21.3
Transmembrane receptors are proteins on the cell surface that function as signal transducers and initiate intracellular signaling cascades.
They may be classified as ion channel receptors, G-protein coupled receptors, and enzyme-linked receptors.
Ion channel receptors are divided into two subtypes. The ligand-gated channels open when a ligand binds to the receptor allowing ions to diffuse through the channel.
In contrast, the voltage-gated channels open and close in response to changes in the charge difference across the membrane, allowing ions to move into or out of the cell.
G-protein coupled receptors or GPCRs have their cytoplasmic domain coupled to a heterotrimeric GTP-binding protein. Ligand binding stimulates the exchange of the GDP in the alpha subunit of G-protein with a GTP. This causes the alpha and beta-gamma subunits to dissociate and interact with other effector proteins.
Enzyme-linked receptors either have a cytoplasmic domain that can function as an enzyme or associate directly with intracellular enzymes. Ligand binding promotes receptor dimerization and enzyme activation.
Cell-surface receptors, also known as transmembrane receptors, are cell surface, membrane-anchored (integral) proteins that bind to external ligand mo…
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