Resistance to Integrase Inhibitors

Integrase (IN) is a clinically validated target for the treatment of human immunodeficiency virus infections and raltegravir exhibits remarkable clinical activity. The next most advanced IN inhibitor is elvitegravir. However, mutant viruses lead to treatment failure and mutations within the IN codin...

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Autores principales: Métifiot, Mathieu, Marchand, Christophe, Maddali, Kasthuraiah, Pommier, Yves
Formato: Texto
Lenguaje:English
Publicado: Molecular Diversity Preservation International (MDPI) 2010
Materias:
Review
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC2920056/
https://www.ncbi.nlm.nih.gov/pubmed/20706558
http://dx.doi.org/10.3390/v2071347
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author Métifiot, Mathieu
Marchand, Christophe
Maddali, Kasthuraiah
Pommier, Yves
author_facet Métifiot, Mathieu
Marchand, Christophe
Maddali, Kasthuraiah
Pommier, Yves
author_sort Métifiot, Mathieu
collection PubMed
description Integrase (IN) is a clinically validated target for the treatment of human immunodeficiency virus infections and raltegravir exhibits remarkable clinical activity. The next most advanced IN inhibitor is elvitegravir. However, mutant viruses lead to treatment failure and mutations within the IN coding sequence appear to confer cross-resistance. The characterization of those mutations is critical for the development of second generation IN inhibitors to overcome resistance. This review focuses on IN resistance based on structural and biochemical data, and on the role of the IN flexible loop i.e., between residues G140-G149 in drug action and resistance.
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spelling pubmed-29200562010-08-11 Resistance to Integrase Inhibitors Métifiot, Mathieu Marchand, Christophe Maddali, Kasthuraiah Pommier, Yves Viruses Review Integrase (IN) is a clinically validated target for the treatment of human immunodeficiency virus infections and raltegravir exhibits remarkable clinical activity. The next most advanced IN inhibitor is elvitegravir. However, mutant viruses lead to treatment failure and mutations within the IN coding sequence appear to confer cross-resistance. The characterization of those mutations is critical for the development of second generation IN inhibitors to overcome resistance. This review focuses on IN resistance based on structural and biochemical data, and on the role of the IN flexible loop i.e., between residues G140-G149 in drug action and resistance. Molecular Diversity Preservation International (MDPI) 2010-06-25 /pmc/articles/PMC2920056/ /pubmed/20706558 http://dx.doi.org/10.3390/v2071347 Text en © 2010 by the authors; licensee MDPI, Basel, Switzerland. http://creativecommons.org/licenses/by/3.0 This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution license (http://creativecommons.org/licenses/by/3.0/).
spellingShingle Review
Métifiot, Mathieu
Marchand, Christophe
Maddali, Kasthuraiah
Pommier, Yves
Resistance to Integrase Inhibitors
title Resistance to Integrase Inhibitors
title_full Resistance to Integrase Inhibitors
title_fullStr Resistance to Integrase Inhibitors
title_full_unstemmed Resistance to Integrase Inhibitors
title_short Resistance to Integrase Inhibitors
title_sort resistance to integrase inhibitors
topic Review
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC2920056/
https://www.ncbi.nlm.nih.gov/pubmed/20706558
http://dx.doi.org/10.3390/v2071347
work_keys_str_mv AT metifiotmathieu resistancetointegraseinhibitors
AT marchandchristophe resistancetointegraseinhibitors
AT maddalikasthuraiah resistancetointegraseinhibitors
AT pommieryves resistancetointegraseinhibitors

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