Open AccessMEK-ing the Most of It: Strategies to Co-target Gαq and MAPK in Uveal Melanoma
Author(s) -
Sathya Neelature Sriramareddy,
Keiran S.M. Smalley
Publication year - 2021
Publication title -
clinical cancer research
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 5.427
H-Index - 324
eISSN - 1557-3265
pISSN - 1078-0432
DOI - 10.1158/1078-0432.ccr-20-4530
Subject(s) - melanoma , mapk/erk pathway , mek inhibitor , medicine , cancer research , kinase , biology , microbiology and biotechnology
Most uveal melanomas harbor mutations in Gαq and show constitutive MAPK activation. Although MEK inhibition has some efficacy against uveal melanoma, clinical responses are typically poor. The Gαq inhibitor-MEK inhibitor combination showed prolonged suppression of MAPK signaling in preclinical uveal melanoma models and led to improved therapeutic responses. See related article by Hitchman et al., p. 1476 .