GRK6
Description
The GRK6 (G protein-coupled receptor kinase 6) is a protein-coding gene located on chromosome 5.
GRK6 is a member of the G protein-coupled receptor kinase subfamily of Ser/Thr protein kinases. It is highly similar to GRK4 and GRK5. GRK6 phosphorylates activated forms of G protein-coupled receptors (GPCRs) to regulate their signaling. This phosphorylation leads to arrestin binding, which prevents receptor activation of G protein transducer proteins, resulting in receptor desensitization. Arrestin binding also directs receptors to specific internalization pathways, removing them from the cell surface and preventing further activation. However, arrestin binding to phosphorylated, active receptors can also enable receptor signaling through arrestin partner proteins. GRK6 and its close relative, GRK5, phosphorylate receptors at sites that promote arrestin-mediated signaling rather than desensitization, internalization, and trafficking (unlike GRK2 and GRK3). This difference contributes to pharmacological biased agonism, where drugs binding to a receptor can preferentially activate specific signaling pathways. GRK6 is widely expressed throughout the body, with particularly high expression in immune cells.
GRK6 is also known as GPRK6.
Associated Diseases
- hereditary angioedema type 3
- congenital factor XII deficiency
- hereditary angioedema
- hypertensive disorder
- Parkinson disease
- multiple sclerosis
- lysosomal storage disease
- Alzheimer disease
- thrombotic disease
