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...

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Published in:Annual review of pharmacology and toxicology 2010-02, Vol.50 (1), p.157-186
Main Authors: JI WOONG CHOI, HERR, Deron R, CHUN, Jerold, NOGUCHI, Kyoko, YUNG, Yun C, LEE, Chang-Wook, MUTOH, Tetsuji, LIN, Mu-En, TEO, Siew T, PARK, Kristine E, MOSLEY, Alycia N
Format: Article
Language:English
Subjects:
Animals
Biological and medical sciences
Cardiovascular Physiological Phenomena
Cell receptors
Cell structures and functions
Fibrosis
Fundamental and applied biological sciences. Psychology
Humans
Immune System - physiology
Lysophospholipids - metabolism
Miscellaneous
Molecular and cellular biology
Neoplasms - etiology
Nervous System Physiological Phenomena
Obesity - etiology
Receptors, Lysophosphatidic Acid - agonists
Receptors, Lysophosphatidic Acid - antagonists & inhibitors
Receptors, Lysophosphatidic Acid - classification
Receptors, Lysophosphatidic Acid - physiology
Reproduction
Signal Transduction
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Summary: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.
ISSN:0362-1642
1545-4304
DOI:10.1146/annurev.pharmtox.010909.105753