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AttributesValues
rdf:type
rdfs:label
  • GPCR Desensitization Pathway
rdfs:subClassOf
Semantic_Type
  • Functional Concept
Preferred_Name
  • GPCR Desensitization Pathway
UMLS_CUI
  • C1517368
BioCarta_ID
  • h_bArrestinPathway
ALT_DEFINITION
  • Homologous desensitization of GPCRs results from the binding of b-arrestins (b-arr) to agonist -occupied receptors following phosphorylation of the receptor by GRKs. b-arrestin binding sterically precludes coupling between the receptor and heterotrimeric G proteins, leading to termination of signaling by G proteins effectors. Receptor-bound b-arrestins also act as adapter proteins, binding to components of the clathrin endocytic machinery including clathrin, b2-adaptin (AP-2). Receptor sequestration reflects the dynamin (Dyn)-dependent endocytosis of GPCRs via clathrin-coated pits. Once internalized, GPCRs exhibit two distinct patterns of b-arrestin interaction. Class A GPCRs, for example the b2 adrenergic receptor, rapidly dissociate from b-arrestin upon internalization. These receptors are trafficked to an acidified endosomal compartment, wherein the ligand is dissociated and the receptor dephosphorylated by a GPCR-specific protein phosphatase PP2A isoform, and are subsequently recycled to the plasma membrane. Class B receptors, for example the angiotensin II AT1a receptor, form stable receptor-b-arrestin complexes. These receptors accumulate in endocytic vesicles and are either targeted for degradation or slowly recycled to the membrane via as yet poorly defined routes.BIOCARTA
Legacy_Concept_Name
  • GPCR_Desensitization_Pathway
FULL_SYN
  • beta-arrestins in GPCR DesensitizationPTBIOCARTA
  • GPCR Desensitization PathwayPTNCI
code
  • C39000
is someValuesFrom of
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