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

Overview

Journal Bioorg Med Chem Lett

Specialty Biochemistry

Date 2008 Jan 9

PMID 18180157

Citations 17

Authors

Anand Mayasundari

Antonio M Ferreira

Liwen He

Neeraj Mahindroo

Don Bashford

Naoaki Fujii

Affiliations

Soon will be listed here.

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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