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ARRB2 Blocking Peptide (C-Term) Synthetic Peptide Catalog # Bp21771b

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ARRB2 Blocking Peptide (C-Term) Synthetic Peptide Catalog # Bp21771b 10320 Camino Santa Fe, Suite G San Diego, CA 92121 Tel: 858.875.1900 Fax: 858.622.0609 ARRB2 Blocking Peptide (C-Term) Synthetic peptide Catalog # BP21771b Specification ARRB2 Blocking Peptide (C-Term) - ARRB2 Blocking Peptide (C-Term) - Product Background Information Functions in regulating agonist-mediated Primary Accession P32121 G-protein coupled receptor (GPCR) signaling by mediating both receptor desensitization and resensitization processes. During homologous ARRB2 Blocking Peptide (C-Term) - Additional Information desensitization, beta-arrestins bind to the GPRK-phosphorylated receptor and sterically preclude its coupling to the cognate G- protein; Gene ID 409 the binding appears to require additional receptor determinants exposed only in the Other Names active receptor conformation. The Beta-arrestin-2, Arrestin beta-2, ARRB2, beta-arrestins target many receptors for ARB2, ARR2 internalization by acting as endocytic adapters (CLASPs, clathrin-associated sorting proteins) Target/Specificity The synthetic peptide sequence is selected and recruiting the GPRCs to the adapter from aa 284-298 of HUMAN ARRB2 protein 2 complex 2 (AP-2) in clathrin-coated pits (CCPs). However, the extent of Format beta-arrestin involvement appears to vary Peptides are lyophilized in a solid powder significantly depending on the receptor, format. Peptides can be reconstituted in agonist and cell type. Internalized solution using the appropriate buffer as arrestin-receptor complexes traffic to needed. intracellular endosomes, where they remain uncoupled from G-proteins. Two different Storage modes of arrestin-mediated internalization Maintain refrigerated at 2-8°C for up to 6 occur. Class A receptors, like ADRB2, OPRM1, months. For long term storage store at ENDRA, D1AR and ADRA1B dissociate from -20°C. beta- arrestin at or near the plasma membrane and undergo rapid recycling. Class B receptors, Precautions like AVPR2, AGTR1, NTSR1, TRHR and TACR1 This product is for research use only. Not internalize as a complex with arrestin and for use in diagnostic or therapeutic traffic with it to endosomal vesicles, procedures. presumably as desensitized receptors, for extended periods of time. Receptor resensitization then requires that ARRB2 Blocking Peptide (C-Term) - Protein receptor-bound arrestin is removed so that the Information receptor can be dephosphorylated and returned to the plasma membrane. Mediates Name ARRB2 endocytosis of CCR7 following ligation of CCL19 but not CCL21. Involved in Synonyms ARB2, ARR2 internalization of P2RY1, P2RY4, P2RY6 and P2RY11 and ATP-stimulated internalization of Function P2RY2. Involved in phosphorylation-dependent Functions in regulating agonist-mediated internalization of OPRD1 and subsequent G-protein coupled receptor (GPCR) signaling recycling or degradation. Involved in by mediating both receptor desensitization ubiquitination of IGF1R. Beta-arrestins function and resensitization processes. During as multivalent adapter proteins that can switch Page 1/4 10320 Camino Santa Fe, Suite G San Diego, CA 92121 Tel: 858.875.1900 Fax: 858.622.0609 homologous desensitization, beta- arrestins the GPCR from a G-protein signaling mode that bind to the GPRK-phosphorylated receptor transmits short-lived signals from the plasma and sterically preclude its coupling to the membrane via small molecule second cognate G-protein; the binding appears to messengers and ion channels to a require additional receptor determinants beta-arrestin signaling mode that transmits a exposed only in the active receptor distinct set of signals that are initiated as the conformation. The beta-arrestins target receptor internalizes and transits the many receptors for internalization by acting intracellular compartment. Acts as signaling as endocytic adapters (CLASPs, clathrin- scaffold for MAPK pathways such as MAPK1/3 associated sorting proteins) and recruiting (ERK1/2) and MAPK10 (JNK3). ERK1/2 and JNK3 the GPRCs to the adapter protein 2 complex activated by the beta-arrestin scaffold are 2 (AP-2) in clathrin-coated pits (CCPs). largely excluded from the nucleus and However, the extent of beta-arrestin confined to cytoplasmic locations such as involvement appears to vary significantly endocytic vesicles, also called beta-arrestin depending on the receptor, agonist and cell type. Internalized arrestin-receptor signalosomes. Acts as signaling scaffold for the complexes traffic to intracellular AKT1 pathway. GPCRs for which the endosomes, where they remain uncoupled beta-arrestin-mediated signaling relies on both from G-proteins. Two different modes of ARRB1 and ARRB2 (codependent regulation) arrestin- mediated internalization occur. include ADRB2, F2RL1 and PTH1R. For some Class A receptors, like ADRB2, OPRM1, GPCRs the beta-arrestin- mediated signaling ENDRA, D1AR and ADRA1B dissociate from relies on either ARRB1 or ARRB2 and is beta-arrestin at or near the plasma inhibited by the other respective beta-arrestin membrane and undergo rapid recycling. form (reciprocal regulation). Increases ERK1/2 Class B receptors, like AVPR2, AGTR1, signaling in AGTR1- and AVPR2- mediated NTSR1, TRHR and TACR1 internalize as a activation (reciprocal regulation). Involved in complex with arrestin and traffic with it to CCR7- mediated ERK1/2 signaling involving endosomal vesicles, presumably as ligand CCL19. Is involved in type-1A desensitized receptors, for extended angiotensin II receptor/AGTR1-mediated ERK periods of time. Receptor resensitization activity. Is involved in type-1A angiotensin II then requires that receptor-bound arrestin receptor/AGTR1-mediated MAPK10 activity. Is is removed so that the receptor can be involved in dopamine-stimulated AKT1 activity dephosphorylated and returned to the in the striatum by disrupting the association of plasma membrane. Mediates endocytosis of AKT1 with its negative regulator PP2A. Involved CCR7 following ligation of CCL19 but not in AGTR1-mediated chemotaxis. Appears to CCL21. Involved in internalization of P2RY1, function as signaling scaffold involved in P2RY4, P2RY6 and P2RY11 and regulation of MIP-1- beta-stimulated ATP-stimulated internalization of P2RY2. CCR5-dependent chemotaxis. Involved in Involved in phosphorylation-dependent attenuation of NF-kappa-B-dependent internalization of OPRD1 and subsequent recycling or degradation. Involved in transcription in response to GPCR or cytokine ubiquitination of IGF1R. Beta- arrestins stimulation by interacting with and stabilizing function as multivalent adapter proteins CHUK. Suppresses UV-induced that can switch the GPCR from a G-protein NF-kappa-B-dependent activation by signaling mode that transmits short-lived interacting with CHUK. The function is signals from the plasma membrane via promoted by stimulation of ADRB2 and small molecule second messengers and ion dephosphorylation of ARRB2. Involved in channels to a beta-arrestin signaling mode p53/TP53- mediated apoptosis by regulating that transmits a distinct set of signals that MDM2 and reducing the MDM2- mediated are initiated as the receptor internalizes degradation of p53/TP53. May serve as nuclear and transits the intracellular compartment. messenger for GPCRs. Upon stimulation of Acts as signaling scaffold for MAPK OR1D2, may be involved in regulation of gene pathways such as MAPK1/3 (ERK1/2) and expression during the early processes of MAPK10 (JNK3). ERK1/2 and JNK3 activated fertilization. Also involved in regulation of by the beta-arrestin scaffold are largely receptors other than GPCRs. Involved in excluded from the nucleus and confined to endocytosis of TGFBR2 and TGFBR3 and down- cytoplasmic locations such as endocytic regulates TGF-beta signaling such as Page 2/4 10320 Camino Santa Fe, Suite G San Diego, CA 92121 Tel: 858.875.1900 Fax: 858.622.0609 vesicles, also called beta-arrestin NF-kappa-B activation. Involved in endocytosis signalosomes. Acts as signaling scaffold for of low-density lipoprotein receptor/LDLR. the AKT1 pathway. GPCRs for which the Involved in endocytosis of smoothened beta-arrestin- mediated signaling relies on homolog/Smo, which also requires ADRBK1. both ARRB1 and ARRB2 (codependent Involved in endocytosis of SLC9A5. Involved in regulation) include ADRB2, F2RL1 and endocytosis of ENG and subsequent PTH1R. For some GPCRs the beta- TGF-beta-mediated ERK activation and arrestin-mediated signaling relies on either migration of epithelial cells. Involved in ARRB1 or ARRB2 and is inhibited by the Toll-like receptor and IL-1 receptor signaling other respective beta-arrestin form through the interaction with TRAF6 which (reciprocal regulation). Increases ERK1/2 prevents TRAF6 autoubiquitination and signaling in AGTR1- and AVPR2-mediated oligomerization required for activation of activation (reciprocal regulation). Involved NF-kappa-B and JUN. Involved in insulin in CCR7-mediated ERK1/2 signaling resistance by acting as insulin-induced involving ligand CCL19. Is involved in type-1A angiotensin II signaling scaffold for SRC, AKT1 and INSR. receptor/AGTR1-mediated ERK activity. Is Involved in regulation of inhibitory signaling of involved in type-1A angiotensin II natural killer cells by recruiting PTPN6 and receptor/AGTR1-mediated MAPK10 activity. PTPN11 to KIR2DL1. Involved in IL8-mediated Is involved in dopamine-stimulated AKT1 granule release in neutrophils. Involved in the activity in the striatum by disrupting the internalization of the atypical chemokine association of AKT1 with its negative receptor ACKR3. regulator PP2A. Involved in AGTR1-mediated chemotaxis. Appears
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