Rational design of the first small-molecule antagonists of NHERF1/EBP50 PDZ domains

  • Bioorg Med Chem Lett. 2008 Feb 1;18(3):942-5. doi: 10.1016/j.bmcl.2007.12.038.
Anand Mayasundari  1 ,  Antonio M Ferreira ,  Liwen He ,  Neeraj Mahindroo ,  Don Bashford ,  Naoaki Fujii
Affiliations
  • 1. Department of Chemical Biology and Therapeutics, St. Jude Children's Research Hospital, Memphis, TN 38105, USA.
PMID: 18180157 DOI: 10.1016/j.bmcl.2007.12.038
Abstract

This report describes the first small-molecule antagonists that specifically target the ligand-binding pocket of PDZ domains of NHERF1 multi-functional adaptor protein. Comparison of the peptide sequence homology between the native ligand of NHERF1 PDZ domains and an indole-based non-peptide chemical scaffold allowed the design of a small-molecule antagonist of NHERF1 PDZ domains.

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