ADRBK1, Blocking Peptide

Beta-adrenergic receptor kinase 1; Beta-ARK-1; G-protein coupled receptor kinase 2; ADRBK1; BARK; BARK1; GRK2

For Research Use Only. Not for use in diagnostic procedures.

The synthetic peptide sequence used to generate the antibody was selected from the C-term region of human GRK2. A 10 to 100 fold molar excess to antibody is recommended. Precise conditions should be optimized for a particular assay.

The synthetic peptide was lyophilized with 100% acetonitrile and is supplied as a powder. Reconstitute with 0.1 ml deionized water for a final concentration of 1 mg/ml.

Maintain refrigerated at 2-8 degree C for up to 6 months. For long term storage store at -20 degree C.

Small volumes of ADRBK1 blocking peptide vial(s) may occasionally become entrapped in the seal of the product vial during shipment and storage. If necessary, briefly centrifuge the vial on a tabletop centrifuge to dislodge any liquid in the container`s cap. Certain products may require to ship with dry ice and additional dry ice fee may apply.

Specifically phosphorylates the agonist-occupied form of the beta-adrenergic and closely related receptors, probably inducing a desensitization of them. Key regulator of LPAR1 signaling. Competes with RALA for binding to LPAR1 thus affecting the signaling properties of the receptor. Desensitizes LPAR1 and LPAR2 in a phosphorylation-independent manner.

79,574 Da

G protein-coupled receptor kinase 2

beta-adrenergic receptor kinase 1

Beta-adrenergic receptor kinase 1

BARK; BARK1; GRK2; Beta-ARK-1  [Similar Products]

ARBK1_HUMAN

The product of this gene phosphorylates the beta-2-adrenergic receptor and appears to mediate agonist-specific desensitization observed at high agonist concentrations. This protein is an ubiquitous cytosolic enzyme that specifically phosphorylates the activated form of the beta-adrenergic and related G-protein-coupled receptors. Abnormal coupling of beta-adrenergic receptor to G protein is involved in the pathogenesis of the failing heart. [provided by RefSeq, Jul 2008]

GRK2: a ubiquitous protein kinase of the GRK family. Phosphorylates the beta-2-adrenergic receptor and related G-protein-coupled receptors. Appears to mediate agonist-specific desensitization observed at high agonist concentrations. Expression level is consistently elevated in chronic human heart failure. Mouse models of severe heart failure have been used to demonstrate that inhibition of BARK1 with a peptide inhibitor is sufficient to increase mean survival, reduce dialation and improve cardiac function.

Protein type: Protein kinase, AGC; Protein kinase, Ser/Thr (non-receptor); EC 2.7.11.15; Kinase, protein; AGC group; GRK family; BARK subfamily

Chromosomal Location of Human Ortholog: 11q13.1

Cellular Component: cytoplasm; cytosol; membrane; plasma membrane

Molecular Function: alpha-2A adrenergic receptor binding; beta-adrenergic receptor kinase activity; Edg-2 lysophosphatidic acid receptor binding; G-protein coupled receptor kinase activity; protein binding; protein kinase activity

Biological Process: acetylcholine receptor signaling, muscarinic pathway; cardiac muscle contraction; desensitization of G-protein coupled receptor protein signaling pathway; entry of virus into host cell; negative regulation of striated muscle contraction; negative regulation of the force of heart contraction by chemical signal; peptidyl-serine phosphorylation; positive regulation of catecholamine secretion; receptor internalization; tachykinin signaling pathway; viral genome replication

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