MEK-ing the Most of It: Strategies to Co-target Gαq and MAPK in Uveal Melanoma

Most uveal melanomas harbor mutations in G alpha q and show constitutive MAPK activation. Although MEK inhibition has some efficacy against uveal melanoma, clinical responses are typically poor. The G alpha q inhibitor-MEK inhibitor combination showed prolonged suppression of MAPK signaling in preclinical uveal melanoma models and led to improved therapeutic responses.

Automated summary

Most uveal melanomas have mutations in G alpha q and show constitutive MAPK activation. While MEK inhibition has limited efficacy, combining G alpha q inhibitor with MEK inhibitor can lead to prolonged suppression of MAPK signaling and improved therapeutic responses in preclinical uveal melanoma models.