Journal
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Volume 227, Issue -, Pages -Publisher
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2021.113967
Keywords
Indoleamine 23-dioxygenase 1; IDO1 inhibitor; IDO1 degrader; Cancer therapy
Categories
Funding
- National Natural Science Foundation of China [82020108030, 81773562, 81973177, 82103997]
- Program for Science & Technology Innovation Talents in Universities of Henan Province [21HASTIT045]
- Science and Technology Project of Henan Province [202102310145]
- Henan Scientific Innovation Talent Team, Department of Education [19IRTSTHN001]
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Indoleamine 2,3-dioxygenase 1 (IDO1) is an important immunosuppressive enzyme in cancer therapy. Multiple IDO1 inhibitors have entered clinical trials, and PROTAC-based degraders also show promise for cancer treatment.
Indoleamine 2,3-dioxygenase 1 (IDO1), a known immunosuppressive enzyme that catalyzes the rate-limiting step in the oxidation of tryptophan (Trp) to kynurenine (Kyn), has received increasing atten-tion as an attractive immunotherapeutic target for cancer therapy. Up to now, eleven small-molecule IDO1 inhibitors have entered clinical trials for the treatment of cancers. In addition, proteolysis target-ing chimera (PROTAC) based degraders also provide prospects for cancer therapy. Herein we present a comprehensive overview of the medicinal chemistry strategies and potential therapeutic applications of IDO1 inhibitors in nonclinical trials and IDO1-PROTAC degraders. (c) 2021 Elsevier Masson SAS. All rights reserved.
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