Anti-GRK5 Antibody Picoband® Fluoro647 Conjugated

G protein-coupled receptor kinase 5?is an?enzyme?that in humans is encoded by the?GRK5?gene. It is mapped to 10q26.11. This gene encodes a member of the guanine nucleotide-binding protein (G protein) -coupled receptor kinase subfamily of the Ser/Thr protein kinase family. The protein phosphorylates the activated forms of G protein-coupled receptors thus initiating their deactivation. It has also been shown to play a role in regulating the motility of polymorphonuclear leukocytes (PMNs) .

A synthetic peptide corresponding to a sequence at the C-terminus of human GRK5, different from the related mouse and rat sequences by three amino acids.

Atherosclerosis, Cardiovascular, G Protein Signaling, Heterotrimeric G Proteins, Protein Phosphorylation, Ser/Thr Kinases, Signal Transduction, Signaling Pathway, Vascular Inflammation

Serine/threonine kinase that phosphorylates preferentially the activated forms of a variety of G-protein- coupled receptors (GPCRs) . Such receptor phosphorylation initiates beta-arrestin-mediated receptor desensitization, internalization, and signaling events leading to their down-regulation. Phosphorylates a variety of GPCRs, including adrenergic receptors, muscarinic acetylcholine receptors (more specifically Gi-coupled M2/M4 subtypes), dopamine receptors and opioid receptors. In addition to GPCRs, also phosphorylates various substrates: Hsc70- interacting protein/ST13, TP53/p53, HDAC5, and arrestin-1/ARRB1. Phosphorylation of ARRB1 by GRK5 inhibits G-protein independent MAPK1/MAPK3 signaling downstream of 5HT4-receptors. Phosphorylation of HDAC5, a repressor of myocyte enhancer factor 2 (MEF2) leading to nuclear export of HDAC5 and allowing MEF2- mediated transcription. Phosphorylation of TP53/p53, a crucial tumor suppressor, inhibits TP53/p53-mediated apoptosis. Phosphorylation of ST13 regulates internalization of the chemokine receptor. Phosphorylates rhodopsin (RHO) (in vitro) and a non G- protein-coupled receptor, LRP6 during Wnt signaling (in vitro) . .

1. Entrez Gene: GRK5 G protein-coupled receptor kinase 5. 2. Bullrich F, Druck T, Kunapuli P, et al. (1995) . Chromosomal mapping of the genes GPRK5 and GPRK6 encoding G protein-coupled receptor kinases GRK5 and GRK6.. Cytogenet. Cell Genet. 70 (3–4) : 250–4. 3. Kunapuli P, Benovic JL (Jul 1993) . Cloning and expression of GRK5: a member of the G protein-coupled receptor kinase family. Proc Natl Acad Sci U S A 90 (12) : 5588–92.

Cytoplasm. Nucleus. Cell membrane; Peripheral membrane protein. Predominantly localized at the plasma membrane; targeted to the cell surface through the interaction with phospholipids. Nucleus localization is regulated in a GPCR and Ca (2+) /calmodulin-dependent fashion.