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新型VISTA小分子抑制剂的设计,合成和抗瘤活动评估

Chengliang Sun^1,2,3, Yuling He^1,4, Gefei Wang^1,2,3

¹State Key Laboratory of Natural Medicines and Jiangsu Key Laboratory of Drug Design and Optimization, China Pharmaceutical University, Nanjing 210009, China.

Journal of medicinal chemistry

|February 27, 2024

概括

研究人员开发了针对VISTA (T细胞激活的V域Ig抑制剂) 的新型小分子抑制剂,用于癌症免疫治疗. 化合物A4表现出强大的抗瘤活性和增强免疫细胞功能,显示出对VISTA向药物开发的希望.

科学领域:

免疫学免疫学免疫学
药理学药理学是指药理学的学科.
在瘤学瘤学.

背景情况:

维斯塔 (V-域Ig抑制T细胞激活) 是一个关键的免疫检查点蛋白.
维斯塔是开发新型癌症免疫疗法的有希望的目标.

研究的目的:

设计,合成和评估VISTA的基于甲基-皮里米丁的小分子抑制剂.
为了确定具有显著抗瘤活性的强效VISTA抑制剂.

主要方法:

分子对接和微量热泳 (MST) 试验被用于识别和表征VISTA抑制剂.
在体外研究中评估了对周围血液单核细胞 (PBMC) 和细胞因子释放的复合效应.
在体内研究评估了抗瘤活性和与PD-L1抗体的协同作用.

主要成果:

确定了一种化合物A1,进一步优化产生了具有高VISTA结合亲和力 (K_D = 0.49 ± 0.20μM) 的A4化合物.
化合物A4激活了PBMCs,增加了IFN-γ的释放,并增强了PBMC对瘤细胞的细胞毒性.
在体内,A4表现出强大的抗瘤作用和与PD-L1抗体的协同活性.

结论:

化合物A4是一种高效的VISTA小分子抑制剂.
这些发现为开发针对VISTA的癌症治疗提供了基础.

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