Pharmacologic Inhibition of MALT1 Protease by Phenothiazines as a Therapeutic Approach for the Treatment of Aggressive ABC-DLBCL

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Pharmacologic Inhibition of MALT1 Protease by Phenothiazines as a Therapeutic Approach for the Treatment of Aggressive ABC-DLBCL

机译：吩噻嗪类药物对MALT1蛋白酶的药理抑制作用作为治疗侵袭性ABC-DLBCL的治疗方法

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Proteolytic activity of the mucosa-associated lymphoid tissue lymphoma translocation protein-1 (MALT1) paracaspase is required for survival of the activated B cell subtype of diffuse large B cell lymphoma (ABC-DLBCL). We have identified distinct derivatives of medicinal active phenothiazines, namely mepazine, thioridazine, and promazine, as small molecule inhibitors of the MALT1 protease. These phenothiazines selectively inhibit cleavage activity of recombinant and cellular MALT1 by a noncompetitive mechanism. Consequently, the compounds inhibit anti-apoptotic NF-κB signaling and elicit toxic effects selectively on MALT1-dependent ABC-DLBCL cells in vitro and in vivo. Our data provide a conceptual proof for a clinical application of distinct phenothiazines in the treatment of ABC-DLBCL.

机译：黏膜相关淋巴样组织淋巴瘤易位蛋白-1（MALT1）对半胱天冬酶的蛋白水解活性是弥漫性大B细胞淋巴瘤（ABC-DLBCL）激活的B细胞亚型生存所必需的。我们已经确定了药用活性吩噻嗪的独特衍生物，即甲哌嗪，硫代哒嗪和丙嗪，作为MALT1蛋白酶的小分子抑制剂。这些吩噻嗪通过非竞争性机制选择性抑制重组MALT1和细胞MALT1的裂解活性。因此，该化合物在体外和体内抑制抗凋亡的NF-κB信号传导，并选择性地对MALT1依赖性ABC-DLBCL细胞产生毒性作用。我们的数据为独特的吩噻嗪在ABC-DLBCL的治疗中的临床应用提供了概念证明。

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《Cancer Cell》 |2012年第6期|共13页
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中图分类肿瘤学;
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1. Pharmacologic Inhibition of MALT1 Protease by Phenothiazines as a Therapeutic Approach for the Treatment of Aggressive ABC-DLBCL [J] . Cancer Cell . 2012,第6期

机译：吩噻嗪类药物对MALT1蛋白酶的药理抑制作用作为治疗侵袭性ABC-DLBCL的治疗方法
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6. Glutaminolysis Mediated by MALT1 Protease Activity Facilitates PD-L1 Expression on ABC-DLBCL Cells and Contributes to Their Immune Evasion [O] . Xichun Xia, Wei Zhou, Chengbin Guo, 2018

机译：MALT1蛋白酶活性介导的谷氨酰胺分解促进PD-L1在ABC-DLBCL细胞上的表达并有助于其免疫逃逸。
7. Pharmacologic Inhibition of MALT1 Protease by Phenothiazines as a Therapeutic Approach for the Treatment of Aggressive ABC-DLBCL [O] . Nagel Daniel, Spranger Stefani, Vincendeau Michelle, 2012

机译：吩噻嗪类药物对MALT1蛋白酶的药理抑制作用作为治疗侵袭性ABC-DLBCL的治疗方法

Pharmacologic Inhibition of MALT1 Protease by Phenothiazines as a Therapeutic Approach for the Treatment of Aggressive ABC-DLBCL

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