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Molecular basis for lysophosphatidic acid receptor antagonist selectivity

Biochimica et Biophysica Acta (BBA) - Molecular and Cell Biology of Lipids, 2002
Recent characterization of lysophosphatidic acid (LPA) receptors has made possible studies elucidating the structure-activity relationships (SAR) for agonist activity at individual receptors. Additionally, the availability of these receptors has allowed the identification of antagonists of LPA-induced effects.
Vineet M, Sardar   +9 more
openaire   +2 more sources

Comparative analyses of lysophosphatidic acid receptor-mediated signaling

Cellular and Molecular Life Sciences, 2015
Lysophosphatidic acid (LPA) is a bioactive lipid mediator that activates G protein-coupled LPA receptors to exert fundamental cellular functions. Six LPA receptor genes have been identified in vertebrates and are classified into two subfamilies, the endothelial differentiation genes (edg) and the non-edg family.
Nobuyuki, Fukushima   +4 more
openaire   +2 more sources

Lysophosphatidic acid-1-receptor targeting agents for fibrosis

Expert Opinion on Investigational Drugs, 2011
The presence of fibrosis is associated with alterations in organ architecture and is responsible for the morbidity of diseases including pneumopathies, systemic sclerosis, liver cirrhosis, chronic cardiovascular diseases, progressive kidney diseases and diabetes.
Rancoule, Chloé   +7 more
openaire   +3 more sources

Functional lysophosphatidic acid receptors expressed in Oryzias latipes

Gene, 2014
Lysophosphatidic acid (LPA) signaling is known to play biological and pathophysiological roles in many types of animals. Medaka (Oryzias latipes) is an experimental fish that can be easily maintained, propagated, and analyzed, and whose genome has been completely sequenced. However, there is limited information available regarding medaka LPA receptors.
Yuji, Morimoto   +6 more
openaire   +2 more sources

Lysophosphatidic acid stimulates pericyte migration via LPA receptor 1

Biochemical and Biophysical Research Communications, 2022
Lysophosphatidic acid (LPA) is a bioactive compound known to regulate various vascular functions. However, despite the fact that many vascular functions are regulated by peri-vascular cells such as pericytes, the effect of LPA on brain pericytes has not been fully evaluated. Thus, we designed this study to evaluate the effects of LPA on brain pericytes.
Yoshino Yonezu   +3 more
openaire   +2 more sources

Characterization of a Receptor Subtype-Selective Lysophosphatidic Acid Mimetic

Molecular Pharmacology, 1998
Despite an intriguing cell biology and the suggestion of a role in pathophysiological responses, the mechanism of action of such lipid phosphoric acid mediators as lysophosphatidic acid (LPA) remains obscure, in part because of an underdeveloped medicinal chemistry.
S B, Hooks   +6 more
openaire   +2 more sources

Stereochemical properties of lysophosphatidic acid receptor activation and metabolism

Biochimica et Biophysica Acta (BBA) - Molecular and Cell Biology of Lipids, 2002
Ligand recognition by G protein-coupled receptors (GPCR), as well as substrate recognition by enzymes, almost always shows a preference for a naturally occurring enantiomer over the unnatural one. Recognition of lysophosphatidic acid (LPA) by its receptors is an exception, as both the natural L (R) and unnatural D (S) stereoisomers of LPA are equally ...
Kazuaki, Yokoyama   +6 more
openaire   +2 more sources

Lysophosphatidic acid receptor (LPAR) modulators: The current pharmacological toolbox

Progress in Lipid Research, 2015
Lysophosphatidic acids (LPA) are key lipid-signalling molecules that regulate a remarkably diverse set of cellular events, such as motility, chemotaxis, cell cycle progression, viability, and wound healing. The physiological and pathophysiological consequences of LPA signalling are evident and misregulation of LPA signalling can lead to pathologies ...
Sabin Llona-Minguez   +2 more
openaire   +3 more sources

Initiation of neuropathic pain requires lysophosphatidic acid receptor signaling

Nature Medicine, 2004
Lysophosphatidic acid (LPA) is a bioactive lipid with activity in the nervous system mediated by G-protein-coupled receptors. Here, we examined the role of LPA signaling in the development of neuropathic pain by pharmacological and genetic approaches, including the use of mice lacking the LPA(1) receptor.
Makoto, Inoue   +5 more
openaire   +2 more sources

Identification and characterization of a lysophosphatidic acid receptor.

Molecular Pharmacology, 1994
A specific binding site for 1-[3H]stearoyl-lysophosphatidic acid (stearoyl-LPA) was identified and characterized in membranes prepared from rat brain and Swiss 3T3 fibroblasts. Specific binding of [3H]LPA to these sites was protein dependent, was saturable, reached equilibrium in 15 min, and was displacable by the addition of excess unlabeled LPA ...
F J, Thomson   +3 more
openaire   +2 more sources

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