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

Bioorganic & Medicinal Chemistry Letters
Anand MayasundariNaoaki Fujii

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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Citations

Jul 30, 2010·Organic & Biomolecular Chemistry·Anders BachKristian Strømgaard
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