The physiological process by which a target cell adjusts the number of specific hormone receptors expressed on its surface or within its cytoplasm in response to changes in hormone concentration or other cellular signals. Regulation is a homeostatic mechanism that determines the cell’s sensitivity to a hormone, with down-regulation typically occurring in response to chronic high exposure and up-regulation in response to chronic low exposure. This dynamic control is fundamental to maintaining endocrine responsiveness.
Origin
This principle is a cornerstone of molecular endocrinology and pharmacology, explaining how cells manage their responsiveness to circulating chemical messengers. The concept of receptor regulation emerged from early studies of insulin and catecholamine signaling, highlighting the cell’s ability to adapt its signal transduction machinery. It is a critical consideration in any hormone replacement therapy.
Mechanism
The mechanism involves intracellular signaling pathways that govern the transcription and translation of receptor genes, as well as the endocytosis and degradation of existing receptors. For example, chronic hyperinsulinemia can lead to the internalization and breakdown of insulin receptors, a process known as down-regulation, which manifests clinically as insulin resistance. Therapeutic regulation aims to restore appropriate receptor expression to enhance hormonal efficacy.
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