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Bioorg Med Chem Lett. 2009 Nov 1;19(21):6087-91. doi: 10.1016/j.bmcl.2009.09.029. Epub 2009 Sep 13.

A dynamic target-based pharmacophoric model mapping the CD4 binding site on HIV-1 gp120 to identify new inhibitors of gp120-CD4 protein-protein interactions.

Author information

  • 1Dipartimento Farmaco Chimico Tecnologico, Università degli Studi di Siena, Via Alcide de Gasperi, 2, 53100 Siena, Italy.

Abstract

A dynamic target-based pharmacophoric model mapping the CD4 binding site on HIV-1 gp120 was built and used to identify new hits able to inhibit gp120-CD4 protein-protein interactions. Two compounds showed micromolar inhibition of HIV-1 replication in cells attributable to an interference with the entry step of infection, by direct interaction with gp120. Inactivity of compounds toward a M475I strain suggested specific contacts with the Phe43 cavity of gp120.

PMID:
19783140
[PubMed - indexed for MEDLINE]
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