LPA receptors: subtypes and biological actions.
Lysophosphatidic acid (LPA) is a small, ubiquitous phospholipid that acts as an extracellular signaling molecule by binding to and activating at least five known G protein-coupled receptors (GPCRs): LPA(1)-LPA(5). They are encoded by distinct genes named LPAR1-LPAR5 in humans and Lpar1-Lpar5 in mice. The biological roles of LPA are diverse and include developmental, physiological, and pathophysiological effects. This diversity is mediated by broad and overlapping expression patterns and multiple downstream signaling pathways activated by cognate LPA receptors. Studies using cloned receptors and genetic knockout mice have been instrumental in uncovering the significance of this signaling system, notably involving basic cellular processes as well as multiple organ systems such as the nervous system. This has further provided valuable proof-of-concept data to support LPA receptors and LPA metabolic enzymes as targets for the treatment of medically important diseases that include neuropsychiatric disorders, neuropathic pain, infertility, cardiovascular disease, inflammation, fibrosis, and cancer.
Choi
Ji Woong
JW
Department of Molecular Biology, Helen L. Dorris Institute for Neurological and Psychiatric Disorders, The Scripps Research Institute, La Jolla, California 92037, USA.
Herr
Deron R
DR
Noguchi
Kyoko
K
Yung
Yun C
YC
Lee
Chang-Wook
CW
Mutoh
Tetsuji
T
Lin
Mu-En
ME
Teo
Siew T
ST
Park
Kristine E
KE
Mosley
Alycia N
AN
Chun
Jerold
J
D000818:Animals; D002320:Cardiovascular Physiological Phenomena; D005355:Fibrosis; D006801:Humans; D007107:Immune System / Q000502:physiology; D008246:Lysophospholipids / Q000378:metabolism; D009369:Neoplasms / Q000209:etiology; D009424:Nervous System Physiological Phenomena; D009765:Obesity / Q000209:etiology; D049368:Receptors, Lysophosphatidic Acid / Q000819:agonists / Q000037:antagonists & inhibitors / Q000145:classification* / Q000502:physiology*; D012098:Reproduction; D015398:Signal Transduction
D008246:Lysophospholipids; D049368:Receptors, Lysophosphatidic Acid; C032881:lysophosphatidic acid