학술논문
Characterization of Potent Paracaspase MALT1 Inhibitors for Hematological Malignancies
Document Type
Article
Author
Yin, Wu; Nie, Zhe; Dingley, Karen; Trzoss, Michael; Krilov, Goran; Marshall, Netonia; Feng, Shulu; Pelletier, Robert; Bell, Jeff; Devine, Paul; Skrdla, Peter; Shimanovich, Roman; Ye, Min; Calkins, David; Grimes, Mary; Tang, Wayne; Placzek, Andrew; Lawrenz, Morgan; McRobb, Fiona; Gerasyuto, Aleksey; Feher, Victoria; Mondal, Sayan; Jensen, Kristian; Wright, Hamish; Weiss, Daniel; Akinsanya, Karen
Source
Blood; November 2021, Vol. 138 Issue: 1, Number 1 Supplement 1 p1187-1187, 1p
Subject
Language
ISSN
00064971; 15280020
Abstract
Introduction:MALT1 (mucosa-associated lymphoid tissue lymphoma translocation protein 1) is a key mediator of the NF-κB signaling pathway, the main driver of a subset of B-cell lymphomas and functions by forming a complex with CARMA1 and BCL10 to mediate antigen receptor-induced lymphocyte activation. MALT1 is considered a potential therapeutic target for several subtypes of non-Hodgkin B-cell lymphomas and chronic lymphocytic leukemia (CLL). Previously, we described the discovery of novel and potent MALT1 inhibitors with anti-proliferative effects in non-Hodgkin B-cell lymphoma cells. Here, we highlight the strong anti-tumor activity of our MALT1 inhibitors across multiple tumor models and the combination potential with agents including standard-of-care.