The research progress of indoleamine 2,3-dioxygenase 1 (IDO1) inhibitors
10.16438/j.0513-4870.2018-0673
- VernacularTitle:吲哚胺2,3-双加氧酶IDO1抑制剂的研究进展
- Author:
Xin-yuan ZHANG
1
;
Guo-nan CUI
1
;
Bai-ling XU
1
Author Information
1. Beijing Key Laboratory of Active Substance Discovery and Druggability Evaluation, Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China
- Publication Type:REVIEWS
- Keywords:
indoleamine 2,3-dioxygenase 1;
IDO1 inhibitors;
structure-activity relationship;
binding mode;
tumor immunotherapy
- From:
Acta Pharmaceutica Sinica
2018;53(11):1784-1796
- CountryChina
- Language:Chinese
-
Abstract:
Indoleamine 2,3-dioxygenase 1 (IDO1) is a key enzyme of L-tryptophan metabolic oxidation pathway, in which the L-tryptophan is transformed into N-formyl kynurenine by oxidative cleavage. IDO1 is considered as a potential target for the development of cancer immunotherapeutic molecules. Up to now, at least 10 drug candidates have been advanced into clinical research. In this review, the binding mode and structure-activity relationships of the representative IDO1 small molecule inhibitors were summarized according the characteristics of chemical structures. Hopefully, this review could provide some insights for further development of novel IDO1 inhibitors.