| Methods for synthesis and uses of inhibitors of ghrelin O-acyltransferase inhibitors as potential therapeutic agents for obesity and diabetes. | |
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MedLine Citation:
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PMID: 20939684 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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The patent claims inhibitors of ghrelin-O-acyltransferase enzyme. These inhibitors were designed as bisubstrate analogs of the enzymatic reaction and were coupled with one of the peptides able to cross cell membranes, the 11-mer Tat peptide. The compound GO-CoA-Tat was studied in vitro and in vivo; after intraperitoneal administration, it enhances insulin response to a glucose load and leads to a statistically significant weight loss in mouse fed with a high fat diet. |
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Authors:
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Luca Costantino |
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Publication Detail:
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Type: Journal Article Date: 2010-10-12 |
Journal Detail:
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Title: Expert opinion on therapeutic patents Volume: 20 ISSN: 1744-7674 ISO Abbreviation: Expert Opin Ther Pat Publication Date: 2010 Nov |
Date Detail:
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Created Date: 2010-10-21 Completed Date: 2011-01-26 Revised Date: - |
Medline Journal Info:
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Nlm Unique ID: 9516419 Medline TA: Expert Opin Ther Pat Country: England |
Other Details:
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Languages: eng Pagination: 1603-7 Citation Subset: IM |
Affiliation:
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Dipartimento di Scienze Farmaceutiche, Università di Modena e R.E., Via Campi 183 41100 Modena, Italy. luca.costantino@unimore.it |
Export Citation:
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| MeSH Terms | |
Descriptor/Qualifier:
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Acyltransferases
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antagonists & inhibitors* Animals Diabetes Mellitus, Type 2 / drug therapy, enzymology Drug Design Enzyme Inhibitors / chemical synthesis, pharmacology* Glucose / administration & dosage Humans Insulin / metabolism Mice Obesity / drug therapy, enzymology Patents as Topic Peptides / administration & dosage, pharmacology* |
| Chemical | |
Reg. No./Substance:
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0/Enzyme Inhibitors; 0/GO-CoA-Tat; 0/Peptides; 11061-68-0/Insulin; 50-99-7/Glucose; EC 2.3.-/Acyltransferases; EC 2.3.-/ghrelin O-acyltransferase, human; EC 2.3.-/ghrelin O-acyltransferase, mouse |
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