Title of article
Rational design of a nonpeptide general chemical scaffold for reversible inhibition of PDZ domain interactions
Author/Authors
Naoaki Fujii، نويسنده , , Jose J. Haresco، نويسنده , , Kathleen A.P. Novak، نويسنده , , Robert M. Gage، نويسنده , , Nicoletta Pedemonte، نويسنده , , David Stokoe، نويسنده , , Irwin D. Kuntz، نويسنده , , R. Kiplin Guy، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2007
Pages
4
From page
549
To page
552
Abstract
Novel small molecules were designed to specifically target the ligand-binding pocket of a PDZ domain. Iterative molecular docking and modeling allowed the design of an indole scaffold 10a as a reversible inhibitor of ligand binding. The 10a scaffold inhibited the interaction between MAGI-3 and PTEN and showed cellular activities that are consistent with the inhibition of NHERF-1 function.
Keywords
PDZ domain , NHERF , Protein–protein , interaction , Drug design
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2007
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
797694
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