Lysophosphatidic acid receptor 5 (LPAR5)

Lysophosphatidic acid receptor 5 (LPAR5), also known as GPR92, is a member of the G protein-coupled receptor (GPCR) family that specifically binds lysophosphatidic acid (LPA), a bioactive phospholipid signaling molecule[1][4][5][6]. LPA signaling through LPAR5 regulates a wide range of cellular processes including inflammation, pain transmission, immune cell function, and development, particularly in the central nervous system[1][3][5][6]. LPAR5 is increasingly recognized as a therapeutic target in conditions such as neuropathic pain, multiple sclerosis, cancer, and inflammatory and degenerative diseases. Pharmacological inhibition of LPAR5 with small-molecule antagonists has demonstrated the ability to blunt pro-inflammatory responses and modulate dysfunctional microglial activity, supporting its potential as a druggable target[1][3][5][6].

Other names

GPR92G protein-coupled receptor 92LPA5

Antagonists inhibit pro-inflammatory signaling via LPA/LPAR5 pathway in microglia and other cells, reducing cytokine and chemokine release and modulating cellular activation states. Inhibition modulates G protein–dependent signaling cascades (via G12/13 and Gq pathways), affecting intracellular calcium, cAMP, and phosphorylation of transcription factors such as STAT1/3, p65, and c-Jun.