基于靶标IDO1、TDO的抑制剂研究进展

Advances in research on inhibitors based on targets:IDO1 and TDO

吲哚胺2,3-双加氧酶1 (IDO1)和色氨酸2,3-双加氧酶(TDO)催化色氨酸代谢的第一步也是限速步骤,与肿瘤免疫耐受和患者的不良预后相关,已经成为肿瘤免疫治疗的重要靶标。到目前为止,有9个IDO1抑制剂、3个IDO1/TDO双靶点抑制剂进入临床试验。本篇综述从药物化学角度总结了IDO1抑制剂、TDO抑制剂、IDO1/TDO双重抑制剂的研究进展。

Indoleamine 2,3-dioxygenase 1(IDO1)and tryptophan 2,3-dioxygenase(TDO)catalyze the initial and rate limiting step in the catabolism of tryptophan,which is related to tumor immune tolerance and poor prognosis in patients.In this regard,two enzymes have become important therapeutic targets for tumor immunotherapy.So far,nine IDO1 inhibitors and three IDO1/TDO dual inhibitors have entered clinical trials.This review summarizes the research progress of IDO1 inhibitors,TDO inhibitors and IDO1/TDO dual inhibitors from the perspective of medicinal chemistry.