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Discovery of Low‐Molecular‐Weight Ligands for the AF6 PDZ Domain
Author(s) -
Joshi Mangesh,
Vargas Carolyn,
Boisguerin Prisca,
Diehl Annette,
Krause Gerd,
Schmieder Peter,
Moelling Karin,
Hagen Volker,
Schade Markus,
Oschkinat Hartmut
Publication year - 2006
Publication title -
angewandte chemie international edition
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 5.831
H-Index - 550
eISSN - 1521-3773
pISSN - 1433-7851
DOI - 10.1002/anie.200503965
Subject(s) - pdz domain , domain (mathematical analysis) , ligand (biochemistry) , block (permutation group theory) , chemistry , groove (engineering) , template , computer science , computational biology , nanotechnology , biology , materials science , biochemistry , mathematics , combinatorics , metallurgy , mathematical analysis , receptor
In the groove : The “drugability” of protein–protein interaction domains is still a matter of debate. The 3D structure of a complex of a small organic ligand and the AF6 PDZ domain revealed the creation of a binding pocket by the ligand (see picture). The derived compound is able to compete with a natural peptide ligand of the domain and represents a basic building block for the generation of selective PDZ inhibitors.