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

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

  2. Author Address

    Panacos Pharmaceut, Gaithersburg, MD 20877 USA. NCI, HIV Drug Resistance Program, Frederick, MD 21702 USA.;Wild, CT, 19008 Oxcart Pl, Gaithersburg, MD 20886 USA.;cwild@aol.com
    1. Year: 2006
    2. Date: Dec
  2. Journal: Virology
    1. 356
    2. 1-2
    3. Pages: 217-224
  4. Type of Article: Article
  5. ISSN: 0042-6822
  1. Abstract:

    3-0-(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. (c) 2006 Elsevier Inc. All rights reserved.

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External Sources

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  2. DOI: 10.1016/j.virol.2006.07.023
  3. View record in Web of Science®
  4. WOS: 000242424800024

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