G protein-coupled receptor 87 (GPR87)

G protein-coupled receptor 87 (GPR87) is an orphan member of the rhodopsin-like (class A) GPCR superfamily, located on human chromosome 3q25. It is characterized by seven transmembrane domains, conserved motifs (such as the DRY motif), and has been identified as a receptor for lysophosphatidic acid (LPA). GPR87 is overexpressed in multiple cancer types, notably squamous cell carcinoma of the lung and bladder, and is essential for tumor cell survival, particularly under stress conditions mediated by p53. Its involvement in signal transduction, cell survival, and metabolic regulation underscores its promise as a therapeutic target in oncology. However, as an orphan receptor, its endogenous ligand was initially unknown and drug development is ongoing, with no approved antagonists or modulators yet.

Other names

GPR87GPR-87G-protein coupled receptor 87CxLT2-like receptor (rare)H963MGC129731

Approaches under investigation include: Antibody-based (mAb) inhibition of cell-surface GPCRs; Small molecule antagonists or inverse agonists blocking signal transduction; RNAi/gene knockdown or gene editing for target inactivation.