Author, as appears in the article.: Torres-Fuentes C; Pastor-Cavada E; Cano R; Kandil D; Shanahan R; Juan R; Shaban H; McGlacken GP; Schellekens H
Department: Bioquímica i Biotecnologia
URV's Author/s: Torres Fuentes, Cristina
Keywords: cachexia ghrelin ghs-r1a Agonist Anamorelin ono-7643 Bias C-3 position Cachexia Cell lung-cancer Double-blind Food-intake G-protein Ghrelin Ghs-r1a Ghs-r1a receptor Japanese patients Quinolones
Abstract: © 2018 by the authors. Licensee MDPI, Basel, Switzerland. Cachexia is a metabolic wasting disorder characterized by progressive weight loss, muscle atrophy, fatigue, weakness, and appetite loss. Cachexia is associated with almost all major chronic illnesses including cancer, heart failure, obstructive pulmonary disease, and kidney disease and significantly impedes treatment outcome and therapy tolerance, reducing physical function and increasing mortality. Current cachexia treatments are limited and new pharmacological strategies are needed. Agonists for the growth hormone secretagogue (GHS-R1a), or ghrelin receptor, prospectively regulate the central regulation of appetite and growth hormone secretion, and therefore have tremendous potential as cachexia therapeutics. Non-peptide GHS-R1a agonists are of particular interest, especially given the high gastrointestinal degradation of peptide-based structures, including that of the endogenous ligand, ghrelin, which has a half-life of only 30 min. However, few compounds have been reported in the literature as non-peptide GHS-R1a agonists. In this paper, we investigate the in vitro potential of quinolone compounds to modulate the GHS-R1a in both transfected human cells and mouse hypothalamic cells. These chemically synthesized compounds demonstrate a promising potential as GHS-R1a agonists, shown by an increased intracellular calcium influx. Further studies are now warranted to substantiate and exploit the potential of these novel quinolone-based compounds as orexigenic therapeutics in conditions of cachexia and other metabolic and eating disorders.
Thematic Areas: Astronomia / física Biochemistry & molecular biology Biodiversidade Biotecnología Catalysis Chemistry, multidisciplinary Ciência da computação Ciência de alimentos Ciências agrárias i Ciências ambientais Ciências biológicas i Ciências biológicas ii Ciências biológicas iii Computer science applications Educação física Engenharias i Engenharias ii Engenharias iv Farmacia Geociências Inorganic chemistry Interdisciplinar Materiais Medicina i Medicina ii Medicina iii Medicina veterinaria Medicine (miscellaneous) Molecular biology Nutrição Odontología Organic chemistry Physical and theoretical chemistry Psicología Química Saúde coletiva Spectroscopy Zootecnia / recursos pesqueiros
licence for use: https://creativecommons.org/licenses/by/3.0/es/
Author's mail: cristina.torres@urv.cat
ISSN: 14220067
Author identifier: 0000-0002-2917-6910
Record's date: 2023-02-19
Papper version: info:eu-repo/semantics/publishedVersion
Link to the original source: https://www.mdpi.com/1422-0067/19/6/1605
Papper original source: International Journal Of Molecular Sciences. 19 (6):
APA: Torres-Fuentes C; Pastor-Cavada E; Cano R; Kandil D; Shanahan R; Juan R; Shaban H; McGlacken GP; Schellekens H (2018). Quinolones modulate ghrelin receptor signaling: Potential for a novel small molecule scaffold in the treatment of cachexia. International Journal Of Molecular Sciences, 19(6), -. DOI: 10.3390/ijms19061605
Licence document URL: http://repositori.urv.cat/ca/proteccio-de-dades/
Article's DOI: 10.3390/ijms19061605
Entity: Universitat Rovira i Virgili
Journal publication year: 2018
Publication Type: Journal Publications
Repositori URV