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Bioorg Med Chem Lett. 2012 May 1;22(9):3358-61. doi: 10.1016/j.bmcl.2012.02.079. Epub 2012 Mar 2.

Blocking HIV-1 entry by a gp120 surface binding inhibitor.

Author information

1
Department of Chemistry, Yale University, New Haven, CT 06520, United States.

Abstract

We report the mode of action of a proteomimetic compound that binds to the exterior surface of gp120 and blocks HIV-1 entry into cells. Using a one cycle time-of-addition study and antibody competition binding studies, we have determined that the compound blocks HIV-1 entry through modulation of key protein-protein interactions mediated by gp120. The compound exhibits anti-HIV-1 replication activities against several pseudotype viruses derived from primary isolates and the resistant strains isolated from existing drug candidates with equal potency. Together, these data provide evidence that the proteomimetic compound represents a novel class of HIV-1 viral entry inhibitor that functions through protein surface recognition in analogy to an antibody.

PMID:
22487177
PMCID:
PMC3640310
DOI:
10.1016/j.bmcl.2012.02.079
[Indexed for MEDLINE]
Free PMC Article

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