发现天然产物鞣花酸是一种有效的 CD73 和 CD39 双重抑制剂。
Discovery of natural product ellagic acid as a potent CD73 and CD39 dual inhibitor.
机构信息
School of Pharmacy, Ningxia Medical University, 1160 Shengli Street, Yinchuan, Ningxia 750004, People's Republic of China.
School of Chemical and Environmental Engineering, Shanghai Institute of Technology, 100 Haiquan Road, Shanghai 201418, People's Republic of China.
出版信息
Bioorg Med Chem Lett. 2021 Feb 15;34:127758. doi: 10.1016/j.bmcl.2020.127758. Epub 2020 Dec 24.
The ATP-adenosine pathway has been recently identified as an attractive immune-oncology target and several drug candidates have been entered clinic trials. Inspired by the report of the first small-molecule CD73inhibitor AB680, we describe the discovery of natural product ellagic acid as a dual CD73 and CD39 inhibitor with an IC value of 1.85 ± 0.21 μM and 0.50 ± 0.22 μM, respectively. The result of cytotoxicity assays indicated that ellagic acid is a valuable lead compound with low cytotoxicity effect for immune therapy.
三磷酸腺苷-腺苷途径最近被确定为一种有吸引力的免疫肿瘤学靶点，已有几种候选药物进入临床试验。受首个小分子 CD73 抑制剂 AB680 报告的启发，我们描述了天然产物鞣花酸作为一种双重 CD73 和 CD39 抑制剂的发现，其 IC 值分别为 1.85±0.21μM 和 0.50±0.22μM。细胞毒性测定结果表明，鞣花酸是一种具有低细胞毒性的免疫治疗有价值的先导化合物。
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