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| | SAR analysis of compounds that inhibit Human Immunodeficiency Virus Fusion. |
| Description: | Data Source: Burnham Center for Chemical Genomics (BCCG) Source Affiliation: Sanford-Burnham Medical Research Institute (SBMRI, San Diego, CA) Network: NIH Molecular Libraries Production Centers Network (MLPCN) Grant Number: 1R21NS059403-01 Assay Provider: Dr. Miriam Gochin, Touro University-California, Vallejo, CA The fusion-active conformation of the envelope protein gp41 of HIV-1 consists of an N-terminal trimeric a-helical coiled coil domain, and three anti-parallel C-terminal helices which fold down the grooves of the coiled coil to form a six-helix bundle. Disruption of the six-helix bundle is considered to be a key component of an effective non-peptide fusion inhibitor. This structure forms as a result of a conformational change in gp41, triggered by gp120 and co-receptor binding to host cell receptors. Prevention of six-helix bundle formation has been recognized as an important mechanism for viral fusion inhibition A metallopeptide-based fluorescence assay has been develope |
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