Biased signaling: A viable strategy to drug ghrelin receptors for the treatment of obesity

Obesity is a global burden and a chronic ailment with damaging overall health effects. Ghrelin, an octanoylated 28 amino acid peptide hormone, is secreted from the oxyntic mucosa of the stomach. Ghrelin acts on regions of the hypothalamus to regulate feeding behavior and glucose homeostasis through...

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Main Author: Karim, Nagi (author)
Other Authors: Habib, Abdella M. (author)
Format: article
Published: 2021
Subjects:
Online Access:http://dx.doi.org/10.1016/j.cellsig.2021.109976
https://www.sciencedirect.com/science/article/pii/S0898656821000644
http://hdl.handle.net/10576/17969
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author Karim, Nagi
author2 Habib, Abdella M.
author2_role author
author_facet Karim, Nagi
Habib, Abdella M.
author_role author
dc.creator.none.fl_str_mv Karim, Nagi
Habib, Abdella M.
dc.date.none.fl_str_mv 2021-03-25T06:31:16Z
2021-07-31
dc.format.none.fl_str_mv application/pdf
dc.identifier.none.fl_str_mv http://dx.doi.org/10.1016/j.cellsig.2021.109976
Nagi K, Habib AM. Biased signaling: A viable strategy to drug ghrelin receptors for the treatment of obesity. Cell Signal. 2021 Mar 10;83:109976. doi: 10.1016/j.cellsig.2021.109976.
08986568
https://www.sciencedirect.com/science/article/pii/S0898656821000644
http://hdl.handle.net/10576/17969
83
dc.language.none.fl_str_mv en
dc.publisher.none.fl_str_mv Elsevier
dc.rights.none.fl_str_mv http://creativecommons.org/licenses/by/4.0/
info:eu-repo/semantics/openAccess
dc.subject.none.fl_str_mv Bias
Ghrelin
Biased agonism
Obesity
Dimer
Functional selectivity
dc.title.none.fl_str_mv Biased signaling: A viable strategy to drug ghrelin receptors for the treatment of obesity
dc.type.none.fl_str_mv Article
info:eu-repo/semantics/publishedVersion
info:eu-repo/semantics/article
description Obesity is a global burden and a chronic ailment with damaging overall health effects. Ghrelin, an octanoylated 28 amino acid peptide hormone, is secreted from the oxyntic mucosa of the stomach. Ghrelin acts on regions of the hypothalamus to regulate feeding behavior and glucose homeostasis through its G protein-coupled receptor. Recently, several central pathways modulating the metabolic actions of ghrelin have been reported. While these signaling pathways can be inhibited or activated by antagonists or agonists, they can also be discriminatingly activated in a “biased” response to impart different degrees of activation in distinct pathways downstream of the receptor. Here, we review recent ghrelin biased signaling findings as well as characteristics of ghrelin hormone and its receptors pertinent for biased signaling. We then evaluate the feasibility for ghrelin receptor biased signaling as a strategy for the development of effective pharmacotherapy in obesity treatment.
eu_rights_str_mv openAccess
format article
id qu_93a5751d4cd7f78d0837f690c7e1c8cc
identifier_str_mv Nagi K, Habib AM. Biased signaling: A viable strategy to drug ghrelin receptors for the treatment of obesity. Cell Signal. 2021 Mar 10;83:109976. doi: 10.1016/j.cellsig.2021.109976.
08986568
83
language_invalid_str_mv en
network_acronym_str qu
network_name_str Qatar University repository
oai_identifier_str oai:qspace.qu.edu.qa:10576/17969
publishDate 2021
publisher.none.fl_str_mv Elsevier
repository.mail.fl_str_mv
repository.name.fl_str_mv
repository_id_str
rights_invalid_str_mv http://creativecommons.org/licenses/by/4.0/
spelling Biased signaling: A viable strategy to drug ghrelin receptors for the treatment of obesityKarim, NagiHabib, Abdella M.BiasGhrelinBiased agonismObesityDimerFunctional selectivityObesity is a global burden and a chronic ailment with damaging overall health effects. Ghrelin, an octanoylated 28 amino acid peptide hormone, is secreted from the oxyntic mucosa of the stomach. Ghrelin acts on regions of the hypothalamus to regulate feeding behavior and glucose homeostasis through its G protein-coupled receptor. Recently, several central pathways modulating the metabolic actions of ghrelin have been reported. While these signaling pathways can be inhibited or activated by antagonists or agonists, they can also be discriminatingly activated in a “biased” response to impart different degrees of activation in distinct pathways downstream of the receptor. Here, we review recent ghrelin biased signaling findings as well as characteristics of ghrelin hormone and its receptors pertinent for biased signaling. We then evaluate the feasibility for ghrelin receptor biased signaling as a strategy for the development of effective pharmacotherapy in obesity treatment.Elsevier2021-03-25T06:31:16Z2021-07-31Articleinfo:eu-repo/semantics/publishedVersioninfo:eu-repo/semantics/articleapplication/pdfhttp://dx.doi.org/10.1016/j.cellsig.2021.109976Nagi K, Habib AM. Biased signaling: A viable strategy to drug ghrelin receptors for the treatment of obesity. Cell Signal. 2021 Mar 10;83:109976. doi: 10.1016/j.cellsig.2021.109976.08986568https://www.sciencedirect.com/science/article/pii/S0898656821000644http://hdl.handle.net/10576/1796983enhttp://creativecommons.org/licenses/by/4.0/info:eu-repo/semantics/openAccessoai:qspace.qu.edu.qa:10576/179692024-07-23T11:23:31Z
spellingShingle Biased signaling: A viable strategy to drug ghrelin receptors for the treatment of obesity
Karim, Nagi
Bias
Ghrelin
Biased agonism
Obesity
Dimer
Functional selectivity
status_str publishedVersion
title Biased signaling: A viable strategy to drug ghrelin receptors for the treatment of obesity
title_full Biased signaling: A viable strategy to drug ghrelin receptors for the treatment of obesity
title_fullStr Biased signaling: A viable strategy to drug ghrelin receptors for the treatment of obesity
title_full_unstemmed Biased signaling: A viable strategy to drug ghrelin receptors for the treatment of obesity
title_short Biased signaling: A viable strategy to drug ghrelin receptors for the treatment of obesity
title_sort Biased signaling: A viable strategy to drug ghrelin receptors for the treatment of obesity
topic Bias
Ghrelin
Biased agonism
Obesity
Dimer
Functional selectivity
url http://dx.doi.org/10.1016/j.cellsig.2021.109976
https://www.sciencedirect.com/science/article/pii/S0898656821000644
http://hdl.handle.net/10576/17969