Tchem GRK2 Beta-adrenergic receptor kinase 1

Protein Summary

Description

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 (PubMed:19306925, PubMed:19715378). Positively regulates ciliary smoothened (SMO)-dependent Hedgehog (Hh) signaling pathway by faciltating the trafficking of SMO into the cilium and the stimulation of SMO activity (By similarity). This gene encodes a member of the G protein-coupled receptor kinase family of proteins. The encoded protein phosphorylates the beta-adrenergic receptor as well as a wide range of other substrates including non-GPCR cell surface receptors, and cytoskeletal, mitochondrial, and transcription factor proteins. Data from rodent models supports a role for this gene in embryonic development, heart function and metabolism. Elevated expression of this gene has been observed in human patients with heart failure and Alzheimer's disease. [provided by RefSeq, Sep 2017]

Uniprot Accession IDs

• P25098
• B0ZBE1
• Q13837
• Q6GTT3
• Beta-ARK-1

Gene Name

• GRK2

Ensembl ID

• ENST00000308595
• ENSP00000312262
• ENSG00000173020

Symbol

• ADRBK1
• BARK
• BARK1
• BARK1
• ADRBK1
• BETA-ARK1

Knowledge Table

Most Knowledge About	Knowledge Value (0 to 1 scale)
biological process	0
biological term	0
cell line	0
cell type or tissue	0
cellular component	0

Protein Classes

PANTHER Classes

Protein / Transferase / Kinase / Protein Kinase / Non-receptor Serine/threonine Protein Kinase / Beta-adrenergic Receptor Kinase 1

DTO Classes

Protein / Kinase / Protein Kinase / Agc Group / Grk Family / Bark Subfamily / Beta-adrenergic Receptor Kinase 1

IDG Development Level Summary

Tdark

These are targets about which virtually nothing is known. They do not have known drug or small molecule activities
- AND - satisfy two or more of the following criteria:

Pubmed score: 593.66   (req: < 5)

Gene RIFs: 166   (req: <= 3)

Antibodies: 626   (req: <= 50)

Tbio

These targets do not have known drug or small molecule activities
- AND - satisfy two or more of the following criteria:

Pubmed score: 593.66   (req: >= 5)

Gene RIFs: 166   (req: > 3)

Antibodies: 626   (req: > 50)

- OR - satisfy the following criterion:

Gene Ontology Terms: 20

Tchem

Target has at least one ChEMBL compound with an activity cutoff of < 30 nM - AND - satisfies the preceding conditions

Active Ligands: 73

Tclin

Target has at least one approved drug - AND - satisfies the preceding conditions

Active Drug: 0