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Article

Structure-Guided Optimization of HIV Integrase Strand Transfer Inhibitors.

Journal of medicinal chemistry - 14 Sept 2017

Zhao Xue Zhi, Smith Steven J, Maskell Daniel P, Métifiot Mathieu, Pye Valerie E, Fesen Katherine, Marchand Christophe, Pommier Yves, Cherepanov Peter, Hughes Stephen H, Burke Terrence R

Abstract excerpt

Integrase mutations can reduce the effectiveness of the first-generation FDA-approved integrase strand transfer inhibitors (INSTIs), raltegravir (RAL) and elvitegravir (EVG). The second-generation agent, dolutegravir (DTG), has enjoyed considerable clinical success; however, resistance-causing mutations that diminish the efficacy of DTG have appeared. Our current findings support and extend the substrate envelope...

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Methodology Data sources Editorial policy Privacy About Contact Helena Bioinformatics

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Source

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Identifiers

PMID: 28737946
DOI: 10.1021/acs.jmedchem.7b00596
PMCID: PMC5601359

Provenance

PubMed metadata and Literature Corpus relationships. Corpus snapshot updated 7 Sept 2026. Manifest publication-graph-cohort-2026-09-07.1.

Source receipt: pubmed, retrieved 7 Sept 2026.

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