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新型三唑取代的咪唑并[1,2 - ]嘧啶化合物作为环鸟苷酸合成酶(cGAS)抑制剂

Novel Triazole-Substituted Imidazo[1,2-]Pyrimidine Compounds as cGAS inhibitors.

作者信息

Zhao Taoqian, Liang Steven H

机构信息

Department of Radiology and Imaging Sciences, Emory University, 1364 Clifton Road, Atlanta, Georgia 30322, United States.

出版信息

ACS Med Chem Lett. 2025 Mar 27;16(4):530-531. doi: 10.1021/acsmedchemlett.5c00136. eCollection 2025 Apr 10.

Abstract

This patent application presents the discovery and characterization of a novel series of triazole-substituted imidazo[1,2-]pyrimidine compounds as selective cGAS inhibitors. These compounds effectively suppress cGAS enzymatic activity and modulate downstream STING signaling, demonstrating potential for treating autoimmune and inflammatory diseases driven by aberrant cytosolic DNA sensing.

摘要

本专利申请介绍了一系列新型三唑取代咪唑并[1,2 - ]嘧啶化合物作为选择性cGAS抑制剂的发现和特性。这些化合物有效地抑制cGAS酶活性并调节下游STING信号传导,显示出治疗由异常胞质DNA感应驱动的自身免疫性疾病和炎症性疾病的潜力。

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本文引用的文献

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Manipulating the cGAS-STING Axis: advancing innovative strategies for osteosarcoma therapeutics.
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cGAS-STING targeting offers novel therapeutic opportunities in neurological diseases.
Ageing Res Rev. 2025 Mar;105:102691. doi: 10.1016/j.arr.2025.102691. Epub 2025 Feb 13.
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cGAS/STING signaling pathway in gynecological malignancies: From molecular mechanisms to therapeutic values.
Front Immunol. 2025 Jan 30;16:1525736. doi: 10.3389/fimmu.2025.1525736. eCollection 2025.
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Identification and development of cGAS inhibitors and their uses to treat Alzheimer's disease.
Neurotherapeutics. 2025 Apr;22(3):e00536. doi: 10.1016/j.neurot.2025.e00536. Epub 2025 Jan 31.

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