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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2012
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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) |
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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 |
work_keys_str_mv |
AT alaingeloen cd36inhibitorsreducepostprandialhypertriglyceridemiaandprotectagainstdiabeticdyslipidemiaandatherosclerosis AT lionelhelin cd36inhibitorsreducepostprandialhypertriglyceridemiaandprotectagainstdiabeticdyslipidemiaandatherosclerosis AT benjaminegeeraert cd36inhibitorsreducepostprandialhypertriglyceridemiaandprotectagainstdiabeticdyslipidemiaandatherosclerosis AT ericmalaud cd36inhibitorsreducepostprandialhypertriglyceridemiaandprotectagainstdiabeticdyslipidemiaandatherosclerosis AT paulholvoet cd36inhibitorsreducepostprandialhypertriglyceridemiaandprotectagainstdiabeticdyslipidemiaandatherosclerosis AT gerardmarguerie cd36inhibitorsreducepostprandialhypertriglyceridemiaandprotectagainstdiabeticdyslipidemiaandatherosclerosis |
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