G protein-coupled receptors (GPCRs) are the largest class of drug targets, largely owing to
their druggability, diversity and physiological efficacy. Many drugs selectively target specific …

Heterotrimeric G proteins are the core upstream elements that transduce and amplify the
cellular signals from G protein–coupled receptors (GPCRs) to intracellular effectors. GPCRs …

The stabilization of different active conformations of G protein–coupled receptors is thought
to underlie the varying efficacies of biased and balanced agonists. Here, profiling the …

Somatic gain-of-function mutations of GNAQ and GNA11, which encode α subunits of
heterotrimeric Gαq/11 proteins, occur in about 85% of cases of uveal melanoma (UM), the …

Inhibitors of heterotrimeric G proteins are being developed as therapeutic agents.
Epitomizing this approach are YM-254890 (YM) and FR900359 (FR), which are efficacious …

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 …

Macrocyclic natural products have been recognized and utilized as new platforms for
designing drugs in pharmaceutical research because the constrained three-dimensional …

The Cancer Genome Atlas (TCGA) uveal melanoma project was a comprehensive multi-
platform deep molecular investigation of 80 uveal melanoma primary tissue samples …

The recent discovery of MRGPRX2 explains mast cell (MC)-dependent symptoms
independently of FcεRI-activation. Because of its novelty, signaling cascades triggered by …

Purpose: All uveal melanoma and a fraction of other melanoma subtypes are driven by
activation of the G-protein alpha-q (Gαq) pathway. Targeting these melanomas has proven …