Structure-enhanced methods in the development of non-nucleoside inhibitors targeting HIV reverse transcriptase variants.

Abstract:

:Resistance continues to emerge as a leading cause for antiretroviral treatment failure. Several mutations in HIV reverse transcriptase (RT) confer resistance to non-nucleoside inhibitors (NNRTIs), vital components of antiretroviral combination therapies. Since the majority of mutations are located in the NNRTI binding pocket, crystal structures of RT variants in complex with NNRTIs have provided ideas for new drug design strategies. This article reviews the impact of RT crystal structures on the multidisciplinary design and development of new inhibitors with improved resistance profiles.

journal_name

Future Microbiol

journal_title

Future microbiology

authors

Frey KM

doi

10.2217/fmb.15.122

subject

Has Abstract

pub_date

2015-01-01 00:00:00

pages

1767-72

issue

11

eissn

1746-0913

issn

1746-0921

journal_volume

10

pub_type

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