Discovery of Low‐Molecular‐Weight Ligands for the AF6 PDZ Domain

Abstract

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. Supporting information for this article is available on the WWW under http://www.wiley-vch.de/contents/jc_2002/2006/z503965_s.pdf or from the author. Please note: The publisher is not responsible for the content or functionality of any supporting information supplied by the authors. Any queries (other than missing content) should be directed to the corresponding author for the article.