Phospholipase C Activators Small Molecules and Peptides

Phospholipase C (PLC) (E.C. 3.1.4.11) represents a group of enzymes that catalyze the hydrolysis of phosphatidylinositol 4,5-bisphosphate (PIP₂) to inositol 1,4,5-trisphosphate (IP₃) and 1,2-diacylglycerol (DAG). IP₃ and DAG both have important second messenger functions.

There are numerous subtypes of phospholipase C; PLCβ1-4, PLCγ1-2, PLCδ1-4, PLCε1, PLCζ1 and PLCη1-2, all which require Ca²⁺ ions for catalytic activity. PLC-β is primarily activated by G_q/11 proteins and PLC-γ is activated by tyrosine kinase-mediated phosphorylation in response to a variety of growth factor and immune system signals. PLCε represents a convergence of the 7-TM and receptor tyrosine kinase signaling pathways.