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Rational Design of the First Small-molecule Antagonists of NHERF1/EBP50 PDZ Domains

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Specialty Biochemistry
Date 2008 Jan 9
PMID 18180157
Citations 17
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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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