[Coreceptors of HIV infection and the development of HIV entry inhibitors: overview and targets].

Abstract

In 1996 CXCR4 was identified as a coreceptor for HIV-1. This finding has lead to further identification of more than ten G-protein-coupled receptors (GPCRs) as coreceptors for HIV/SIV. Cell tropisms and coreceptor uses of HIV during the course of HIV infection are summarized. Promiscuous properties of correlations between chemokines and their chemokine receptor uses and also between variable amino acid sequences in the V3 region of HIV gp120 Env and HIV coreceptor uses are discussed. This promiscuous property of HIV-1 is claimed to be a possible cause of a difficulty in developing highly effective entry inhibitors and in addition to allow rapid appearance of immune escape HIV mutants. Representative agents that inhibit HIV entry with a special reference to inhibitors of coreceptor use and gp41 function are summarized. gp41 is discussed as a promising target for the development of effective entry inhibitors.

• Authors: Hiroo Hoshino
• Journal: Nihon rinsho. Japanese journal of clinical medicine (Nihon Rinsho) Vol. 60 Issue 1 Pg. 81-7 (Jan 2002) ISSN: 0047-1852 [Print] Japan
• PMID: 11808343 (Publication Type: English Abstract, Journal Article, Review)

Chemical References

• HIV Envelope Protein gp120
• HIV Envelope Protein gp41
• HIV Fusion Inhibitors
• Ligands
• Receptors, CCR5
• Receptors, CXCR4
• Receptors, Cell Surface
• Receptors, Chemokine
• GTP-Binding Proteins

Topics

• Amino Acid Sequence
• Animals
• Drug Design
• GTP-Binding Proteins
• HIV Envelope Protein gp120 (chemistry, genetics)
• HIV Envelope Protein gp41
• HIV Fusion Inhibitors
• HIV Infections
• HIV-1 (pathogenicity)
• Humans
• Ligands
• Mutation
• Receptors, CCR5
• Receptors, CXCR4
• Receptors, Cell Surface
• Receptors, Chemokine