CQ80(CQ80) - 药物靶点：PEPD x XPNPEP1_专利_临床

概要

基本信息

药物类型

小分子化药

别名-

靶点

PEPD x XPNPEP1

作用机制

PEPD抑制剂(peptidase D inhibitors)、XPNPEP1抑制剂(X-prolyl aminopeptidase 1 inhibitors)

治疗领域-

在研适应症-

非在研适应症-

原研机构

Memorial Sloan Kettering Cancer Center

在研机构

Memorial Sloan Kettering Cancer Center

非在研机构-

最高研发阶段药物发现

首次获批日期-

最高研发阶段(中国)-

特殊审评-

关联

100 项与 CQ80 相关的临床结果

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100 项与 CQ80 相关的转化医学

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100 项与 CQ80 相关的专利（医药）

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1

项与 CQ80 相关的文献（医药）

2023-02-23·Journal of Medicinal Chemistry1区 · 医学

Optimized M24B Aminopeptidase Inhibitors for CARD8 Inflammasome Activation

1区 · 医学

Article

作者: Orth-He, Elizabeth L. ; Chen, Qifeng ; Bachovchin, Daniel A. ; Ball, Daniel P. ; Wang, Alvin ; Covelli, Dominic J. ; Bhattacharjee, Abir ; Rao, Sahana D. ; Huang, Hsin-Che ; Wang, Qinghui ; Hsiao, Jeffrey C.

Inflammasomes are innate immune signaling platforms that trigger pyroptotic cell death. NLRP1 and CARD8 are related human inflammasomes that detect similar danger signals, but NLRP1 has a higher activation threshold and triggers a more inflammatory form of pyroptosis. Both sense the accumulation of intracellular peptides with Xaa-Pro N-termini, but Xaa-Pro peptides on their own without a second danger signal only activate the CARD8 inflammasome. We recently reported that a dual inhibitor of the Xaa-Pro-cleaving M24B aminopeptidases PEPD and XPNPEP1 called CQ31 selectively activates the CARD8 inflammasome by inducing the build-up of Xaa-Pro peptides. Here, we performed structure-activity relationship studies on CQ31 to develop the optimized dual PEPD/XPNPEP1 inhibitor CQ80 that more effectively induces CARD8 inflammasome activation. We anticipate that CQ80 will become a valuable tool to study the basic biology and therapeutic potential of selective CARD8 inflammasome activation.

100 项与 CQ80 相关的药物交易

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