Study of Gq mutations and their inhibitors in uveal melanoma / 药学学报
Acta Pharmaceutica Sinica
; (12): 1382-1392, 2020.
Article
Dans Zh
| WPRIM
| ID: wpr-823309
Responsable en Bibliothèque :
WPRO
ABSTRACT
Uveal melanoma (UM) is one of most common ocular cancers and is extremely malignant; so far there is no effective treatment. Moreover, the survival period is only 2-7 months after metastasis. It has been proven that more than 83% of uveal melanomas harbor mutations in G protein subunit α q (GNAQ) or G protein subunit α 11 (GNA11), among which 95% are a Q209P/L single-site mutation. Q209P/L mutations lead to dysfunction of guanine triphosphatase (GTPase) in the G protein and result in constitutive activation of downstream pathways including mitogen-activated protein kinase (MAPK), phosphoinositide 3-kinase (PI3K)/protein kinase B (AKT), Ras homologue (Rho)/ Rho-associated kinase (Rock)/Yes-associated protein (YAP) and others. Therefore, targeting GNAQ/GNA11 mutations are potential strategies for UM treatment. This review will focus on roles of G protein mutations in UM progression, and the potential therapeutic effects of GNAQ/GNA11 inhibitors, and will provide insights into basic and clinical research on UM treatment.
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Indice:
WPRIM
langue:
Zh
Texte intégral:
Acta Pharmaceutica Sinica
Année:
2020
Type:
Article