Galanin receptor 2 (GALR2)

Galanin receptor 2 (GALR2) is a member of the G protein-coupled receptor (GPCR) superfamily and is encoded by the GALR2 gene[1][5][6]. It is one of three known receptors for the neuropeptide galanin and is predominantly expressed in the central and peripheral nervous systems, as well as the gastrointestinal tract and endocrine tissues[1][6]. GALR2 mediates the biological effects of galanin by activating intracellular signaling primarily via Gq/11 proteins, leading to the stimulation of phospholipase C, increased intracellular calcium, and activation of protein kinase C pathways, but is also capable of coupling to Gi proteins[1][3]. Its activation influences neurotransmitter release, hormone secretion (e.g., growth hormone), modulation of cardiac activity, inhibition of gastrointestinal motility, pain modulation (analgesia), and various neuroendocrine and neuronal processes[1][2]. GALR2 is emerging as a relevant therapeutic target in pain, neurodegenerative and psychiatric disorders, and several cancers, where it can act as a tumor suppressor or be silenced depending on the context[4][8]. Selective ligands, including both agonists and antagonists, are under investigation for their potential therapeutic applications in these diseases[2][4]. Structural studies have enabled detailed modeling of ligand binding and receptor activation, informing rational drug design targeting GALR2[3][5][6].

Other names

GALR2Galanin receptor type 2Galanin receptor subtype 2

Agonism via Gq-mediated activation of phospholipase C/protein kinase C signaling Activation of CaMKII and PKC pathways (analgesic effect in pain models) Dual coupling to Gq and Gi proteins Induction of apoptosis and inhibition of cell proliferation in certain tumor types