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Lysophosphatidic acid (LPA) receptor modulators: Structural features and recent development

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ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2021.113574

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Lysophospholipase D; Lysophosphatidic acid; Proliferation; Migration; Invasion; G-protein coupled receptors; Endothelial differentiating gene; LPA modulators

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Lysophosphatidic acid (LPA) and its receptors play crucial roles in cellular activities and are implicated in the pathogenesis of various diseases. Current research focuses on LPA receptors as new therapeutic targets for treating LPA-associated disorders.
Lysophosphatidic acid (LPA) activates six LPA receptors (LPAR1-6) and regulates various cellular activities such as cell proliferation, cytoprotection, and wound healing. Many studies elucidated the pathological outcomes of LPA are due to the alteration in signaling pathways, which include migration and invasion of cancer cells, fibrosis, atherosclerosis, and inflammation. Current pathophysiological research on LPA and its receptors provides a means that LPA receptors are new therapeutic targets for disorders associated with LPA. Various chemical modulators are developed and are under investigation to treat a wide range of pathological complications. This review summarizes the physiological and pathological roles of LPA signaling, development of various LPA modulators, their structural features, patents, and their clinical outcomes. (C) 2021 Elsevier Masson SAS. All rights reserved.

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