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通过基于SPR的高通量选发现小分子CHI3L1抑制剂

Longfei Zhang, Hossam Hammouda Nada Hammouda, Moustafa T Gabr

bioRxiv : the preprint server for biology

|September 5, 2025

概括

研究人员发现了向与癌症相关的小分子抑制剂CHI3L1. 这些抑制剂在干扰质母细胞瘤模型中的癌症生长和免疫逃避机制方面具有前景.

科学领域:

生物化学
癌症学
药物发现

背景情况:

基因酶3样1 (CHI3L1) 是一种关键蛋白质,参与癌症的发展和免疫逃避.
在癌症患者中CHI3L1水平升高是常见的,使其成为重要的治疗点.

研究的目的:

为CHI3L1开发新的小分子抑制剂.
建立和验证用于识别CHI3L1结合物的高通量选平台.

主要方法:

表面等离子共振 (SPR) 用于小分子的高通量选.
通过AlphaLISA测试来评估CHI3L1- 黄素-3的相互作用中断.
分析化合物结合的分子对接和动力学模拟.
用于功能评估的三维质母细胞球体模型.

主要成果:

确定并验证了两个CHI3L1结合剂,化合物1-4和1-7,其解离常数 (Kd) 处于低微分子范围.
证明 1- 7 化合物有效降低质母细胞球体活力并抑制STAT3酸化.
证实了已识别的化合物中断了CHI3L1- 黄素-3的相互作用.

结论:

SPR是选CHI3L1抑制剂的可靠平台.
在相关的质母细胞瘤模型中,1- 7 化合物表现出强烈的抗癌活性.
已识别的小分子为开发CHI3L1向癌症治疗提供了有希望的线索.

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