From belly to brain: targeting the ghrelin receptor in appetite and food intake regulation

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dc.contributor.author Howick, Kenneth P.
dc.contributor.author Griffin, Brendan T.
dc.contributor.author Cryan, John F.
dc.contributor.author Schellekens, Harriët
dc.date.accessioned 2017-01-31T15:52:03Z
dc.date.available 2017-01-31T15:52:03Z
dc.date.issued 2017-01-27
dc.identifier.citation Howick, K., Griffin, B., Cryan, J. and Schellekens, H. (2017) 'From Belly to Brain: Targeting the Ghrelin Receptor in Appetite and Food Intake Regulation', International Journal of Molecular Sciences, 18(2), 273. doi:10.3390/ijms18020273 en
dc.identifier.volume 18 en
dc.identifier.issued 2 en
dc.identifier.startpage 273-1 en
dc.identifier.endpage 273-38 en
dc.identifier.issn 1422-0067
dc.identifier.uri http://hdl.handle.net/10468/3546
dc.identifier.doi 10.3390/ijms18020273
dc.description.abstract Ghrelin is the only known peripherally-derived orexigenic hormone, increasing appetite and subsequent food intake. The ghrelinergic system has therefore received considerable attention as a therapeutic target to reduce appetite in obesity as well as to stimulate food intake in conditions of anorexia, malnutrition and cachexia. As the therapeutic potential of targeting this hormone becomes clearer, it is apparent that its pleiotropic actions span both the central nervous system and peripheral organs. Despite a wealth of research, a therapeutic compound specifically targeting the ghrelin system for appetite modulation remains elusive although some promising effects on metabolic function are emerging. This is due to many factors, ranging from the complexity of the ghrelin receptor (Growth Hormone Secretagogue Receptor, GHSR-1a) internalisation and heterodimerization, to biased ligand interactions and compensatory neuroendocrine outputs. Not least is the ubiquitous expression of the GHSR-1a, which makes it impossible to modulate centrallymediated appetite regulation without encroaching on the various peripheral functions attributable to ghrelin. It is becoming clear that ghrelin’s central signalling is critical for its effects on appetite, body weight regulation and incentive salience of food. Improving the ability of ghrelin ligands to penetrate the blood brain barrier would enhance central delivery to GHSR-1a expressing brain regions, particularly within the mesolimbic reward circuitry. en
dc.format.mimetype application/pdf en
dc.language.iso en en
dc.publisher MDPI en
dc.rights © 2017 by the authors; licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (http://creativecommons.org/licenses/by/4.0/). en
dc.rights.uri http://creativecommons.org/licenses/by/4.0/ en
dc.subject Ghrelin en
dc.subject Desacyl-ghrelin en
dc.subject Appetite en
dc.subject GHSR-1a en
dc.subject Obesity en
dc.subject Cachexia en
dc.subject Food reward en
dc.subject Mesolimbic reward circuitry en
dc.subject Blood brain barrier en
dc.title From belly to brain: targeting the ghrelin receptor in appetite and food intake regulation en
dc.type Article (peer-reviewed) en
dc.internal.authorcontactother Brendan Griffin, School Of Pharmacy, University College Cork, Cork, Ireland. +353-21-490-3000 Email: brendan.griffin@ucc.ie en
dc.internal.availability Full text available en
dc.date.updated 2017-01-31T15:44:35Z
dc.description.version Published Version en
dc.internal.rssid 381764255
dc.description.status Peer reviewed en
dc.identifier.journaltitle International Journal of Molecular Sciences en
dc.internal.copyrightchecked No !!CORA!! en
dc.internal.licenseacceptance Yes en
dc.internal.IRISemailaddress brendan.griffin@ucc.ie en


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© 2017 by the authors; licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (http://creativecommons.org/licenses/by/4.0/). Except where otherwise noted, this item's license is described as © 2017 by the authors; licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (http://creativecommons.org/licenses/by/4.0/).
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