Effects of Oncogenic Gα_q and Gα₁₁ Inhibition by FR900359 in Uveal Melanoma.

ABSTRACT: Uveal melanoma is the most common intraocular tumor in adults and often metastasizes to the liver, leaving patients with few options. Recurrent activating mutations in the G proteins, Gα_q and Gα₁₁, are observed in approximately 93% of all uveal melanomas. Although therapeutic intervention of downstream Gα_q/11 targets has been unsuccessful in treating uveal melanoma, we have found that the Gα_q/11 inhibitor, FR900359 (FR), effectively inhibits oncogenic Gα_q/11 signaling in uveal melanoma cells expressing either mutant Gα_q or Gα₁₁. Inhibition of oncogenic Gα_q/11 by FR results in cell-cycle arrest and induction of apoptosis. Furthermore, colony formation is prevented by FR treatment of uveal melanoma cells

SUBMITTER: Lapadula D 

PROVIDER: S-EPMC6445713 | biostudies-literature | 2019 Apr

REPOSITORIES: biostudies-literature