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Brvar, M. ; O'Neill, T.J. ; Plettenburg, O. ; Krappmann, D.

An updated patent review of MALT1 inhibitors (2021-present).

Expert Opin. Ther. Patents, DOI: 10.1080/13543776.2025.2484371 (2025)
DOI PMC
Open Access Green möglich sobald Postprint bei der ZB eingereicht worden ist.
INTRODUCTION: MALT1 paracaspase acts as molecular scaffold and a proteolytic enzyme in immune cells. MALT1 has emerged as a promising drug target for cancer therapy, and especially for targeting MALT1 in aggressive lymphomas. Drug discovery programs yielded potent and selective MALT1 protease inhibitors. First-in-class MALT1 inhibitors have been moved to early clinical trials to evaluate safety and efficacy. AREAS COVERED: This review will provide an update regarding the mode of action, the chemical space and therapeutic use of MALT1 inhibitors based on recent patents and the scientific literature (05/2021-12/2024). EXPERT OPINION: Allosteric inhibition is preferred mode of action to inhibit the MALT1 protease. Chemical advances largely focus on improving binding and inhibition in the allosteric site of MALT1. New composition of matter has been generated, but a clinical proof for the safety and efficacy of allosteric MALT1 inhibitors is still pending. We still lack potent and selective competitive or covalent MALT1 inhibitors, indicating the challenges with targeting the active site. Further, MALT1 protein degraders and MALT1 scaffolding inhibitors have been developed, which may have distinct inhibitory profiles compared to allosteric MALT1 protease inhibitors, but more potent and selective compounds are needed to judge the feasibility and usefulness of these approaches.
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Publikationstyp Artikel: Journalartikel
Dokumenttyp Review
Korrespondenzautor
Schlagwörter Allosteric Inhibition ; Autoimmunity ; Cancer ; Lymphoma ; Malt1 ; Paracaspase ; Protac ; Protease ; Regulatory T Cells; Paracaspase Malt1; Protease; Activation; Responses; Therapy; Btk
ISSN (print) / ISBN 1354-3776
e-ISSN 1744-7674
Zeitschrift Expert Opinion on Therapeutic Patents
Verlag Taylor & Francis
Verlagsort 2-4 Park Square, Milton Park, Abingdon Or14 4rn, Oxon, England
Nichtpatentliteratur Publikationen
Begutachtungsstatus Peer reviewed
Institut(e) Research Unit Signaling and Translation (SAT)
Institute of Medicinal Chemistry (IMC)
Förderungen Deutsche Krebshilfe e.V.