A physiological or therapeutic process that results in an increase in the number or sensitivity of specific cell surface receptors capable of binding peptide hormones or growth factors. This up-regulation is a crucial mechanism for enhancing cellular responsiveness to circulating signaling molecules, thereby amplifying the downstream biological effect of a peptide. Clinically, this is a target for maximizing the efficacy of endogenous or exogenous peptide-based therapies.
Origin
The term is derived from receptor pharmacology and cellular endocrinology, describing one of the key regulatory mechanisms for signal transduction. Cells dynamically adjust their receptor expression to maintain sensitivity and adapt to fluctuating hormone concentrations.
Mechanism
Up-regulation can be triggered by several factors, including sustained low concentrations of the peptide hormone itself, which prompts the cell to synthesize more receptors to “catch” the scarce signal. Conversely, certain therapeutic agents can directly stimulate the transcription and translation of receptor genes. The resulting increase in receptor density enhances the cell’s capacity to bind the peptide, leading to a stronger and more robust intracellular signaling cascade.
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