81 articles for thisTarget
The following articles (labelled with PubMed ID or TBD) are for your review
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Article Title
Organization
New ligands of the ghrelin receptor based on the 1,2,4-triazole scaffold by introduction of a second chiral center.
University Of Montpellier
Orally active ghrelin receptor inverse agonists and their actions on a rat obesity model.
Asubio Pharma
2-Aminoalkyl nicotinamide derivatives as pure inverse agonists of the ghrelin receptor.
Asubio Pharma
New trisubstituted 1,2,4-triazoles as ghrelin receptor antagonists.
University Of Montpellier
Rational design of dual peptides targeting ghrelin and Y2 receptors to regulate food intake and body weight.
Universit£T Leipzig
Evaluation and synthesis of polar aryl- and heteroaryl spiroazetidine-piperidine acetamides as ghrelin inverse agonists.
Pfizer
Identification, optimization, and pharmacology of acylurea GHS-R1a inverse agonists.
Astrazeneca
Discovery of 2-Pyridylpyrimidines as the First Orally Bioavailable GPR39 Agonists.
Novartis Institutes For Biomedical Research
Discovery of PF-5190457, a Potent, Selective, and Orally Bioavailable Ghrelin Receptor Inverse Agonist Clinical Candidate.
Pfizer
Identification of potent, selective, CNS-targeted inverse agonists of the ghrelin receptor.
Pfizer
Antiproliferative activity on human prostate carcinoma cell lines of new peptidomimetics containing the spiroazepinoindolinone scaffold.
Universit£
Aryl sulphonyl amides as potent agonists of the growth hormone secretagogue (ghrelin) receptor.
Glaxosmithkline
Tetrahydroisoquinoline 1-carboxamides as growth hormone secretagogues.
Bristol-Myers Squibb Pharmaceutical Research Institute
Macrocycles are great cycles: applications, opportunities, and challenges of synthetic macrocycles in drug discovery.
Universite£
An aromatic region to induce a switch between agonism and inverse agonism at the ghrelin receptor.
Universit£T Leipzig
Synthesis and pharmacological evaluation of indolinone derivatives as novel ghrelin receptor antagonists.
Sanofi Research
Azapeptide analogues of the growth hormone releasing peptide 6 as cluster of differentiation 36 receptor ligands with reduced affinity for the growth hormone secretagogue receptor 1a.
Universit£
Structure and activity relationship in the (S)-N-chroman-3-ylcarboxamide series of voltage-gated sodium channel blockers.
Astrazeneca
Identification of spirocyclic piperidine-azetidine inverse agonists of the ghrelin receptor.
Pfizer
Fluorine and rhenium substituted ghrelin analogues as potential imaging probes for the growth hormone secretagogue receptor.
University Of Western Ontario
Discovery of N-(3-fluorophenyl)-1-[(4-([(3S)-3-methyl-1-piperazinyl]methyl)phenyl)acetyl]-4-piperidinamine (GSK962040), the first small molecule motilin receptor agonist clinical candidate.
Glaxosmithkline
(D)-2-tert-Butoxycarbonylamino-5,5-difluoro-5-phenyl-pentanoic acid: synthesis and incorporation into the growth hormone secretagogues.
Bristol Myers Squibb
Tetrazole based amides as growth hormone secretagogues.
Bristol-Myers Squibb Research And Development
Optimization of 1H-tetrazole-1-alkanenitriles as potent orally bioavailable growth hormone secretagogues.
Bristol-Myers Squibb Pharmaceutical Research Institute
Design and synthesis of tetrazole-based growth hormone secretagogue: the SAR studies of the O-benzyl serine side chain.
Bristol Myers Squibb
Modeling of human ghrelin receptor (hGHS-R1a) in its close state and validation by molecular docking.
Universit£
Quinazolinone derivatives as orally available ghrelin receptor antagonists for the treatment of diabetes and obesity.
Bayer Pharmaceuticals
Construction of human ghrelin receptor (hGHS-R1a) model using a fragmental prediction approach and validation through docking analysis.
Universit£
Structure-activity relationships of the oxindole growth hormone secretagogues.
Sumitomo Pharmaceuticals
2002 Alfred Burger Award Address in Medicinal Chemistry. Natural products and design: interrelated approaches in drug discovery.
Merck Research Laboratories
Spiro(indoline-3,4'-piperidine) growth hormone secretagogues as ghrelin mimetics.
Merck Research Laboratories
Modeling directed design and biological evaluation of quinazolinones as non-peptidic growth hormone secretagogues.
Merck Research Laboratories
Substituted azaquinazolinones as modulators of GHSr-1a for the treatment of type II diabetes and obesity.
Prosidion
Synthesis 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).
The Johns Hopkins University School Of Medicine
Spiroindolones, a potent compound class for the treatment of malaria.
Swiss Tropical And Public Health Institute
Identification of piperazine-bisamide GHSR antagonists for the treatment of obesity.
Amgen
The discovery and optimisation of benzazepine sulfonamide and sulfones as potent agonists of the motilin receptor.
Glaxosmithkline
Discovery and optimization of novel 4-[(aminocarbonyl)amino]-N-[4-(2-aminoethyl)phenyl]benzenesulfonamide ghrelin receptor antagonists.
Merck Research Laboratories
Triazole oxytocin antagonists: Identification of an aryloxyazetidine replacement for a biaryl substituent.
Pfizer
The discovery of biaryl carboxamides as novel small molecule agonists of the motilin receptor.
Glaxosmithkline
Discovery and optimization of (R)-prolinol-derived agonists of the Growth Hormone Secretagogue receptor (GHSR).
Bristol-Myers Squibb
Pharmacological and pharmacokinetic characterization of 2-piperazine-alpha-isopropyl benzylamine derivatives as melanocortin-4 receptor antagonists.
Neurocrine Biosciences
Identification of an efficacy switch region in the ghrelin receptor responsible for interchange between agonism and inverse agonism.
University Of Copenhagen
New trisubstituted 1,2,4-triazole derivatives as potent ghrelin receptor antagonists. 3. Synthesis and pharmacological in vitro and in vivo evaluations.
University Of Montpellier
Trisubstituted 1,2,4-triazoles as ligands for the ghrelin receptor: on the significance of the orientation and substitution at position 3.
University Of Montpellier
Design, synthesis, in vitro, and in vivo characterization of phenylpiperazines and pyridinylpiperazines as potent and selective antagonists of the melanocortin-4 receptor.
Neurocrine Biosciences
Discovery, synthesis, and structure-activity studies of tetrazole based growth hormone secretagogues.
Bristol-Myers Squibb Pharmaceutical Research Institute
Pyrrolidinones as potent functional antagonists of the human melanocortin-4 receptor.
Neurocrine Biosciences
Pyrrolidinones as orally bioavailable antagonists of the human melanocortin-4 receptor with anti-cachectic activity.
Neurocrine Biosciences
Synthesis and pharmacological in vitro and in vivo evaluations of novel triazole derivatives as ligands of the ghrelin receptor. 1.
University Of Montpellier
Optimization of 2,4-diaminopyrimidines as GHS-R antagonists: side chain exploration.
Abbott Laboratories
Synthesis and structure-activity relationships of isoxazole carboxamides as growth hormone secretagogue receptor antagonists.
Abbott Laboratories
Discovery of tetralin carboxamide growth hormone secretagogue receptor antagonists via scaffold manipulation.
Abbott Laboratories
Novel isoxazole carboxamides as growth hormone secretagogue receptor (GHS-R) antagonists.
Abbott Laboratories
Identification of structurally diverse growth hormone secretagogue agonists by virtual screening and structure-activity relationship analysis of 2-formylaminoacetamide derivatives.
Institute For Life Science Research
Parallel solid-phase synthesis of disubstituted (5-biphenyltetrazolyl) hydantoins and thiohydantoins targeting the growth hormone secretagogue receptor.
Novo Nordisk
Discovery and biological characterization of capromorelin analogues with extended half-lives.
Pfizer
Bridging computational modeling with amino acid replacements to investigate GHS-R1a-peptidomimetic recognition.
Lawson Health Research Institute
Recent progress in the discovery of ghrelin
National Institute On Alcohol Abuse And Alcoholism
Development of Nonpeptidic Inverse Agonists of the Ghrelin Receptor (GHSR) Based on the 1,2,4-Triazole Scaffold.
Univ Montpellier
Identification and Optimization of Pyrrolidine Derivatives as Highly Potent Ghrelin Receptor Full Agonists.
Astrazeneca
Identification of novel GPR81 agonist lead series for target biology evaluation.
Astrazeneca
Structure-function studies on the new growth hormone-releasing peptide, ghrelin: minimal sequence of ghrelin necessary for activation of growth hormone secretagogue receptor 1a.
Merck Research Laboratories
N-Terminal Liver-Expressed Antimicrobial Peptide 2 (LEAP2) Region Exhibits Inverse Agonist Activity toward the Ghrelin Receptor.
Universit£
Peptidomimetic growth hormone secretagogues. Design considerations and therapeutic potential.
Merck Research Laboratories
Development of a high specific activity sulfur-35-labeled sulfonamide radioligand that allowed the identification of a new growth hormone secretagogue receptor.
Merck Research Laboratories
Potent achiral agonists of the growth hormone secretagogue (ghrelin) receptor. Part 2: Lead optimisation.
Glaxosmithkline
Potent achiral agonists of the ghrelin (growth hormone secretagogue) receptor. Part I: Lead identification.
Glaxosmithkline
Rational Design, Synthesis, and Pharmacological Characterization of Novel Ghrelin Receptor Inverse Agonists as Potential Treatment against Obesity-Related Metabolic Diseases.
Sib Swiss Institute Of Bioinformatics
Identification and Pharmacological Profile of an Indane Based Series of Ghrelin Receptor Full Agonists.
Astrazeneca
