A novel non-peptidic agonist of the ghrelin receptor with orexigenic activity in vivo

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dc.contributor.author Pastor-Cavada, Elena
dc.contributor.author Pardo, Leticia M.
dc.contributor.author Kandil, Dalia
dc.contributor.author Torres-Fuentes, Cristina
dc.contributor.author Clarke, Sarah L.
dc.contributor.author Shaban, Hamdy
dc.contributor.author McGlacken, Gerard P.
dc.contributor.author Schellekens, Harriët
dc.date.accessioned 2016-12-12T17:24:16Z
dc.date.available 2016-12-12T17:24:16Z
dc.date.issued 2016-11-07
dc.identifier.citation Pastor-Cavada, E., Pardo, L. M., Kandil, D., Torres-Fuentes, C., Clarke, S. L., Shaban, H., McGlacken, G. P. and Schellekens, H. (2016) 'A novel non-peptidic agonist of the ghrelin receptor with orexigenic activity in vivo', Scientific Reports, 6, 36456 (13pp). doi:10.1038/srep36456 en
dc.identifier.volume 6 en
dc.identifier.startpage 1 en
dc.identifier.endpage 13 en
dc.identifier.issn 2045-2322
dc.identifier.uri http://hdl.handle.net/10468/3370
dc.identifier.doi 10.1038/srep36456
dc.description.abstract Loss of appetite in the medically ill and ageing populations is a major health problem and a significant symptom in cachexia syndromes, which is the loss of muscle and fat mass. Ghrelin is a gut-derived hormone which can stimulate appetite. Herein we describe a novel, simple, non-peptidic, 2-pyridone which acts as a selective agonist for the ghrelin receptor (GHS-R1a). The small 2-pyridone demonstrated clear agonistic activity in both transfected human cells and mouse hypothalamic cells with endogenous GHS-R1a receptor expression. In vivo tests with the hit compound showed significant increased food intake following peripheral administration, which highlights the potent orexigenic effect of this novel GHS-R1a receptor ligand. en
dc.description.sponsorship Science Foundation Ireland (SFI/12/IP/1315 and SFI/12/RC/2275); Irish Research Council for Science and Technology and Pfizer Process Development Centre, Cork (Enterprise Partnership Scheme) en
dc.format.mimetype application/pdf en
dc.language.iso en en
dc.publisher Nature Publishing Group en
dc.rights © 2016, the Authors. This work is licensed under a Creative Commons Attribution 4.0 International License. The images or other third party material in this article are included in the article’s Creative Commons license, unless indicated otherwise in the credit line; if the material is not included under the Creative Commons license, users will need to obtain permission from the license holder to reproduce the material. To view a copy of this license, visit http://creativecommons.org/licenses/by/4.0/ en
dc.rights.uri http://creativecommons.org/licenses/by/4.0/ en
dc.subject Growth hormone secretagogue en
dc.subject Food intake en
dc.subject Medicinal chemistry en
dc.subject Older adults en
dc.subject Mechanisms en
dc.subject Secretion en
dc.subject Fluorine en
dc.subject Peptide en
dc.subject Healthy en
dc.subject Anorexia-cachexia en
dc.title A novel non-peptidic agonist of the ghrelin receptor with orexigenic activity in vivo en
dc.type Article (peer-reviewed) en
dc.internal.authorcontactother Harriet Schellekens, Biosciences Institute, University College Cork, Cork, Ireland. +353-21-490-3000 Email: h.schellekens@ucc.ie en
dc.internal.availability Full text available en
dc.date.updated 2016-12-09T12:52:42Z
dc.description.version Published Version en
dc.internal.rssid 375019510
dc.internal.wokid WOS:000387038400001
dc.contributor.funder Science Foundation Ireland en
dc.contributor.funder Irish Research Council for Science, Engineering and Technology en
dc.contributor.funder Universidad de Sevilla en
dc.contributor.funder Pfizer Process Development Centre, Cork
dc.description.status Peer reviewed en
dc.identifier.journaltitle Scientific Reports en
dc.internal.copyrightchecked Yes en
dc.internal.licenseacceptance Yes en
dc.internal.IRISemailaddress H.Schellekens@ucc.ie en
dc.identifier.articleid 36456


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© 2016, the Authors. This work is licensed under a Creative Commons Attribution 4.0 International License. The images or other third party material in this article are included in the article’s Creative Commons license, unless indicated otherwise in the credit line; if the material is not included under the Creative Commons license, users will need to obtain permission from the license holder to reproduce the material. To view a copy of this license, visit http://creativecommons.org/licenses/by/4.0/ Except where otherwise noted, this item's license is described as © 2016, the Authors. This work is licensed under a Creative Commons Attribution 4.0 International License. The images or other third party material in this article are included in the article’s Creative Commons license, unless indicated otherwise in the credit line; if the material is not included under the Creative Commons license, users will need to obtain permission from the license holder to reproduce the material. To view a copy of this license, visit http://creativecommons.org/licenses/by/4.0/
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