Tchem KCNJ3 G protein-activated inward rectifier potassium channel 1

Protein Summary

Description

This potassium channel is controlled by G proteins. Inward rectifier potassium channels are characterized by a greater tendency to allow potassium to flow into the cell rather than out of it. Their voltage dependence is regulated by the concentration of extracellular potassium; as external potassium is raised, the voltage range of the channel opening shifts to more positive voltages. The inward rectification is mainly due to the blockage of outward current by internal magnesium. This receptor plays a crucial role in regulating the heartbeat. Potassium channels are present in most mammalian cells, where they participate in a wide range of physiologic responses. The protein encoded by this gene is an integral membrane protein and inward-rectifier type potassium channel. The encoded protein, which has a greater tendency to allow potassium to flow into a cell rather than out of a cell, is controlled by G-proteins and plays an important role in regulating heartbeat. It associates with three other G-protein-activated potassium channels to form a heteromultimeric pore-forming complex that also couples to neurotransmitter receptors in the brain and whereby channel activation can inhibit action potential firing by hyperpolarizing the plasma membrane. These multimeric G-protein-gated inwardly-rectifying potassium (GIRK) channels may play a role in the pathophysiology of epilepsy, addiction, Down's syndrome, ataxia, and Parkinson's disease. Alternative splicing results in multiple transcript variants encoding distinct proteins. [provided by RefSeq, May 2012]

Uniprot Accession IDs

• P48549
• B4DEW7
• Q8TBI0
• GIRK-1

Gene Name

• KCNJ3

Ensembl ID

• ENST00000295101
• ENSP00000295101
• ENSG00000162989
• ENST00000544049
• ENSP00000438410

Symbol

• GIRK1
• KGA
• GIRK1
• KIR3.1

Knowledge Table

Most Knowledge About	Knowledge Value (0 to 1 scale)
molecular function	0.9
disease perturbation	0.68
PubMedID	0.66
disease	0.63
microRNA	0.59

Protein Classes

DTO Classes

Protein / Ion Channel / Inward Rectifier-type Potassium Channel Family / Kcnj3 Subfamily / G Protein-activated Inward Rectifier Potassium Channel 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: 277.86   (req: < 5)

Gene RIFs: 24   (req: <= 3)

Antibodies: 407   (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: 277.86   (req: >= 5)

Gene RIFs: 24   (req: > 3)

Antibodies: 407   (req: > 50)

- OR - satisfy the following criterion:

Gene Ontology Terms: 11

Tchem

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

Active Ligands: 4

Tclin

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

Active Drug: 0