Quinazolinone derivatives as orally available ghrelin receptor antagonists for the treatment of diabetes and obesity.
about
The role of ghrelin in reward-based eatingGSK1614343, a novel ghrelin receptor antagonist, produces an unexpected increase of food intake and body weight in rodents and dogs.Obesity treatment: novel peripheral targets.Therapeutic Potential of Targeting the Ghrelin Pathway.Integrating GHS into the Ghrelin System.In vitro selection of a peptide antagonist of growth hormone secretagogue receptor using cDNA display.Altered ghrelin secretion in mice in response to diet-induced obesity and Roux-en-Y gastric bypass.Pharmacological characterization of the first in class clinical candidate PF-05190457: a selective ghrelin receptor competitive antagonist with inverse agonism that increases vagal afferent firing and glucose-dependent insulin secretion ex vivo.Catalytic antibody degradation of ghrelin increases whole-body metabolic rate and reduces refeeding in fasting miceConstitutive activation of G protein-coupled receptors and diseases: insights into mechanisms of activation and therapeutics.Functionally biased signalling properties of 7TM receptors - opportunities for drug development for the ghrelin receptor.From Belly to Brain: Targeting the Ghrelin Receptor in Appetite and Food Intake Regulation.Growth hormone secretagogue receptor deficiency in mice protects against obesity-induced hypertension.Current and potential roles of ghrelin in clinical practice.Ghrelin receptor modulators and their therapeutic potential.MC4R dimerization in the paraventricular nucleus and GHSR/MC3R heterodimerization in the arcuate nucleus: is there relevance for body weight regulation?Ghrelin receptor modulators: a patent review (2011 - 2014).Advances in metal-catalyzed cross-coupling reactions of halogenated quinazolinones and their quinazoline derivatives.Molecular modeling, enzyme activity, anti-inflammatory and antiarthritic activities of newly synthesized quinazoline derivatives.Development of Fluorinated Non-Peptidic Ghrelin Receptor Ligands for Potential Use in Molecular Imaging.Approved and Off-Label Uses of Obesity Medications, and Potential New Pharmacologic Treatment Options.Ghrelin increases the rewarding value of high-fat diet in an orexin-dependent manner.Recent advances in potential clinical application of ghrelin in obesity.Disruption of cue-potentiated feeding in mice with blocked ghrelin signaling.Characterization of the insulin sensitivity of ghrelin receptor KO mice using glycemic clampsSynthesis and in vivo evaluation of (S)-6-(4-fluorophenoxy)-3-((1-[11C]methylpiperidin-3-yl)methyl)-2-o-tolylquinazolin-4(3H)-one, a potential PET tracer for growth hormone secretagogue receptor (GHSR).Evaluation and synthesis of polar aryl- and heteroaryl spiroazetidine-piperidine acetamides as ghrelin inverse agonists.Synthesis and Photophysical Properties of Polycarbo-Substituted Quinazolines Derived from the 2-Aryl-4-chloro-6-iodoquinazolines.Long-term treatment with the ghrelin receptor antagonist [d-Lys3]-GHRP-6 does not improve glucose homeostasis in nonobese diabetic MKR mice.Synthesis, Anti-microbial and Molecular Docking Studies of Quinazolin-4(3H)-one Derivatives
P2860
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P2860
Quinazolinone derivatives as orally available ghrelin receptor antagonists for the treatment of diabetes and obesity.
description
2007 nî lūn-bûn
@nan
2007年の論文
@ja
2007年学术文章
@wuu
2007年学术文章
@zh
2007年学术文章
@zh-cn
2007年学术文章
@zh-hans
2007年学术文章
@zh-my
2007年学术文章
@zh-sg
2007年學術文章
@yue
2007年學術文章
@zh-hant
name
Quinazolinone derivatives as o ...... tment of diabetes and obesity.
@en
Quinazolinone derivatives as o ...... tment of diabetes and obesity.
@nl
type
label
Quinazolinone derivatives as o ...... tment of diabetes and obesity.
@en
Quinazolinone derivatives as o ...... tment of diabetes and obesity.
@nl
prefLabel
Quinazolinone derivatives as o ...... tment of diabetes and obesity.
@en
Quinazolinone derivatives as o ...... tment of diabetes and obesity.
@nl
P2093
P356
P1476
Quinazolinone derivatives as o ...... tment of diabetes and obesity.
@en
P2093
Alexandros Vakalopoulos
Andrea C McClure
Astrid A Ortiz
Brian T Bloomquist
Chih-Yuan Chuang
Derek B Lowe
Donald E Bierer
Georgiy Bondar
James A Kristie
James N Livingston
P304
P356
10.1021/JM070071+
P407
P577
2007-09-21T00:00:00Z