Determinants of activity of the HIV-1 maturation inhibitor PA-457

F Li, D Zoumplis, C Matallana, N.R. Kilgore, M Reddick, A.S. Yunus, Catherine Sarah Adamson, K Salzwedel, D.E. Martin, G.P. Allaway, E.O. Freed, C.T. Wild

Research output: Contribution to journalArticlepeer-review

59 Citations (Scopus)


3-O-(3′,3′-dimethylsuccinyl) betulinic acid, also termed PA-457 or DSB, is a novel HIV-1 inhibitor that blocks virus maturation by disrupting cleavage of the capsid precursor, CA-SP1. To better define the molecular target for PA-457, we prepared a panel of mutant viruses with point deletions spanning the CA-SP1 cleavage domain and characterized each of these viruses for PA-457 sensitivity. Our results indicate that amino acid residues in the N-terminal half of SP1 serve as determinants of PA-457 activity, while residues in the C-terminal half of SP1 were not involved in compound activity. These findings support and extend previous observations that PA-457 is a specific inhibitor of CA-SP1 cleavage and identify the CA-SP1 domain as the primary viral determinant for this novel inhibitor of HIV-1 replication.
Original languageEnglish
Pages (from-to)217-224
Issue number1-2
Publication statusPublished - Dec 2006


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