| Adipose tissue-targeted 11β-hydroxysteroid dehydrogenase type 1 inhibitor protects against diet-induced obesity. | |
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MedLine Citation:
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PMID: 21325744 Owner: NLM Status: Publisher |
Abstract/OtherAbstract:
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Current pharmacological treatments for obesity and metabolic syndrome have various limitations. Recently, adipose tissue 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) has been proposed as a novel therapeutic target for the treatment of obesity and metabolic syndrome. Nevertheless, there is no adipose tissue-targeted 11β-HSD1 inhibitor available now. We sought to develop a new 11β-HSD1 pharmacological inhibitor that homes specifically to the white adipose tissue and aimed to investigate whether adipose tissue-targeted 11β-HSD1 inhibitor might decrease body weight gain and improve glucose tolerance in diet-induced obesity mice. BVT.2733, an 11β-HSD1 selective inhibitor was connected with a peptide CKGGRAKDC that homes to white fat vasculature. CKGGRAKDC-BVT.2733 (T-BVT) or an equimolar mixture of CKGGRAKDC and BVT.2733 (NT-BVT) was given to diet-induced obesity mice for two weeks through subcutaneous injection. T-BVT decreased body weight gain, improved glucose tolerance and decreased adipocyte size compared with vehicle treated mice. In adipose tissue T-BVT administration significantly increased adiponectin, vaspin mRNA levels; In liver T-BVT administration decreased the mRNA level of phosphoenolpyruvate carboxykinase (PEPCK), increased the mRNA levels of mitochondrial carnitine palmi-toyltransferase-I (mCPT-I) and peroxisome proliferator-activated receptor α (PPARα). No significant differences in adipocyte size and hepatic gene expression were observed after treatment with NT-BVT compared with vehicle treated mice, though NT-BVT also decreased body weight gain, improved glucose tolerance, and increased uncoupling protein-2 (UCP-2) mRNA levels in muscle. These results suggest that an adipose tissue-targeted pharmacological inhibitor of 11β-HSD1 may prove to be a new approach for the treatment of obesity and metabolic syndrome. |
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Authors:
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Juan Liu; Long Wang; Aisen Zhang; Wenjuan Di; Xiao Zhang; Lin Wu; Jing Yu; Juanmin Zha; Shan Lv; Peng Cheng; Miao Hu; Yujie Li; Hanmei Qi; Guoxian Ding; Yi Zhong |
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Publication Detail:
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Type: JOURNAL ARTICLE Date: 2011-2-17 |
Journal Detail:
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Title: Endocrine journal Volume: - ISSN: 1348-4540 ISO Abbreviation: - Publication Date: 2011 Feb |
Date Detail:
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Created Date: 2011-2-17 Completed Date: - Revised Date: - |
Medline Journal Info:
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Nlm Unique ID: 9313485 Medline TA: Endocr J Country: - |
Other Details:
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Languages: ENG Pagination: - Citation Subset: - |
Affiliation:
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Department of Geratology, the First Hospital Affiliated to Nanjing Medical University, Nanjing, P.R.China. |
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From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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