Clinical Endocrinology & Metabolism

 Internalization of GPCRs: implication in receptor function, physiology and diseases
G protein-coupled receptors (GPCRs) are the largest family of membrane receptors and mediate the effects of numerous hormones and neurotransmitters. The nearly 1,000 GPCRs encoded by the human genome regulate virtually all physiological functions and are implicated in the pathogenesis of prevalent human diseases such as thyroid disorders, hypertension or Parkinsonīs disease. As a result, 30 to 50% of all currently prescribed drugs are targeting these receptors. Once activated, GPCRs induce signals at the cell surface.