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SAR by oxime-containing peptide libraries: Application to Tsg101 ligand optimization

  1. Author:
    Liu, F.
    Stephen, A. G.
    Waheed, A. A.
    Aman, M. J.
    Freed, E. O.
    Fisher, R. J.
    Burke, T. R.

  2. Author Address

    Liu, Fa, Burke, Terrence R., Jr.] NCI, Med Chem Lab, CCR, Frederick, MD 21702 USA. [Stephen, Andrew G.; Fisher, Robert J.] SAIC, Adv Technol Program, Prot Chem Lab, Frederick, MD 21702 USA. [Waheed, Abdul A.; Freed, Eric O.] NCI, HIV Drug Resistance Program, CCR, Frederick, MD 21702 USA. [Aman, M. Javad] USA, Med Res Inst Infect Dis, Frederick, MD 21702 USA.
    1. Year: 2008
  2. Journal: Chembiochem
    1. 9
    2. 12
    3. Pages: 2000-2004
  4. Type of Article: Article
  1. Abstract:

    HIV-1 viral assembly requires a direct interaction between a Pro-Thr-Ala-Pro ("PTAP") motif in the viral protein Gag-p6 and the cellular endosomal sorting factor Tsg101. In an effort to develop competitive inhibitors of this interaction, an SAR study was conducted based on the application of post solid-phase oxime formation involving the sequential insertion of aminooxy-containing residues within a nonamer parent, peptide followed by reaction with libraries of aldehydes. Approximately 15-20-fold enhancement in binding affinity was achieved by this approach.

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External Sources

  1. PMID: 18655064

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