The ups, downs and new trends of IDO1 inhibitors

doi:10.1016/j.bioorg.2021.104815

	The ups, downs and new trends of IDO1 inhibitors
	Chen, Shulun 1,2,3; Tan, Jing 1,2,3; Zhang, Ao 1,2,3,4
刊名	BIOORGANIC CHEMISTRY
	2021-05-01
卷号	110 页码:12
关键词	Immunotherapy Cancer Indoleamine 2,3-dioxygenase Tryptophan 2,3-dioxygenase Inhibitors Checkpoint Inhibitor
ISSN号	0045-2068
DOI	10.1016/j.bioorg.2021.104815
通讯作者	Zhang, Ao(ao6919zhang@sjtu.edu.cn)
英文摘要	Cancer immunotherapy has become an emerging driving force in the development of innovative strategies to fight against cancer. Despite the significant clinical benefits that many cancer patients have gained, the generally average response rate of similar to 20% is far behind the expectation for immune checkpoint inhibitors (ICIs). Combination of ICIs with indoleamine 2,3-dioxygenase-1 (IDO1) inhibitors is considered as an alternative solution and has proved effective in tremendous preclinical studies. However, the failure of phase III ECHO-301/KEYNOTE-252 trial seriously dampened the enthusiasm on the rationality of IDO1-targeting strategy. Fortunately, in spite of the ups and downs in the developmental journey of IDO1 inhibitors, multiple new approaches have been proposed to bridge the gap between lab to the clinic. Here, we review the recent advances in the development of small molecule inhibitors targeting IDO1 especially the new trend of IDO1 inhibitors after ECHO-301 clinical trials, including dual or pan-inhibitors targeting IDO1 and TDO or IDO2, apo-IDO1 inhibitors, IDO1 PROTACs, as well as other IDO1 inhibitors.
资助项目	Shanghai Jiao Tong University[AF1700037] ; Shanghai Jiao Tong University[WF220217002] ; Shanghai Jiao Tong University[WH10117001]
WOS关键词	2,3-DIOXYGENASE 1 INHIBITORS ; INDUCED PROTEIN-DEGRADATION ; HUMAN INDOLEAMINE 2,3-DIOXYGENASE ; DRUG DISCOVERY ; CANCER-IMMUNOTHERAPY ; GCN2 KINASE ; STAGE-III ; IN-VITRO ; INDOLEAMINE-2,3-DIOXYGENASE ; DERIVATIVES
WOS研究方向	Biochemistry & Molecular Biology ; Chemistry
语种	英语
出版者	ACADEMIC PRESS INC ELSEVIER SCIENCE
WOS记录号	WOS:000647574400002
内容类型	期刊论文
源URL	[http://119.78.100.183/handle/2S10ELR8/297326]
专题	中国科学院上海药物研究所
通讯作者	Zhang, Ao
作者单位	1.Shanghai Jiao Tong Univ, Sch Pharm, Pharm Ctr 10, Shanghai 200240, Peoples R China 2.Chinese Acad Sci, Shanghai Inst Mat Med SIMM, CAS Key Lab Receptor Res, Shanghai 201203, Peoples R China 3.Univ Chinese Acad Sci, Beijing 100049, Peoples R China 4.Shanghai Jiao Tong Univ, Sch Pharm, Shanghai Key Lab Mol Engn Chiral Drugs, Shanghai 200240, Peoples R China
推荐引用方式 GB/T 7714	Chen, Shulun,Tan, Jing,Zhang, Ao. The ups, downs and new trends of IDO1 inhibitors[J]. BIOORGANIC CHEMISTRY,2021,110:12.
APA	Chen, Shulun,Tan, Jing,&Zhang, Ao.(2021).The ups, downs and new trends of IDO1 inhibitors.BIOORGANIC CHEMISTRY,110,12.
MLA	Chen, Shulun,et al."The ups, downs and new trends of IDO1 inhibitors".BIOORGANIC CHEMISTRY 110(2021):12.