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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. 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.
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: cancio r. 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.
Gln145Met/Leu changes in human immunodeficiency virus type 1 reverse transcriptase confer resistance to nucleoside and nonnucleoside analogs and impair virus replication.
Paolucci S, Baldanti F, Maga G, Cancio R, Zazzi M, Zavattoni M, Chiesa A, Spadari S, Gerna G. Paolucci S, et al. Among authors: cancio r. Antimicrob Agents Chemother. 2004 Dec;48(12):4611-7. doi: 10.1128/AAC.48.12.4611-4617.2004. Antimicrob Agents Chemother. 2004. PMID: 15561833 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: cancio r. 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.
Selective targeting of the HIV-1 reverse transcriptase catalytic complex through interaction with the "primer grip" region by pyrrolobenzoxazepinone non-nucleoside inhibitors correlates with increased activity towards drug-resistant mutants.
Zanoli S, Gemma S, Butini S, Brindisi M, Joshi BP, Campiani G, Fattorusso C, Persico M, Crespan E, Cancio R, Spadari S, Hübscher U, Maga G. Zanoli S, et al. Among authors: cancio r. Biochem Pharmacol. 2008 Jul 15;76(2):156-68. doi: 10.1016/j.bcp.2008.04.009. Epub 2008 Apr 29. Biochem Pharmacol. 2008. PMID: 18541223
34 results