The molecular and cellular processes by which a target cell increases the number or sensitivity of its surface receptors in response to specific physiological cues or therapeutic interventions. This phenomenon is a key adaptive mechanism that enhances cellular responsiveness to a hormone or neurotransmitter, thereby amplifying the biological signal. Upregulation is often triggered by a lack of stimulating ligand or by specific signaling molecules, serving as a critical strategy to restore or maximize hormonal efficacy in a clinical setting.
Origin
This term is a fundamental concept in molecular endocrinology and pharmacology, describing one of the primary ways cells maintain sensitivity to their environment. It is the counter-mechanism to receptor downregulation, which occurs upon chronic overstimulation. The clinical application of these mechanisms is central to desensitization avoidance protocols.
Mechanism
The process typically involves increased gene transcription and translation of the receptor protein, followed by the insertion of newly synthesized receptors into the cell membrane. A common trigger is prolonged exposure to low levels of the ligand, causing the cell to become “hypersensitive” by increasing its receptor count. Furthermore, certain growth factors or pharmacological agents can stabilize existing receptors on the cell surface, preventing their internalization and degradation, effectively increasing the net functional concentration.
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