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The status of the lysophosphatidic acid receptor type 1 (LPA1R)

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González Gil, Inés and Zian, Debora and Vázquez Villa, Henar and Ortega Gutiérrez, Silvia and López Rodríguez, María L. (2015) The status of the lysophosphatidic acid receptor type 1 (LPA1R). Medicinal Chemical Communications, 6 . pp. 13-23. ISSN 2040-2503 (Print) , 2040-2511 (Online)

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Official URL: http://pubs.rsc.org/en/content/articlelanding/2015/md/c4md00333k#!divAbstract



Abstract

Lysophospholipids are lipid molecules that are receiving growing attention because, in addition to their structural function in the cell membrane, they are now regarded as important regulators for diverse biological functions through activation of specific receptors. These receptors have been characterized during the last two decades as G protein-coupled receptors (GPCRs) and, among them, two families stand out: lysophosphatidic acid (LPA1–6) and sphingosine 1-phoshate (S1P1–5) receptors. Despite their interest, the high structural similarity between them has restrained the development of selective and high affinity ligands and therefore the elucidation of the role of these receptors in the central nervous system (CNS). This review provides an overview about the different LPA receptors with a special focus on the LPA1 subtype from a medicinal chemistry perspective. It summarizes the most recent developments in the search for selective and specific agonists and antagonists of the LPA1 receptor and highlights their current status in the drug development pipeline.


Item Type:Article
Uncontrolled Keywords:EMTREE drug terms: am 095; am 966; bms 986020; digoxin; flurbiprofen; G protein coupled receptor; ki 16425; lysophosphatidic acid receptor; membrane phospholipid; montelukast; protein LPA1R; receptor blocking agent; receptor subtype; sar 100842; unclassified drug EMTREE medical terms: cell migration; cell proliferation; cell survival; drug design; drug development; drug potentiation; drug receptor binding; drug screening; drug structure; fibrosing alveolitis; human; lipid degradation; medicinal chemistry; membrane structure; neurologic disease; nonhuman; phase 1 clinical trial (topic); phase 2 clinical trial (topic); phospholipid synthesis; protein function; Review; signal transduction; structure analysis; systemic sclerosis; tissue distribution
Subjects:Sciences > Chemistry > Chemistry, Organic
ID Code:34470
Deposited On:25 Nov 2015 11:31
Last Modified:01 Jul 2016 23:01

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