Chemokine antagonists as therapeutics: focus on HIV-1.

Abstract:

:Human immunodeficiency virus type 1 (HIV-1) entry into target cells is a multistep process involving the interaction of viral envelope proteins with cell surface receptors. Binding to CD4 is followed by engagement of specific chemokine receptors (CCR5 or CXCR4), triggering molecular rearrangements in the envelope transmembrane subunit that result in membrane fusion. Chemokine receptor antagonists that block the interaction of the HIV-1 envelope with CCR5 or CXCR4 potently inhibit HIV-1 in vitro. Pilot studies of orally bioavailable small-molecule CCR5 inhibitors in HIV-1-infected subjects have provided proof of concept for this novel drug class; phase III safety and efficacy trials are under way.

journal_name

Annu Rev Med

authors

Tsibris AM,Kuritzkes DR

doi

10.1146/annurev.med.58.080105.102908

subject

Has Abstract

pub_date

2007-01-01 00:00:00

pages

445-59

eissn

0066-4219

issn

1545-326X

journal_volume

58

pub_type

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