The dynamic physiological process involving the up-regulation or down-regulation of hormone receptor numbers on target cell surfaces or within the cytoplasm in response to ambient hormone concentrations or cellular demands. This tuning mechanism is crucial for maintaining cellular sensitivity and appropriate physiological response magnitudes. It represents a key point of hormonal regulation distal to secretion.
Origin
This concept is derived from pharmacology and cellular biology, describing ligand-receptor dynamics. Down-regulation occurs with chronic high exposure, while up-regulation often occurs during periods of relative hormone deficiency. The tuning ensures that the cell adapts its responsiveness to the prevailing endocrine environment.
Mechanism
Chronic exposure to high levels of a hormone, such as excessive insulin, can trigger internalization and degradation of its receptors, reducing density and dampening the signal—a process known as homologous desensitization. Conversely, hormone withdrawal can lead to increased receptor expression to maximize sensitivity to low circulating levels. This fine-tuning mechanism prevents cellular exhaustion or overstimulation.
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