HIV-1 protease mutation 82M contributes to phenotypic resistance to protease inhibitors in subtype G

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HIV-1 protease mutation 82M contributes to phenotypic resistance to protease inhibitors in subtype G.

OBJECTIVES The purpose of this study was the qualitative and quantitative assessment of the in vitro effect of HIV-1 protease (PR) mutation 82M on replication capacity and susceptibility to the eight clinically available PR inhibitors (PIs). METHODS The 82M substitution was introduced by site-directed mutagenesis in wild-type subtype B and G strains, as well as reverted back to wild-type in a...

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Resistance mechanism of human immunodeficiency virus type-1 protease to inhibitors: A molecular dynamic approach

Human immunodeficiency virus type 1 (HIV-1) protease inhibitors comprise an important class of drugs used in HIV treatments. However, mutations of protease genes accelerated by low fidelity of reverse transcriptase yield drug resistant mutants of reduced affinities for the inhibitors. This problem is considered to be a serious barrier against HIV treatment for the foreseeable future. In this st...

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HIV-1 protease inhibitors.

Treatment of human immunodeficiency virus type 1 (HIV-1) infection with regimens that include protease inhibitors (PIs) has contributed to marked improvements in HIV-related disease progression and mortality. Five PIs are approved by the US Food and Drug Administration and have potent activity in vitro. PIs with 2 nucleoside analogue reverse transcriptase inhibitors have demonstrated prolonged ...

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Role of Gag in HIV Resistance to Protease Inhibitors

Cleavage of Gag and Gag-Pol precursors by the viral protease is an essential step in the replication cycle of HIV. Protease inhibitors, which compete with natural cleavage sites, strongly impair viral infectivity and have proven to be highly valuable in the treatment of HIV-infected subjects. However, as with all other antiretroviral drugs, the clinical benefit of protease inhibitors can be com...

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Screening Efficacy of Available HIV Protease Inhibitors on COVID-19 Protease

Background and Aim: Advent of COVID-19 attracted the attentions of researchers to develop drugs for its treatment. Besides efforts on developing new drugs, screening available drugs for efficacy on COVID-19 could be an urgent action of initiating its pharmacotherapy. In this study, efficacy of HIV protease inhibitors on COVID-19 protease has been examined. Methods: Molecular docking based scree...

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ژورنال

عنوان ژورنال: Journal of Antimicrobial Chemotherapy

سال: 2012

ISSN: 0305-7453,1460-2091

DOI: 10.1093/jac/dks010