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A novel assay to identify entry inhibitors that block binding of HIV-1 gp120 to CCR5

descriptionPublicationkeyboard_double_arrow_right Article 01 Sep 2004Publisher:Elsevier BVJournal:Virology, volume 326, pages 299-309 (issn: 0042-6822,

Authors: Qian Zhao; Yuxian He; Asim K. Debnath; Gabriel Alespeiti;

doi: 10.1016/j.virol.2004.06.022

pmid: 15321703

A novel assay to identify entry inhibitors that block binding of HIV-1 gp120 to CCR5

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Abstract

HIV-1 infection is initiated by the interaction of the envelope glycoprotein gp120 with the cellular receptor CD4 that triggers conformational changes in gp120 necessary for subsequent interaction with a coreceptor CCR5 (or CXCR4). The CD4-induced (CD4i) conformation of gp120 can be mimicked by a full-length single chain (FLSC) protein consisting of gp120 linked with the D1D2 domains of CD4 by a 20-amino-acid linker. We have used this protein to establish a flow cytometry-based assay and an ELISA-based assay to identify inhibitors that block the binding of gp120 to CCR5. Both assays are specific for detecting the known CCR5 antagonist TAK-779, but the ELISA-based assay was more sensitive, simple, inexpensive, and rapid; thus, it can be adapted to high throughput screening (HTS). The ELISA-based method was validated with a diverse set of known antagonists, for example, TAK-779, AOP-RANTES, PSC-RANTES, and several mAbs.

Related Organizations

New York Blood Center
United States

Keywords

Benzylamines, Receptors, CXCR4, Receptors, CCR5, Anti-HIV Agents, Protein Conformation, Envelope glycoprotein, Enzyme-Linked Immunosorbent Assay, HIV Infections, HIV Envelope Protein gp120, Cyclams, Cell Line, Heterocyclic Compounds, Virology, Animals, Flow cytometry, Fusion, Dose-Response Relationship, Drug, Virulence, HIV, Entry inhibitor, Flow Cytometry, Amides, Quaternary Ammonium Compounds, CCR5 Receptor Antagonists, CD4 Antigens, HIV-1, Cell-based assay, ELISA, CCR5, Coreceptor

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