《生命科学》 2023, 35(7): 956-965

二氢乳清酸脱氢酶抑制剂适应症及其抗肿瘤临床研究进展

皇泽慧^1,2 , 姜凯龙^2,* , 李　佳^1,2,*

¹遵义医科大学，遵义 563099 ²中科中山药物创新研究院，中山 528400

摘　要：

二氢乳清酸脱氢酶(dihydroorotate dehydrogenase, DHODH) 催化二氢乳清酸转化为乳清酸，是嘧啶核苷酸从头合成途径的限速酶。DHODH 与自身免疫疾病、病毒感染、肿瘤等多种疾病的发生发展密切相关，已有DHODH 抑制剂被批准用于治疗自身免疫疾病，而肿瘤是继自身免疫疾病后又一具有上市潜力的适应症。本文就DHODH 抑制剂的适应症及其抗肿瘤临床研究进展进行综述。

通讯作者：姜凯龙 , Email:jiangkailong@zidd.ac.cn 李　佳 , Email: jli@simm.ac.cn

The indications and the clinical antitumor progress of dihydroorotate dehydrogenase inhibitors

HUANG Ze-Hui^1,2 , JIANG Kai-Long^2,* , LI Jia^1,2,*

¹Zunyi Medical University, Zunyi 563099, China ²Zhongshan Institute for Drug Discovery, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Zhongshan 528400, China

Abstract:

Dihydroorotate dehydrogenase (DHODH) catalyzes the conversion of dihydroorotate into orotate, which is the rate-limiting enzyme of de novo pyrimidine nucleotide biosynthetic pathway. DHODH is closely related to the occurrence and development of various diseases, including autoimmune diseases, viral infections, tumors and so on. DHODH inhibitors have been approved for the treatment of autoimmune diseases, and tumor is another indication with market potential. This article reviews the indications and the clinical antitumor progress of DHODH inhibitors.

Communication Author：JIANG Kai-Long , Email:jiangkailong@zidd.ac.cn LI Jia , Email: jli@simm.ac.cn