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Recent progress in discovery of small-molecule CCR5 chemokine receptor ligands as HIV-1 inhibitors.

Abstract：

:This review addresses key pharmacology and virology issues relevant in discovery and development of CCR5 antagonists as anti-HIV drugs, such as target validation, receptor internalization, allosterism, viral resistance and tropism. Recent progress in the discovery and development of CCR5 antagonists, SAR and clinical status are reviewed. Finally, modeling-based structure of CCR5 is discussed in the context of a small-molecule antagonism of the CCR5 receptor.

journal_name

Bioorg Med Chem

journal_title

Bioorganic & medicinal chemistry

authors

Kazmierski W,Bifulco N,Yang H,Boone L,DeAnda F,Watson C,Kenakin T

doi

10.1016/s0968-0896(03)00161-5

subject

Has Abstract

pub_date

2003-07-03 00:00:00

pages

2663-76

issue

13

eissn

0968-0896

issn

1464-3391

pii

S0968089603001615

journal_volume

11

pub_type

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