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| Figure 1: Pharmacological agents for the inhibition of Gαq and downstream signalling. Once activated by a GPCR agonist, Gαq signalling activates Phospholipase C-beta (PLC-β), which hydrolyses Phosphatidylinositol 4,5-bisphosphate (PIP2) leading to the production of Inositol triphosphate (IP3) and Calcium (Ca+2) activating Protein tyrosine kinase 2 (PYK2) which leads to protooncogene tyrosine proteine kinase Src (c-Src) activating Ras Guanine nucleotide exchange factors (Ras GEF) which leads to the activation of MAPK signalling. PLC-β can also signal through Diacylglycerol (DAG) which activates protein kinase C which then leads to the activation of MAPK signalling. |
