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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. Copyright © 2021 Elsevier Masson SAS. All rights reserved.


Bhagyalalitha Meduri, Gurubasavaraj Veeranna Pujar, T Durai Ananda Kumar, H S Akshatha, Arun Kumar Sethu, Manisha Singh, Abhinav Kanagarla, Bijo Mathew. Lysophosphatidic acid (LPA) receptor modulators: Structural features and recent development. European journal of medicinal chemistry. 2021 Oct 15;222:113574

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PMID: 34126459

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