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- W3106847441 abstract "MALT1 plays a central role in immune cell activation by transducing NF-κB signaling, and its proteolytic activity represents a key node for therapeutic intervention. Two cycles of scaffold morphing of a high-throughput biochemical screening hit resulted in the discovery of MLT-231, which enabled the successful pharmacological validation of MALT1 allosteric inhibition in preclinical models of humoral immune responses and B-cell lymphomas. Herein, we report the structural activity relationships (SARs) and analysis of the physicochemical properties of a pyrazolopyrimidine-derived compound series. In human T-cells and B-cell lymphoma lines, MLT-231 potently and selectively inhibits the proteolytic activity of MALT1 in NF-κB-dependent assays. Both in vitro and in vivo profiling of MLT-231 support further optimization of this in vivo tool compound toward preclinical characterization." @default.
- W3106847441 created "2020-12-07" @default.
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- W3106847441 date "2020-11-30" @default.
- W3106847441 modified "2023-10-16" @default.
- W3106847441 title "Discovery of Potent, Highly Selective, and <i>In Vivo</i> Efficacious, Allosteric MALT1 Inhibitors by Iterative Scaffold Morphing" @default.
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- W3106847441 doi "https://doi.org/10.1021/acs.jmedchem.0c01245" @default.
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