Inhibition of immunosuppressive indoleamine 2,3-dioxygenase by targeting the heme and apo-form.
Chem Commun (Camb)
; 57(3): 395-398, 2021 Jan 14.
Article
em En
| MEDLINE
| ID: mdl-33326535
ABSTRACT
Inhibition of immunomodulating enzyme indoleamine 2,3-dioxygenase 1 (IDO1) is considered one of the potential approaches in the fight against cancer and other diseases. Comprehensive biophysical and cellular studies have shown that quinine derivatives effectively inhibit the activity of IDO1. Mechanistic studies revealed that the potent quinine derivatives compete with heme for binding to apo-IDO1 and perturb its reversible binding propensity to apo-IDO1 via the formation of a heme-inhibitor complex. This IDO1 inhibitory pathway could provide new avenues to immunotherapy-based drug discovery strategies.
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Quinina
/
Inibidores Enzimáticos
/
Indolamina-Pirrol 2,3,-Dioxigenase
Limite:
Humans
Idioma:
En
Revista:
Chem Commun (Camb)
Assunto da revista:
QUIMICA
Ano de publicação:
2021
Tipo de documento:
Article
País de afiliação:
Índia