SAR by Oxime‐Containing Peptide Libraries: Application to Tsg101 Ligand Optimization
Year: 2008
Type: article
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.
Source: ChemBioChem
Authors: Fa Liu, Andrew G. Stephen, Abdul A. Waheed, M. Javad Aman, Eric O. Freed, Robert J. Fisher, Terrence R. Burke
Language: English
Subfield: Molecular Biology
Domain: Life Sciences
Open Access status: green
OpenAlex ID: W2105570737