Modulators of calpain activity: inhibitors and activators as potential drugs

Dókus, Endre Levente and Yousef, Mo'ath and Bánóczi, Zoltán (2020) Modulators of calpain activity: inhibitors and activators as potential drugs. Pharmaceutics, 15 (4). pp. 471-486. ISSN 1999-4923

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Abstract

Introduction Calpains are intracellular Ca2+-dependent cysteine proteases with 15 known members in the enzyme family. They act as regulatory enzymes, their cleavage modifies the function of their substrates. As their substrates have important roles in many physiological processes, adequate function of calpains is mandatory for normal cellular functions. Adverse operation of them is often related with diseases (e.g. neurodegenerative disorders, cancer, type 2 diabetes mellitus or limb-girdle muscular dystrophy type 2A). Areas covered Herein, the authors give an overview about calpains, their structure, physiological and pathological functions. The challenges in the drug discovery of calpain inhibitors and activators are enlightened by summarising examples that eventuated good candidates. Going through these examples new and applicable strategies are discussed. Expert opinion Calpain enzymes are attractive targets to design inhibitors or activators for drug development. This research area has high potential, although it has many challenges. The selective and targeted inhibition or activation of calpains is needed. Thus the studies focused on the improvement of these properties of drug candidates.

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