GRK3/BARK2

GRK3, also known as beta-adrenergic receptor kinase 2 (BARK2), is the paralogue of GRK2 and shares its G protein signalling homology-kinase-pleckstrin homology domain layout, but has a far narrower tissue distribution, being highest in olfactory epithelium, heart and certain brain nuclei. It desensitises the same broad set of agonist-occupied receptors, including beta-adrenergic, opioid and dopamine receptors, and its expression rises in olfactory neurons following odorant exposure as part of sensory adaptation. Human genetic studies have associated GRK3 variants with bipolar disorder and migraine susceptibility. Recombinant GRK3 permits direct comparison with GRK2 in desensitisation, arrestin-recruitment and isoform-selective inhibitor screening.