G protein-coupled receptor 34 (GPR34)

G protein-coupled receptor 34 (GPR34) is a member of the class A (rhodopsin-like) family of GPCRs and is encoded by the GPR34 gene in humans[3]. It is an integral membrane protein with seven transmembrane domains[3], and it primarily binds to the endogenous lipid ligand lysophosphatidylserine (LysoPS)[1][3]. GPR34 mediates intracellular signal transduction via activation of heterotrimeric G proteins, leading to diverse physiological responses. Recent structural studies have revealed the mechanisms of activation and inhibition, and suggest that GPR34 plays pathogenic roles in diseases such as neuropathic pain and various cancers[1]. While no approved drugs currently target GPR34 in the clinic, selective antagonists like YL-365 are in preclinical development[1]. Given the centrality of GPCRs as drug targets and the emerging associations of GPR34 with disease, it is considered a receptor with significant therapeutic potential[2][4].

Other names

Probable G-protein coupled receptor 34GPR34PGR34G protein-coupled receptor 34

Agonists (e.g., Lysophosphatidylserine) bind GPR34, inducing conformational changes that enable coupling to G i-proteins and activating downstream signaling[1]. Antagonists (e.g., YL-365) stabilize an inactive state of GPR34, blocking endogenous ligand action and downstream signaling[1].