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Breaking the Dogma of the Metal-Coordinating Carboxylate Group in Integrin Ligands: Introducing Hydroxamic Acids to the MIDAS To Tune Potency and Selectivity

✍ Scribed by Dominik Heckmann; Burkhardt Laufer; Luciana Marinelli; Vittorio Limongelli; Ettore Novellino; Grit Zahn; Roland Stragies; Horst Kessler

Publisher: John Wiley and Sons
Year: 2009
Tongue: English
Weight: 638 KB
Volume: 48
Category: Article
ISSN: 0044-8249
DOI: 10.1002/anie.200900206

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✦ Synopsis

Abstract

A suitable substitute: All integrin receptors bind their ligands, which contain an aspartate residue, in the metal‐ion‐ dependent adhesion site (MIDAS). So far all attempts to replace the carboxyl group of aspartate with other, pharmacologically favorable isosteric groups have failed. Now it has been shown that a hydroxamic acid group can replace the carboxyl group; the resulting ligand retains its high binding activity. The picture shows one such ligand in the binding site of αvβ3.magnified image

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Cover Picture: Breaking the Dogma of the

Cover Picture: Breaking the Dogma of the Metal-Coordinating Carboxylate Group in Integrin Ligands: Introducing Hydroxamic Acids to the MIDAS To Tune Potency and Selectivity (Angew. Chem. Int. Ed. 24/2009)

✍ Dominik Heckmann; Burkhardt Laufer; Luciana Marinelli; Vittorio Limongelli; Etto 📂 Article 📅 2009 🏛 John Wiley and Sons 🌐 English ⚖ 994 KB