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Receptor Downregulation

Targets & Receptors

A decrease in the number of functional receptors on the cell surface, typically in response to prolonged or excessive agonist stimulation. Mechanisms include receptor internalization via endocytosis, lysosomal degradation, and reduced gene transcription. Clinically, downregulation contributes to drug tolerance and is exploited therapeutically by GnRH agonists.

उदाहरण

  • Beta-adrenergic receptor downregulation with chronic isoproterenol
  • GnRH receptor downregulation by leuprolide (prostate cancer)
  • Insulin receptor downregulation in hyperinsulinemia

क्या आप जानते हैं?

A decrease in the number of functional receptors on the cell surface, typically in response to prolonged or excessive agonist stimulation. Mechanisms include receptor internalization via endocytosis, lysosomal degradation, and …