Discovery and Preclinical Evaluation of BMS-986242, a Potent, Selective Inhibitor of Indoleamine-2,3-dioxygenase 1.
Journal
ACS medicinal chemistry letters
ISSN: 1948-5875
Titre abrégé: ACS Med Chem Lett
Pays: United States
ID NLM: 101521073
Informations de publication
Date de publication:
11 Feb 2021
11 Feb 2021
Historique:
received:
20
12
2020
accepted:
22
01
2021
entrez:
19
2
2021
pubmed:
20
2
2021
medline:
20
2
2021
Statut:
epublish
Résumé
Indoleamine 2,3-dioxygenase 1 (IDO1) is a heme-containing dioxygenase enzyme implicated in cancer immune response. This account details the discovery of BMS-986242, a novel IDO1 inhibitor designed for the treatment of a variety of cancers including metastatic melanoma and renal cell carcinoma. Given the substantial interest around this target for cancer immunotherapy, we sought to identify a structurally differentiated clinical candidate that performs comparably to linrodostat (BMS-986205) in terms of both
Identifiants
pubmed: 33603977
doi: 10.1021/acsmedchemlett.0c00668
pmc: PMC7883469
doi:
Types de publication
Journal Article
Langues
eng
Pagination
288-294Informations de copyright
© 2021 American Chemical Society.
Déclaration de conflit d'intérêts
The authors declare no competing financial interest.
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