Generic placeholder image

Letters in Drug Design & Discovery

Editor-in-Chief

ISSN (Print): 1570-1808
ISSN (Online): 1875-628X

Synthesis and Evaluation of Calpain Inhibitors Carrying Muscle Cell Targeting Groups

Author(s): P. Weyermann, H. Herzner, C. Lescop, H. Siendt, R. Bolliger, M. Hennebohle, C. Rummey, A. Briguet, I. Courdier-Fruh, M. Erb, M. Foster, J.P. Magyar, A. von Sprecher and T. Meier

Volume 3, Issue 3, 2006

Page: [152 - 158] Pages: 7

DOI: 10.2174/157018006776286916

Price: $65

Abstract

Inhibition of the cysteine protease calpain is a promising strategy for the treatment of muscular dystrophies including Duchenne Muscular Dystrophy. For the treatment to be effective, uptake of the inhibitors into the muscle cells is a prerequisite. A series of α-ketoamide calpain inhibitors carrying various muscle cell targeting capping groups was synthesized. Compounds with charged or highly polar targeting groups were not able to cross the cellular membrane. Introduction of lipoic acid as end cap yielded cell permeable calpain inhibitors with nanomolar potency.

Keywords: Calpain inhibitor, ketoamide, duchenne muscular dystrophy, lipoic acid


Rights & Permissions Print Cite
© 2024 Bentham Science Publishers | Privacy Policy