Lysophosphatidic acid receptor 3 (LPA3)

Lysophosphatidic acid receptor 3 (LPA3) is a G protein-coupled receptor that serves as a cellular receptor for the bioactive lipid lysophosphatidic acid (LPA). It belongs to the lysophospholipid/EDG family of GPCRs and predominantly couples to several heterotrimeric G proteins, mediating diverse intracellular signaling cascades including mobilization of intracellular calcium, activation of mitogen-activated protein kinases, and modulation of cyclic nucleotide second messengers. LPA3 plays key roles in cell proliferation, survival, migration, and development, and has been implicated in numerous physiological and pathological processes, especially in cancer progression, reproductive biology, fibrosis, and neurodegenerative disorders. Therapeutic modulation of LPA3 is an area of active research, but clinical use is limited by the need for high receptor selectivity and management of potential side effects.

Other names

LPA3EDG7Lysophosphatidic acid receptor 3LPAR3Edg-7

Agonists like LPA activate LPA3 by binding to its extracellular domain, leading to G protein-mediated signal transduction through Gi/Go and Gq/G11 proteins, affecting downstream effectors such as adenylyl cyclase inhibition, intracellular calcium release, and MAPK activation. Antagonists (e.g., Ki16425) block LPA binding, preventing receptor activation and downstream signaling effects, such as cell migration and proliferation.