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Article

HIV-1 entry inhibition by small-molecule CCR5 antagonists: a combined molecular modeling and mutant study using a high-throughput assay.

Virology - 10 May 2011

Labrecque Jean, Metz Markus, Lau Gloria, Darkes Marilyn C, Wong Rebecca S Y, Bogucki David, Carpenter Bryon, Chen Gang, Li Tongshuang, Nan Susan, Schols Dominique, Bridger Gary J, Fricker Simon P, Skerlj Renato T

Abstract excerpt

Based on the attrition rate of CCR5 small molecule antagonists in the clinic the discovery and development of next generation antagonists with an improved pharmacology and safety profile is necessary. Herein, we describe a combined molecular modeling, CCR5-mediated cell fusion, and receptor site-directed mutagenesis approach to study the molecular interactions of six structurally diverse compounds (aplaviroc,...

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Share to CCR5 Receptor Antagonists
Share to High-Throughput Screening Assays

Methodology Data sources Editorial policy Privacy About Contact Helena Bioinformatics

Share to HIV Fusion Inhibitors

Share to Mutagenesis, Site-Directed

Share to Receptors, CCR5

Share to Reproducibility of Results

Share to Stereoisomerism

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Source

Identifiers

PMID: 21388649
DOI: 10.1016/j.virol.2011.02.016

Genes

CCR5

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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