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高通量屏幕识别MAS9作为一种新型抑制剂的C型莱克受体-2 (CLEC-2) - 波多普拉宁相互作用

Marcin A Sowa^1,2,3, Yan Wu¹, Jan van Groningen⁴

¹Institute for Cardiovascular and Metabolic Research (ICMR), School of Biological Sciences, University of Reading, Reading, UK.

British journal of pharmacology

|April 24, 2025

概括

研究人员确定了MAS9,一种新的小分子抑制剂,其向C型学菌素类受体-2 (CLEC-2). 马斯9有效抑制CLEC-2介导的血小板激活,为血栓炎症和癌症提供潜在的治疗应用.

科学领域:

生物化学生物化学
药理学药理学是指药理学的学科.
免疫学免疫学免疫学

背景情况:

C型甲状腺样受体-2 (CLEC-2) 是一个血小板受体,对各种生理和病理过程至关重要.
与波多普拉宁的CLEC-2相互作用与淋巴血管生成,血管完整性,器官发育和瘤转移有关.
激活CLEC-2可启动涉及Syk酶的信号级联.

研究的目的:

确定和描述一种新的CLEC-2小分子抑制剂.
为了研究CLEC-2抑制剂的治疗潜力.

主要方法:

使用AlphaScreen测定来识别CLEC-2抑制剂的高通量查.
在模拟模型中预测结合部位相互作用.
功能性测试 (聚合计,扩散,酸化) 以评估抑制剂对血小板激活的疗效.

主要成果:

对18476个分子的查产生了14个候选分子,MAS9被选中进行进一步研究.
预计MAS9将与CLEC-2配方Podoplanin和Rhodocytin结合在相同的部位.
马斯9证明抑制了CLEC-2介导的血小板聚合,扩散,信号和纤维素因子结合.

结论:

马斯9有选择性地抑制CLEC-2,与GPVI抑制不同.
马斯9显示为治疗血栓炎症和癌症的治疗剂.
需要进一步的临床前研究来评估MAS9的治疗潜力.

关键词:

在AlphaScreen上使用.在 CLEC‐2 中,血小板血小板血小板是什么?波多普拉尼尼 (podoplanin) 是一种小分子分子小分子

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