G-Protein–Coupled Receptors

    • G-protein–coupled receptors (GPCRs) make up a large family of cell surface receptors activated by a wide range of ligands, including hormones and neurotransmitters.
    • GPCRs via ligand–receptor interaction can regulate several intracellular signal transduction pathways such as PLC-PKC, AKT/mTOR, and MAPKs, which play a pivotal role in cell proliferation and tumorigenesis.
    • Phospholipase C β (PLCβ) cleaves phosphatidyl inositol biphosphate (PIP2) in the membrane to yield diacylglycerol (DAG) and inositol triphosphate (IP3). IP3 acts as a second messenger that regulates cytosolic Ca2+ levels, which affect cellular functions sm and transcription, and DAG binds and activates protein kinase C (PKC) family (>10 members).
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