Human GRK5 (His Tag) recombinant protein

Human GRK5 (His Tag) recombinant protein

• DataSheet
• Material Safety Data Sheets (MSDS)

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).

G protein-coupled receptor kinase 5

GRK5; GPRK5; FLJ39780

P34947

GRK5; GPRK5

Baculovirus-Insect Cells

A DNA sequence encoding the human GRK5 (NP_005299.1) (Met 1-Ser 590) was fused with a polyhistidine tag at the C-terminus.

Human

The recombinant human GRK5 consists of 600 amino acids and predicts a molecular mass of 69 kDa. The apparent molecular mass of rhGRK5 is approximately 58 kDa in SDS-PAGE under reducing conditions.

> 90 % as determined by SDS-PAGE

No Kinase Activity