Document Detail

Characterization of New Stable Ghrelin Analogs with Long-lasting Orexigenic Potency.
MedLine Citation:
PMID:  22182933     Owner:  NLM     Status:  Publisher    
Ghrelin, the only known peripherally produced and centrally acting peptide that stimulates food intake, is synthesized primarily in the stomach and acts through the growth hormone secretagogue receptor (GHS-R1a). In addition to its orexigenic effect, ghrelin stimulates the release of growth hormone (GH). In this study, we investigated the biological properties of full-length and shortened ghrelin analogs in which octanoylated Ser3 is replaced with an octanoic acid moiety coupled to diaminopropionic acid (Dpr). Ghrelin analogs stabilized with Dpr(N-octanoyl) in position 3 and non-coded amino acids in position 1 (sarcosine) and/or position 4 (naphtylalanine or cyclohexylalanine) were found to possess affinities similar to ghrelin for cell membranes with transfected GHS-R1a. In vivo, the prolonged orexigenic effect of analogs containing Dpr(N-octanoyl)3 compared to that of ghrelin in adult mice, and a similar impact on GH secretion in young mice were found. Full-length [Dpr(N-octanoyl)3]ghrelin and its analogs with a non-coded amino acid in position 1 and/or 4 showed significantly prolonged stability in blood plasma when compared to ghrelin. Ghrelin analogs with a prolonged orexigenic effect are potential treatments for GH deficiency or cachexia that accompanies chronic diseases. Desoctanoylated ghrelin analogs and N-terminal penta- and octapeptides of ghrelin did not show any biological activity.
Lenka Maletinska; Miroslava Pychova; Martina Holubova; Miroslava Blechova; Zuzana Demianova; Tomas Elbert; Blanka Zelezna
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Publication Detail:
Type:  JOURNAL ARTICLE     Date:  2011-12-19
Journal Detail:
Title:  The Journal of pharmacology and experimental therapeutics     Volume:  -     ISSN:  1521-0103     ISO Abbreviation:  -     Publication Date:  2011 Dec 
Date Detail:
Created Date:  2011-12-20     Completed Date:  -     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  0376362     Medline TA:  J Pharmacol Exp Ther     Country:  -    
Other Details:
Languages:  ENG     Pagination:  -     Citation Subset:  -    
1 Institute of Organic Chemistry and Biochemistry;
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