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ARRB1 (Beta-arrestin-1) is a protein that switches other genes on and off. In the public catalogues the evidence so far is association rather than a proven role.
Functions in regulating agonist-mediated G protein-coupled receptor (GPCR) signalling by mediating both receptor desensitisation and resensitisation processes. During homologous desensitisation, beta-arrestins bind to the GPCR-phosphorylated receptor and sterically preclude its coupling to the cognate G protein; the binding appears to require additional receptor determinants exposed only in the active receptor conformation. The beta-arrestins target many receptors for internalisation by acting as endocytic adapters (CLASPs, clathrin-associated sorting proteins) and recruiting the GPRCs to the adapter protein 2 complex 2 (AP-2) in clathrin-coated pits (CCPs).
Open Targets scores its association with cancer at 0.62 (direct and indirect evidence; datatypes literature 0.95, affected pathway 0.97, animal model 0.48, genetic association 0.00).
In plain words · ARRB1 (Beta-arrestin-1) is a protein that switches other genes on and off. In the public catalogues the evidence so far is association rather than a proven role.
ARRB1 (Beta-arrestin-1) is a protein that switches other genes on and off. In the public catalogues the evidence so far is association rather than a proven role.
Functions in regulating agonist-mediated G protein-coupled receptor (GPCR) signalling by mediating both receptor desensitisation and resensitisation processes.
No product in this corpus aims at ARRB1 yet. Transcription factors have no pocket to plug, so drugs either degrade them or block the partner protein they need to dock on DNA.
First described 1993. Earliest sequence paper UniProt cites for the protein: Parruti et al, J. Biol. Chem, 1993, "Molecular analysis of human beta-arrestin-1: cloning, tissue distribution, and regulation of expression. Identification of two isoforms generated by alternative splicing". Source.
Sources: HGNC HGNC:711 (approved symbol, name, aliases, locus and cross-references (hgnc_complete_set.txt)); UniProt P49407 (protein name, function text, keywords and locations (REST API)); Open Targets ENSG00000137486 (association with cancer (MONDO_0004992) 0.62; (GraphQL API, CC0))
Functions in regulating agonist-mediated G protein-coupled receptor (GPCR) signalling by mediating both receptor desensitisation and resensitisation processes. During homologous desensitisation, beta-arrestins bind to the GPCR-phosphorylated receptor and sterically preclude its coupling to the cognate G protein; the binding appears to require additional receptor determinants exposed only in the active receptor conformation. The beta-arrestins target many receptors for internalisation by acting as endocytic adapters (CLASPs, clathrin-associated sorting proteins) and recruiting the GPRCs to the adapter protein 2 complex 2 (AP-2) in clathrin-coated pits (CCPs). However, the extent of beta-arrestin involvement appears to vary significantly depending on the receptor, agonist and cell type. Internalised arrestin-receptor complexes traffic to intracellular endosomes, where they remain uncoupled from G proteins. Two different modes of arrestin-mediated internalisation occur. Location: Cytoplasm; Nucleus; Cell membrane; Membrane, clathrin-coated pit (UniProt). Locus 11q13.4 (HGNC).
Query for this target: (TITLE:"ARRB1" OR ABSTRACT:"ARRB1" OR TITLE:"arrestin beta 1" OR ABSTRACT:"arrestin beta 1" OR TITLE:"Beta-arrestin-1" OR ABSTRACT:"Beta-arrestin-1" OR TITLE:"ARR1" OR ABSTRACT:"ARR1") AND (cancer OR tumor OR tumour OR oncology OR carcinoma OR lymphoma OR leukemia OR leukaemia OR myeloma OR sarcoma OR melanoma OR glioma). Results are unfiltered search hits about ARRB1, not a curated reading list.