscher U, Spadari S, Maga G. Locatelli GA, et al. Among authors: hubscher u. Antimicrob Agents Chemother. 2004 May;48(5):1570-80. doi: 10.1128/AAC.48.5.1570-1580.2004. Antimicrob Agents Chemother. 2004. PMID: 15105107 Free PMC article.
Drug resistance mutations in the nucleotide binding pocket of human immunodeficiency virus type 1 reverse transcriptase differentially affect the phosphorolysis-dependent primer unblocking activity in the presence of stavudine and zidovudine and its inhibition by efavirenz.
Crespan E, Locatelli GA, Cancio R, Hübscher U, Spadari S, Maga G. Crespan E, et al. Among authors: hubscher u. Antimicrob Agents Chemother. 2005 Jan;49(1):342-9. doi: 10.1128/AAC.49.1.342-349.2005. Antimicrob Agents Chemother. 2005. PMID: 15616314 Free PMC article.
High potency of indolyl aryl sulfone nonnucleoside inhibitors towards drug-resistant human immunodeficiency virus type 1 reverse transcriptase mutants is due to selective targeting of different mechanistic forms of the enzyme.
Cancio R, Silvestri R, Ragno R, Artico M, De Martino G, La Regina G, Crespan E, Zanoli S, Hübscher U, Spadari S, Maga G. Cancio R, et al. Among authors: hubscher u. Antimicrob Agents Chemother. 2005 Nov;49(11):4546-54. doi: 10.1128/AAC.49.11.4546-4554.2005. Antimicrob Agents Chemother. 2005. PMID: 16251294 Free PMC article.
267 results