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Infectious Disorders - Drug Targets

Editor-in-Chief

ISSN (Print): 1871-5265
ISSN (Online): 2212-3989

HIV Co-Receptor CCR5: Structure and Interactions with Inhibitors

Author(s): Ting Wang and Yong Duan

Volume 9, Issue 3, 2009

Page: [279 - 288] Pages: 10

DOI: 10.2174/1871526510909030279

Price: $65

Abstract

The CC-chemokine receptor 5 (CCR5), a membrane protein belonging to the G-protein coupled receptor superfamily, has been identified as an essential co-receptor for HIV entry into the cells, and small molecules that inhibit HIV entry by targeting CCR5 have been in fast development as antiviral agents. This review focuses on computational studies of predicting the CCR5 structure and its interactions with known small molecule inhibitors and discusses how the recently solved GPCR structures would provide new insights into the modeling of CCR5-inhibitior binding. In addition, this review pays a particular attention to the design of the inhibitors that specifically interrupt the viral entry co-receptor activity of CCR5 while preserving its normal chemokine receptor function to minimize side effects and toxicity.

Keywords: CC-chemokine Receptor 5 (CCR5), HIV entry inhibitors, homology modeling, G-protein coupled receptor (GPCR), molecular docking, drug design


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