Figure 2.

Pharmacological agents to inhibit downstream signaling intermediated of Gαq. Once GPCR is activated by its agonist, Gαq signaling activates phospholipase C β (PLCβ), which leads to the hydrolysis of phosphatidylinositol 4,5-biphosphate (PIP₂) and diacylglycerol (DAG). The former leads to initiate the release of 1,4,5-inositol tris phosphate (IP₃) initiating calcium release, activating protein tyrosine kinase 2 (PYK2), which leads to proto-oncogene tyrosine protein kinase (Src) activating Ras guanine nucleotide exchange factor (Ras GEF), which leads to the activation of MAPK signaling. MAPK signaling pathway can also be downstream of DAG that activates protein kinase C (PKC), which leads to the activation of MAPK signaling. Gαq signaling can also go indirect of PLCβ by activating Rho GEF leading to the activation of the Rho/ROCK signaling pathway.