| Characterization of New Stable Ghrelin Analogs with Long-lasting Orexigenic Potency. | |
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MedLine Citation:
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PMID: 22182933 Owner: NLM Status: Publisher |
Abstract/OtherAbstract:
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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. |
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Authors:
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Lenka Maletinska; Miroslava Pychova; Martina Holubova; Miroslava Blechova; Zuzana Demianova; Tomas Elbert; Blanka Zelezna |
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Publication Detail:
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Type: JOURNAL ARTICLE Date: 2011-12-19 |
Journal Detail:
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Title: The Journal of pharmacology and experimental therapeutics Volume: - ISSN: 1521-0103 ISO Abbreviation: - Publication Date: 2011 Dec |
Date Detail:
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Created Date: 2011-12-20 Completed Date: - Revised Date: - |
Medline Journal Info:
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Nlm Unique ID: 0376362 Medline TA: J Pharmacol Exp Ther Country: - |
Other Details:
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Languages: ENG Pagination: - Citation Subset: - |
Affiliation:
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1 Institute of Organic Chemistry and Biochemistry; |
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From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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