Articles with "autotaxin" as a keyword



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Establishment of a novel, cell-based autotaxin assay.

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Published in 2021 at "Analytical biochemistry"

DOI: 10.1016/j.ab.2021.114322

Abstract: Autotaxin (ATX) plays an important role in (patho-)physiological lysophosphatidic acid (LPA) signaling. Here we describe the establishment of novel cell-based ATX assay formats. ATX-mediated LPA generation is detected by using a stable LPA receptor reporter… read more here.

Keywords: atx; autotaxin; novel cell; cell based ... See more keywords
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Oxidative stress mediated myocardial lysophosphatidic acid signaling

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Published in 2018 at "Free Radical Biology and Medicine"

DOI: 10.1016/j.freeradbiomed.2018.10.206

Abstract: The bioactive lysophosphatidic acid (LPA) plays a well-known role in atherosclerotic disease, whereas, its role in myocardial function remains virtually unexplored. Following acute myocardial infarction, serum LPA concentration rises by six-fold over control human subjects,… read more here.

Keywords: autotaxin; lpa; lpp3; lysophosphatidic acid ... See more keywords
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Identification and pharmacological characterization of a novel inhibitor of autotaxin in rodent models of joint pain.

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Published in 2017 at "Osteoarthritis and cartilage"

DOI: 10.1016/j.joca.2016.09.006

Abstract: OBJECTIVE Autotaxin is a secreted lysophospholipase that mediates the conversion of lysophosphatidyl choline (LPC) to lysophosphatidic acid (LPA), a bioactive lipid mediator. Autotaxin levels in plasma and synovial fluid correlate with disease severity in patients… read more here.

Keywords: inhibitor; autotaxin; joint pain; inhibitor autotaxin ... See more keywords
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A Novel Autotaxin Inhibitor for the Treatment of Idiopathic Pulmonary Fibrosis: A Clinical Candidate Discovered Using DNA-Encoded Chemistry.

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Published in 2020 at "Journal of medicinal chemistry"

DOI: 10.1021/acs.jmedchem.0c00688

Abstract: The activity of the secreted phosphodiesterase autotaxin produces the inflammatory signaling molecule LPA and has been associated with a number of human diseases including idiopathic pulmonary fibrosis (IPF). We screened a single DNA-encoded chemical library… read more here.

Keywords: idiopathic pulmonary; autotaxin; chemistry; dna encoded ... See more keywords
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Structure-Based Design of a Novel Class of Autotaxin Inhibitors Based on Endogenous Allosteric Modulators

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Published in 2022 at "Journal of Medicinal Chemistry"

DOI: 10.1021/acs.jmedchem.2c00368

Abstract: Autotaxin (ATX) facilitates the hydrolysis of lysophosphatidylcholine to lysophosphatidic acid (LPA), a bioactive phospholipid, which facilitates a diverse range of cellular effects in multiple tissue types. Abnormal LPA expression can lead to the progression of… read more here.

Keywords: autotaxin; based design; atx; class ... See more keywords
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Rational Design of Autotaxin Inhibitors by Structural Evolution of Endogenous Modulators.

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Published in 2017 at "Journal of medicinal chemistry"

DOI: 10.1021/acs.jmedchem.6b01743

Abstract: Autotaxin produces the bioactive lipid lysophosphatidic acid (LPA) and is a drug target of considerable interest for numerous pathologies. We report the expedient, structure-guided evolution of weak physiological allosteric inhibitors (bile salts) into potent competitive… read more here.

Keywords: evolution; inhibitors structural; autotaxin; rational design ... See more keywords
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Hydroxamic Acids Constitute a Novel Class of Autotaxin Inhibitors that Exhibit in Vivo Efficacy in a Pulmonary Fibrosis Model.

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Published in 2018 at "Journal of medicinal chemistry"

DOI: 10.1021/acs.jmedchem.8b00232

Abstract: Autotaxin (ATX) catalyzes the hydrolysis of lysophosphatidylcholine (LPC) generating the lipid mediator lysophosphatidic acid (LPA). Both ATX and LPA are involved in various pathological inflammatory conditions, including fibrosis and cancer, and have attracted great interest… read more here.

Keywords: atx; fibrosis; autotaxin; hydroxamic acids ... See more keywords
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Autotaxin activity predicts transplant-free survival in primary sclerosing cholangitis

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Published in 2019 at "Scientific Reports"

DOI: 10.1038/s41598-019-44762-7

Abstract: Autotaxin has been associated with liver disease severity and transplant-free survival. This study aimed to validate autotaxin as a biomarker in two cohorts of Norwegian large-duct PSC patients, one discovery panel (nā€‰=ā€‰165) and one validation… read more here.

Keywords: transplant free; autotaxin; free survival; autotaxin activity ... See more keywords
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Autotaxin is a potential link between genetic risk factors and immunological disturbances of plasmacytoid dendritic cells in systematic lupus erythematosus

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Published in 2022 at "Lupus"

DOI: 10.1177/09612033221128494

Abstract: Background The importance of autotaxin, an enzyme that catalyzes lysophospholipid production, has recently been recognized in various diseases, including cancer and autoimmune diseases. Herein, we examined the role of autotaxin in systemic lupus erythematosus (SLE),… read more here.

Keywords: autotaxin; patients sle; expression; risk factors ... See more keywords
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Commonalities Between ARDS, Pulmonary Fibrosis and COVID-19: The Potential of Autotaxin as a Therapeutic Target

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Published in 2021 at "Frontiers in Immunology"

DOI: 10.3389/fimmu.2021.687397

Abstract: Severe COVID-19 is characterized by acute respiratory distress syndrome (ARDS)-like hyperinflammation and endothelial dysfunction, that can lead to respiratory and multi organ failure and death. Interstitial lung diseases (ILD) and pulmonary fibrosis confer an increased… read more here.

Keywords: covid; autotaxin; pulmonary fibrosis; therapeutic target ... See more keywords
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Autotaxin Inhibition with IOA-289 Decreases Breast Tumor Growth in Mice whereas Knockout of Autotaxin in Adipocytes Does Not

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Published in 2023 at "Cancers"

DOI: 10.3390/cancers15112937

Abstract: Simple Summary Breast cancer cells produce negligible quantities of autotaxin. We hypothesized that the autotaxin produced by inflamed breast adipocytes adjacent to breast tumors provides a major source of autotaxin secretion that drives breast tumor… read more here.

Keywords: growth; breast tumor; mice; autotaxin ... See more keywords