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

Journal Article (Journal Article)

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.

Full Text

Duke Authors

Cited Authors

  • Tsou, LK; Chen, C-H; Dutschman, GE; Cheng, Y-C; Hamilton, AD

Published Date

  • May 1, 2012

Published In

Volume / Issue

  • 22 / 9

Start / End Page

  • 3358 - 3361

PubMed ID

  • 22487177

Pubmed Central ID

  • PMC3640310

Electronic International Standard Serial Number (EISSN)

  • 1464-3405

Digital Object Identifier (DOI)

  • 10.1016/j.bmcl.2012.02.079


  • eng

Conference Location

  • England