Follicle-Stimulating Hormone Receptor: Advances and Remaining Challenges.

摘要: Follicle-stimulating hormone (FSH) is produced in the pituitary and essential for reproduction. It specifically binds to a membrane receptor (FSHR) expressed somatic cells of gonads. The FSH/FSHR system presents many peculiarities compared classical G protein-coupled receptors (GPCRs). FSH large naturally heterogeneous heterodimeric glycoprotein. FSHR characterized by very NH2-terminal extracellular domain, which participates activation/inactivation switch receptor. Once activated, couples Gαs and, some instances, other Gα-subunits. GPCR kinases β-arrestins are also recruited account its desensitization, control trafficking intracellular signaling. Of note, internalization recycling fast involve early endosomes (EE) instead EE. All transduction mechanisms triggered upon stimulation lead activation complex signaling network that controls gene expression acting at multiple levels. integration these not only leads context-adapted responses from target gonadal but indirectly affects fate germ cells. Depending on physiological/developmental stage, elicits proliferation, differentiation, or apoptosis order maintain homeostasis reproductive system. Pharmacological tools targeting recently came fore open promising prospects both basic research therapeutic applications. This chapter provides an updated review most salient aspects biology pharmacology.