Peptide Receptor Activation is the specific binding event of a peptide hormone, such as insulin or growth hormone, to its corresponding transmembrane receptor located on the surface of a target cell, initiating a defined intracellular signaling cascade. This binding event is the primary trigger for the peptide’s intended physiological action within that specific tissue. Receptor activation kinetics are highly dependent on ligand concentration and receptor density.
Origin
This concept is derived directly from endocrinology, where ‘peptide’ denotes the class of small protein hormones synthesized via ribosomal machinery, and ‘receptor activation’ describes the functional consequence of ligand binding to the membrane protein.
Mechanism
Activation involves the peptide ligand binding to the extracellular domain of the receptor, inducing dimerization or a necessary conformational change that exposes or activates the intracellular kinase domain. This leads to autophosphorylation and the subsequent recruitment of downstream signaling molecules like Insulin Receptor Substrates (IRS) or STAT proteins. Proper activation fidelity is essential for accurate downstream metabolic or growth responses.
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