Lysophosphatidic Acid Receptor Antagonists and Cancer: The Current Trends, Clinical Implications, and Trials

Lysophosphatidic acid (LPA) is a bioactive lipid mediator primarily derived from membrane phospholipids. LPA initiates cellular effects upon binding to a family of G protein-coupled receptors, termed LPA receptors (LPAR1 to LPAR6). LPA signaling drives cell migration and proliferation, cytokine prod...

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Main Authors: Yu-Hsuan Lin, Yueh-Chien Lin, Chien-Chin Chen
Format: Article
Language:English
Published: MDPI AG 2021-06-01
Series:Cells
Subjects:
Online Access:https://www.mdpi.com/2073-4409/10/7/1629
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author Yu-Hsuan Lin
Yueh-Chien Lin
Chien-Chin Chen
author_facet Yu-Hsuan Lin
Yueh-Chien Lin
Chien-Chin Chen
author_sort Yu-Hsuan Lin
collection DOAJ
description Lysophosphatidic acid (LPA) is a bioactive lipid mediator primarily derived from membrane phospholipids. LPA initiates cellular effects upon binding to a family of G protein-coupled receptors, termed LPA receptors (LPAR1 to LPAR6). LPA signaling drives cell migration and proliferation, cytokine production, thrombosis, fibrosis, angiogenesis, and lymphangiogenesis. Since the expression and function of LPA receptors are critical for cellular effects, selective antagonists may represent a potential treatment for a broad range of illnesses, such as cardiovascular diseases, idiopathic pulmonary fibrosis, voiding dysfunctions, and various types of cancers. More new LPA receptor antagonists have shown their therapeutic potentials, although most are still in the preclinical trial stage. This review provided integrative information and summarized preclinical findings and recent clinical trials of different LPA receptor antagonists in cancer progression and resistance. Targeting LPA receptors can have potential applications in clinical patients with various diseases, including cancer.
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spelling doaj.art-57d530c8c1d04362b00dea966193fd762023-11-22T02:12:05ZengMDPI AGCells2073-44092021-06-01107162910.3390/cells10071629Lysophosphatidic Acid Receptor Antagonists and Cancer: The Current Trends, Clinical Implications, and TrialsYu-Hsuan Lin0Yueh-Chien Lin1Chien-Chin Chen2Institute of Biomedical Sciences, National Sun Yat-Sen University, Kaohsiung 804, TaiwanDepartment of Life Science, National Taiwan University, Taipei 106, TaiwanDepartment of Pathology, Ditmanson Medical Foundation Chia-Yi Christian Hospital, Chiayi 600, TaiwanLysophosphatidic acid (LPA) is a bioactive lipid mediator primarily derived from membrane phospholipids. LPA initiates cellular effects upon binding to a family of G protein-coupled receptors, termed LPA receptors (LPAR1 to LPAR6). LPA signaling drives cell migration and proliferation, cytokine production, thrombosis, fibrosis, angiogenesis, and lymphangiogenesis. Since the expression and function of LPA receptors are critical for cellular effects, selective antagonists may represent a potential treatment for a broad range of illnesses, such as cardiovascular diseases, idiopathic pulmonary fibrosis, voiding dysfunctions, and various types of cancers. More new LPA receptor antagonists have shown their therapeutic potentials, although most are still in the preclinical trial stage. This review provided integrative information and summarized preclinical findings and recent clinical trials of different LPA receptor antagonists in cancer progression and resistance. Targeting LPA receptors can have potential applications in clinical patients with various diseases, including cancer.https://www.mdpi.com/2073-4409/10/7/1629antagonistcancerclinical triallysophosphatidic acidlysophosphatidic receptortherapy
spellingShingle Yu-Hsuan Lin
Yueh-Chien Lin
Chien-Chin Chen
Lysophosphatidic Acid Receptor Antagonists and Cancer: The Current Trends, Clinical Implications, and Trials
Cells
antagonist
cancer
clinical trial
lysophosphatidic acid
lysophosphatidic receptor
therapy
title Lysophosphatidic Acid Receptor Antagonists and Cancer: The Current Trends, Clinical Implications, and Trials
title_full Lysophosphatidic Acid Receptor Antagonists and Cancer: The Current Trends, Clinical Implications, and Trials
title_fullStr Lysophosphatidic Acid Receptor Antagonists and Cancer: The Current Trends, Clinical Implications, and Trials
title_full_unstemmed Lysophosphatidic Acid Receptor Antagonists and Cancer: The Current Trends, Clinical Implications, and Trials
title_short Lysophosphatidic Acid Receptor Antagonists and Cancer: The Current Trends, Clinical Implications, and Trials
title_sort lysophosphatidic acid receptor antagonists and cancer the current trends clinical implications and trials
topic antagonist
cancer
clinical trial
lysophosphatidic acid
lysophosphatidic receptor
therapy
url https://www.mdpi.com/2073-4409/10/7/1629
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AT chienchinchen lysophosphatidicacidreceptorantagonistsandcancerthecurrenttrendsclinicalimplicationsandtrials