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Published on: July 25, 2013
Rational design of the first small-molecule antagonists of NHERF1/EBP50 PDZ domains
Anand Mayasundari1, Antonio M Ferreira, Liwen He
1Department of Chemical Biology and Therapeutics, St. Jude Children's Research Hospital, Memphis, TN 38105, USA.
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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