Chemical Probes for Profiling of MALT1 Protease Activity

Author:

Verhelst Steven H. L.12,Prothiwa Michaela3ORCID

Affiliation:

1. Department of Cellular and Molecular Medicine KU Leuven – University of Leuven Herestraat 49, box 901b 3000 Leuven Belgium

2. Leibniz Institut für Analytische Wissenschaften – ISAS – e.V. Otto-Hahn Strasse 6b 44227 Dortmund Germany

3. Department of Pharmaceutical Sciences University of Antwerp Universiteitsplein 1 2610 Antwerp Belgium

Abstract

AbstractThe paracaspase MALT1 is a key regulator of the human immune response. It is implicated in a variety of human diseases. For example, deregulated protease activity drives the survival of malignant lymphomas and is involved in the pathophysiology of autoimmune/inflammatory diseases. Thus, MALT1 has attracted attention as promising drug target. Although many MALT1 inhibitors have been identified, molecular tools to study MALT1 activity, target engagement and inhibition in complex biological samples, such as living cells and patient material, are still scarce. Such tools are valuable to validate MALT1 as a drug target in vivo and to assess yet unknown biological roles of MALT1. In this review, we discuss the recent literature on the development and biological application of molecular tools to study MALT1 activity and inhibition.

Publisher

Wiley

Subject

Organic Chemistry,Molecular Biology,Molecular Medicine,Biochemistry

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