Characterization of New Stable Ghrelin Analogs with Prolonged Orexigenic Potency
Identifikátory výsledku
Kód výsledku v IS VaVaI
<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F61388963%3A_____%2F12%3A00376293" target="_blank" >RIV/61388963:_____/12:00376293 - isvavai.cz</a>
Výsledek na webu
<a href="http://dx.doi.org/10.1124/jpet.111.185371" target="_blank" >http://dx.doi.org/10.1124/jpet.111.185371</a>
DOI - Digital Object Identifier
<a href="http://dx.doi.org/10.1124/jpet.111.185371" target="_blank" >10.1124/jpet.111.185371</a>
Alternativní jazyky
Jazyk výsledku
angličtina
Název v původním jazyce
Characterization of New Stable Ghrelin Analogs with Prolonged Orexigenic Potency
Popis výsledku v původním jazyce
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 Ser(3) is replaced with an octanoic acid moiety coupled to diaminopropionic acid (Dpr). Ghrelin analogs stabilized with Dpr(N-octanoyl) in position 3 and noncoded amino acids in position 1 (sarcosine) and/or position 4 (naphthylalanine or cyclohexylalanine) were found to possess affinities similar to those of ghrelin for cell membranes with transfected GHS-R1a. In vivo, the prolonged orexigenic effects of analogs containing Dpr(N-octanoyl) 3 compared with that of ghrelin in adult mice and a similar impact on GH secretion in young mice were found. Full-length [Dpr(
Název v anglickém jazyce
Characterization of New Stable Ghrelin Analogs with Prolonged Orexigenic Potency
Popis výsledku anglicky
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 Ser(3) is replaced with an octanoic acid moiety coupled to diaminopropionic acid (Dpr). Ghrelin analogs stabilized with Dpr(N-octanoyl) in position 3 and noncoded amino acids in position 1 (sarcosine) and/or position 4 (naphthylalanine or cyclohexylalanine) were found to possess affinities similar to those of ghrelin for cell membranes with transfected GHS-R1a. In vivo, the prolonged orexigenic effects of analogs containing Dpr(N-octanoyl) 3 compared with that of ghrelin in adult mice and a similar impact on GH secretion in young mice were found. Full-length [Dpr(
Klasifikace
Druh
J<sub>x</sub> - Nezařazeno - Článek v odborném periodiku (Jimp, Jsc a Jost)
CEP obor
CE - Biochemie
OECD FORD obor
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Návaznosti výsledku
Projekt
<a href="/cs/project/GA303%2F09%2F0744" target="_blank" >GA303/09/0744: Vliv ghrelinu a estrogenu na metabolický syndrom u obézních myších samic</a><br>
Návaznosti
Z - Vyzkumny zamer (s odkazem do CEZ)
Ostatní
Rok uplatnění
2012
Kód důvěrnosti údajů
S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů
Údaje specifické pro druh výsledku
Název periodika
Journal of Pharmacology and Experimental Therapeutics
ISSN
0022-3565
e-ISSN
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Svazek periodika
340
Číslo periodika v rámci svazku
3
Stát vydavatele periodika
US - Spojené státy americké
Počet stran výsledku
6
Strana od-do
781-786
Kód UT WoS článku
000300619000031
EID výsledku v databázi Scopus
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