期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 25, 期 14, 页码 2800-2803出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2015.05.009
关键词
Ghrelin; Ghrelin O-acyltransferase; 1,2,3-Triazole; Serine acylation; Peptidomimetic
资金
- Foundation for Prader-Willi Research (FPWR)
- American Diabetes Association [1-13-JF-30-BR]
- Basil O'Connor Starter Scholar Award [5-FY14-81]
- March of Dimes
- National Science Foundation predoctoral fellowship [DGE-1247399]
- Syracuse University
Inhibitors of ghrelin O-acyltransferase (GOAT) have untapped potential as therapeutics targeting obesity and diabetes. We report the first examples of GOAT inhibitors incorporating a triazole linkage as a biostable isosteric replacement for the ester bond in ghrelin and amide bonds in previously reported GOAT inhibitors. These triazole-containing inhibitors exhibit sub-micromolar inhibition of the human isoform of GOAT (hGOAT), and provide a foundation for rapid future chemical diversification and optimization of hGOAT inhibitors. (C) 2015 Elsevier Ltd. All rights reserved.
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