CD36 inhibitors reduce postprandial hypertriglyceridemia and protect against diabetic dyslipidemia and atherosclerosis.

CD36 is recognized as a lipid and fatty acid receptor and plays an important role in the metabolic syndrome and associated cardiac events. The pleiotropic activity and the multiple molecular associations of this scavenger receptor with membrane associated molecules in different cells and tissues hav...

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Autores principales: Alain Geloen, Lionel Helin, Benjamine Geeraert, Eric Malaud, Paul Holvoet, Gerard Marguerie
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Lenguaje:EN
Publicado: Public Library of Science (PLoS) 2012
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Acceso en línea:https://doaj.org/article/4639332cd7ca4104a34711ed04f4f491
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spelling oai:doaj.org-article:4639332cd7ca4104a34711ed04f4f4912021-11-18T07:17:22ZCD36 inhibitors reduce postprandial hypertriglyceridemia and protect against diabetic dyslipidemia and atherosclerosis.1932-620310.1371/journal.pone.0037633https://doaj.org/article/4639332cd7ca4104a34711ed04f4f4912012-01-01T00:00:00Zhttps://www.ncbi.nlm.nih.gov/pmc/articles/pmid/22662181/pdf/?tool=EBIhttps://doaj.org/toc/1932-6203CD36 is recognized as a lipid and fatty acid receptor and plays an important role in the metabolic syndrome and associated cardiac events. The pleiotropic activity and the multiple molecular associations of this scavenger receptor with membrane associated molecules in different cells and tissues have however questioned its potential as a therapeutic target. The present study shows that it is possible to identify low molecular weight chemicals that can block the CD36 binding and uptake functions. These inhibitors were able to reduce arterial lipid deposition, fatty acid intestinal transit, plasma concentration of triglycerides and glucose, to improve insulin sensitivity, glucose tolerance and to reduce the plasma concentration of HbAc1 in different and independent rodent models. Correlation between the anti-CD36 activity of these inhibitors and the known pathophysiological activity of this scavenger receptor in the development of atherosclerosis and diabetes were observed at pharmacological doses. Thus, CD36 might represent an attractive therapeutic target.Alain GeloenLionel HelinBenjamine GeeraertEric MalaudPaul HolvoetGerard MargueriePublic Library of Science (PLoS)articleMedicineRScienceQENPLoS ONE, Vol 7, Iss 5, p e37633 (2012)
institution DOAJ
collection DOAJ
language EN
topic Medicine
R
Science
Q
spellingShingle Medicine
R
Science
Q
Alain Geloen
Lionel Helin
Benjamine Geeraert
Eric Malaud
Paul Holvoet
Gerard Marguerie
CD36 inhibitors reduce postprandial hypertriglyceridemia and protect against diabetic dyslipidemia and atherosclerosis.
description CD36 is recognized as a lipid and fatty acid receptor and plays an important role in the metabolic syndrome and associated cardiac events. The pleiotropic activity and the multiple molecular associations of this scavenger receptor with membrane associated molecules in different cells and tissues have however questioned its potential as a therapeutic target. The present study shows that it is possible to identify low molecular weight chemicals that can block the CD36 binding and uptake functions. These inhibitors were able to reduce arterial lipid deposition, fatty acid intestinal transit, plasma concentration of triglycerides and glucose, to improve insulin sensitivity, glucose tolerance and to reduce the plasma concentration of HbAc1 in different and independent rodent models. Correlation between the anti-CD36 activity of these inhibitors and the known pathophysiological activity of this scavenger receptor in the development of atherosclerosis and diabetes were observed at pharmacological doses. Thus, CD36 might represent an attractive therapeutic target.
format article
author Alain Geloen
Lionel Helin
Benjamine Geeraert
Eric Malaud
Paul Holvoet
Gerard Marguerie
author_facet Alain Geloen
Lionel Helin
Benjamine Geeraert
Eric Malaud
Paul Holvoet
Gerard Marguerie
author_sort Alain Geloen
title CD36 inhibitors reduce postprandial hypertriglyceridemia and protect against diabetic dyslipidemia and atherosclerosis.
title_short CD36 inhibitors reduce postprandial hypertriglyceridemia and protect against diabetic dyslipidemia and atherosclerosis.
title_full CD36 inhibitors reduce postprandial hypertriglyceridemia and protect against diabetic dyslipidemia and atherosclerosis.
title_fullStr CD36 inhibitors reduce postprandial hypertriglyceridemia and protect against diabetic dyslipidemia and atherosclerosis.
title_full_unstemmed CD36 inhibitors reduce postprandial hypertriglyceridemia and protect against diabetic dyslipidemia and atherosclerosis.
title_sort cd36 inhibitors reduce postprandial hypertriglyceridemia and protect against diabetic dyslipidemia and atherosclerosis.
publisher Public Library of Science (PLoS)
publishDate 2012
url https://doaj.org/article/4639332cd7ca4104a34711ed04f4f491
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AT benjaminegeeraert cd36inhibitorsreducepostprandialhypertriglyceridemiaandprotectagainstdiabeticdyslipidemiaandatherosclerosis
AT ericmalaud cd36inhibitorsreducepostprandialhypertriglyceridemiaandprotectagainstdiabeticdyslipidemiaandatherosclerosis
AT paulholvoet cd36inhibitorsreducepostprandialhypertriglyceridemiaandprotectagainstdiabeticdyslipidemiaandatherosclerosis
AT gerardmarguerie cd36inhibitorsreducepostprandialhypertriglyceridemiaandprotectagainstdiabeticdyslipidemiaandatherosclerosis
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