Literature DB >> 16475939

HIV-1 reverse transcriptase: a therapeutical target in the spotlight.

H C Castro1, N I V Loureiro, M Pujol-Luz, A M T Souza, M G Albuquerque, D O Santos, L M Cabral, I C Frugulhetti, C R Rodrigues.   

Abstract

Human Immunodeficiency Virus type 1 Reverse Transcriptase (HIV-1 RT) is one of the most important targets for treatment of Acquired Immune Deficiency Syndrome (AIDS). It catalyzes the reverse transcription of HIV-RNA into a double stranded DNA, and the knowledge of its substrate specificity and catalytic mechanism has guided the development of several inhibitors widely used on current HIV/AIDS therapy. However, mutations in HIV-1 RT structure can lead to the emergence of drug-resistant virus strains. The goal of this review is to summarize relevant structural features of HIV-1 RT and its inhibitors in such a way that this cost-effective target in the development of new antiretroviral drugs is particularly highlighted.

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Year:  2006        PMID: 16475939     DOI: 10.2174/092986706775476089

Source DB:  PubMed          Journal:  Curr Med Chem        ISSN: 0929-8673            Impact factor:   4.530


  13 in total

1.  Antiviral activity and in vitro mutation development pathways of MK-6186, a novel nonnucleoside reverse transcriptase inhibitor.

Authors:  Meiqing Lu; Peter J Felock; Vandna Munshi; Renee C Hrin; Ying-Jie Wang; Youwei Yan; Sanjeev Munshi; Georgia B McGaughey; Robert Gomez; Neville J Anthony; Theresa M Williams; Jay A Grobler; Daria J Hazuda; Philip M McKenna; Michael D Miller; Ming-Tain Lai
Journal:  Antimicrob Agents Chemother       Date:  2012-03-05       Impact factor: 5.191

2.  In vitro resistance selection with doravirine (MK-1439), a novel nonnucleoside reverse transcriptase inhibitor with distinct mutation development pathways.

Authors:  Meizhen Feng; Deping Wang; Jay A Grobler; Daria J Hazuda; Michael D Miller; Ming-Tain Lai
Journal:  Antimicrob Agents Chemother       Date:  2014-11-10       Impact factor: 5.191

3.  Doravirine and Islatravir Have Complementary Resistance Profiles and Create a Combination with a High Barrier to Resistance.

Authors:  Ming-Tain Lai; Meizhen Feng; Min Xu; Winnie Ngo; Tracy L Diamond; Carey Hwang; Jay A Grobler; Daria J Hazuda; Ernest Asante-Appiah
Journal:  Antimicrob Agents Chemother       Date:  2022-05-02       Impact factor: 5.191

4.  Antiviral activity of MK-4965, a novel nonnucleoside reverse transcriptase inhibitor.

Authors:  Ming-Tain Lai; Vandna Munshi; Sinoeun Touch; Robert M Tynebor; Thomas J Tucker; Philip M McKenna; Theresa M Williams; Daniel J DiStefano; Daria J Hazuda; Michael D Miller
Journal:  Antimicrob Agents Chemother       Date:  2009-03-16       Impact factor: 5.191

5.  Mutations in human immunodeficiency virus type 1 RNase H primer grip enhance 3'-azido-3'-deoxythymidine resistance.

Authors:  Krista A Delviks-Frankenberry; Galina N Nikolenko; Rebekah Barr; Vinay K Pathak
Journal:  J Virol       Date:  2007-04-11       Impact factor: 5.103

6.  In vitro characterization of MK-1439, a novel HIV-1 nonnucleoside reverse transcriptase inhibitor.

Authors:  Ming-Tain Lai; Meizhen Feng; Jean-Pierre Falgueyret; Paul Tawa; Marc Witmer; Daniel DiStefano; Yuan Li; Jason Burch; Nancy Sachs; Meiqing Lu; Elizabeth Cauchon; Louis-Charles Campeau; Jay Grobler; Youwei Yan; Yves Ducharme; Bernard Côté; Ernest Asante-Appiah; Daria J Hazuda; Michael D Miller
Journal:  Antimicrob Agents Chemother       Date:  2013-12-30       Impact factor: 5.191

7.  Inhibitory activity of 9-phenylcyclohepta[d]pyrimidinedione derivatives against different strains of HIV-1 as non-nucleoside reverse transcriptase inhibitors.

Authors:  Yang Huang; Xiaowei Wang; Xiaoling Yu; Lin Yuan; Ying Guo; Weisi Xu; Tiejun Liu; Junyi Liu; Yiming Shao; Liying Ma
Journal:  Virol J       Date:  2011-05-15       Impact factor: 4.099

8.  Molecular docking studies of marine diterpenes as inhibitors of wild-type and mutants HIV-1 reverse transcriptase.

Authors:  Leonardo A Miceli; Valéria L Teixeira; Helena C Castro; Carlos R Rodrigues; Juliana F R Mello; Magaly G Albuquerque; Lucio M Cabral; Monique A de Brito; Alessandra M T de Souza
Journal:  Mar Drugs       Date:  2013-10-29       Impact factor: 5.118

9.  Synthesis and biological evaluation of 2-thioxopyrimidin-4(1H)-one derivatives as potential non-nucleoside HIV-1 reverse transcriptase inhibitors.

Authors:  Nagy M Khalifa; Mohamed A Al-Omar
Journal:  Int J Mol Sci       Date:  2014-11-12       Impact factor: 5.923

10.  Prediction of mutational tolerance in HIV-1 protease and reverse transcriptase using flexible backbone protein design.

Authors:  Elisabeth Humphris-Narayanan; Eyal Akiva; Rocco Varela; Shane Ó Conchúir; Tanja Kortemme
Journal:  PLoS Comput Biol       Date:  2012-08-23       Impact factor: 4.475

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