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Livres
Articles (38)
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Mechanisms of peptide and nonpeptide ligand binding to Class B G-protein-coupled receptors

Sam R.J. Hoare

Journal:

Drug Discovery Today

Année:

2005

Langue:

english

Fichier:

PDF, 459 KB

english, 2005

Receptor binding kinetics equations: Derivation using the Laplace transform method

Hoare, Sam R.J.

Journal:

Journal of Pharmacological and Toxicological Methods

Année:

2017

Langue:

english

Fichier:

PDF, 778 KB

english, 2017

Diet and Mental Health During Emerging Adulthood: A Systematic Review

Collins, Sam, Dash, Sarah, Allender, Steven, Jacka, Felice, Hoare, Erin

Journal:

Emerging Adulthood

Année:

2020

Fichier:

PDF, 476 KB

2020

Pharmacological and pharmacokinetic characterization of 2-piperazine-α-isopropyl benzylamine derivatives as melanocortin-4 receptor antagonists

Chen Chen, Fabio C. Tucci, Wanlong Jiang, Joe A. Tran, Beth A. Fleck, Sam R. Hoare, Jenny Wen, Takung Chen, Michael Johns, Stacy Markison, Alan C. Foster, Dragan Marinkovic, Caroline W. Chen, Melissa

Journal:

Bioorganic & Medicinal Chemistry

Année:

2008

Langue:

english

Fichier:

PDF, 328 KB

english, 2008

Pyrrolidinones as potent functional antagonists of the human melanocortin-4 receptor

Wanlong Jiang, Fabio C. Tucci, Joe A. Tran, Beth A. Fleck, Jenny Wen, Stacy Markison, Dragan Marinkovic, Caroline W. Chen, Melissa Arellano, Sam R. Hoare, Michael Johns, Alan C. Foster, John Saunders,

Journal:

Bioorganic & Medicinal Chemistry Letters

Année:

2007

Langue:

english

Fichier:

PDF, 129 KB

english, 2007

Synthesis and characterization of pyrrolidine derivatives as potent agonists of the human melanocortin-4 receptor

Wanlong Jiang, Joe A. Tran, Fabio C. Tucci, Beth A. Fleck, Sam R. Hoare, Stacy Markison, Jenny Wen, Caroline W. Chen, Dragan Marinkovic, Melissa Arellano, Alan C. Foster, Chen Chen

Journal:

Bioorganic & Medicinal Chemistry Letters

Année:

2007

Langue:

english

Fichier:

PDF, 265 KB

english, 2007

Identification and characterization of pyrrolidine diastereoisomers as potent functional agonists and antagonists of the human melanocortin-4 receptor

Chen Chen, Wanlong Jiang, Joe A. Tran, Fabio C. Tucci, Beth A. Fleck, Stacy Markison, Jenny Wen, Ajay Madan, Sam R. Hoare, Alan C. Foster, Dragan Marinkovic, Caroline W. Chen, Melissa Arellano, John S

Journal:

Bioorganic & Medicinal Chemistry Letters

Année:

2008

Langue:

english

Fichier:

PDF, 199 KB

english, 2008

Discovery of NBI-77860/GSK561679, a potent corticotropin-releasing factor (CRF1) receptor antagonist with improved pharmacokinetic properties

John E. Tellew, Marion Lanier, Manisha Moorjani, Emily Lin, Zhiyong Luo, Deborah H. Slee, Xiaohu Zhang, Sam R.J. Hoare, Dimitri E. Grigoriadis, Yves St. Denis, Romano Di Fabio, Enza Di Modugno, John S

Journal:

Bioorganic & Medicinal Chemistry Letters

Année:

2010

Langue:

english

Fichier:

PDF, 1.76 MB

english, 2010

A potent and selective nonpeptide antagonist of the melanocortin-4 receptor induces food intake in satiated mice

Joseph Pontillo, Joseph A. Tran, Stacy Markison, Margaret Joppa, Beth A. Fleck, Dragan Marinkovic, Melissa Arellano, Fabio C. Tucci, Marion Lanier, Jodie Nelson, John Saunders, Sam R.J. Hoare, Alan C.

Journal:

Bioorganic & Medicinal Chemistry Letters

Année:

2005

Langue:

english

Fichier:

PDF, 152 KB

english, 2005

The Discrepancy Between the Binding Affinity of PTH (1–34) and RS 66271 is Explained by Interaction of the PTH/PTHrP Receptor With G-Protein

Sam R. J. Hoare, Ted B. Usdin

Journal:

Journal of Bone and Mineral Research

Année:

2000

Langue:

english

Fichier:

PDF, 44 KB

english, 2000

Single amino acid residue determinants of non-peptide antagonist binding to the corticotropin-releasing factor1 (CRF1) receptor

Sam R.J. Hoare, Brock T. Brown, Mark A. Santos, Siobhan Malany, Stephen F. Betz, Dimitri E. Grigoriadis

Journal:

Biochemical Pharmacology

Année:

2006

Langue:

english

Fichier:

PDF, 676 KB

english, 2006

Kinetics of nonpeptide antagonist binding to the human gonadotropin-releasing hormone receptor: Implications for structure–activity relationships and insurmountable antagonism

Susan K. Sullivan, Sam R.J. Hoare, Beth A. Fleck, Yun-Fei Zhu, Christopher E. Heise, R. Scott Struthers, Paul D. Crowe

Journal:

Biochemical Pharmacology

Année:

2006

Langue:

english

Fichier:

PDF, 655 KB

english, 2006

Quantitative cell membrane-based radioligand binding assays for parathyroid hormone receptors

Sam R.J Hoare, Ted B Usdin

Journal:

Journal of Pharmacological and Toxicological Methods

Année:

1999

Langue:

english

Fichier:

PDF, 149 KB

english, 1999

Conformational states of the corticotropin releasing factor 1 (CRF1) receptor: detection, and pharmacological evaluation by peptide ligands

Sam R.J Hoare, Susan K Sullivan, Anil Pahuja, Nicholas Ling, Paul D Crowe, Dimitri E Grigoriadis

Journal:

Peptides

Année:

2003

Langue:

english

Fichier:

PDF, 296 KB

english, 2003

Peptide ligand binding properties of the corticotropin-releasing factor (CRF) type 2 receptor: pharmacology of endogenously expressed receptors, G-protein-coupling sensitivity and determinants of CRF2 receptor selectivity

Sam R.J. Hoare, Susan K. Sullivan, Jun Fan, Khamkeo Khongsaly, Dimitri E. Grigoriadis

Journal:

Peptides

Année:

2005

Langue:

english

Fichier:

PDF, 553 KB

english, 2005

G-protein-coupled receptors: what limits high-affinity agonist binding?

Sam R.J Hoare

Journal:

Trends in Pharmacological Sciences

Année:

2000

Langue:

english

Fichier:

PDF, 63 KB

english, 2000

Specificity and stability of a new PTH1 receptor antagonist, mouse TIP(7–39)

Sam R.J Hoare, Ted B Usdin

Journal:

Peptides

Année:

2002

Langue:

english

Fichier:

PDF, 219 KB

english, 2002

Bioconcentration of triclosan and methyl-triclosan in marine mussels (Mytilus galloprovincialis) under laboratory conditions and in metropolitan waters of Gulf St Vincent, South Australia

Kookana, Rai S., Shareef, Ali, Fernandes, Milena B., Hoare, Sonja, Gaylard, Sam, Kumar, Anu

Journal:

Marine Pollution Bulletin

Année:

2013

Langue:

english

Fichier:

PDF, 691 KB

english, 2013

Phenylguanidines as Selective Nonpeptide Melanocortin-5 Receptor Antagonists

Chen,, Yu, Jinghua, Fleck, Beth A., Hoare, Sam R. J., Saunders, John, Foster, Alan C.

Journal:

Journal of Medicinal Chemistry

Année:

2004

Langue:

english

Fichier:

PDF, 86 KB

english, 2004

Ligand Affinity for Amino-Terminal and Juxtamembrane Domains of the Corticotropin Releasing Factor Type I Receptor: Regulation by G-Protein and Nonpeptide Antagonists

Hoare, Sam R. J., Sullivan, Sue K., Schwarz, David A., Ling, Nicholas, Vale, Wylie W., Crowe, Paul D., Grigoriadis, Dimitri E.

Journal:

Biochemistry

Année:

2004

Langue:

english

Fichier:

PDF, 268 KB

english, 2004

Design, Synthesis, In Vitro, and In Vivo Characterization of Phenylpiperazines and Pyridinylpiperazines as Potent and Selective Antagonists of the Melanocortin-4 Receptor

Tran, Joe A., Jiang, Wanlong, Tucci, Fabio C., Fleck, Beth A., Wen, Jenny, Sai, Yang, Madan, Ajay, Chen, Ta Kung, Markison, Stacy, Foster, Alan C., Hoare, Sam R., Marks, Daniel, Harman, John, Chen, Ca

Journal:

Journal of Medicinal Chemistry

Année:

2007

Langue:

english

Fichier:

PDF, 438 KB

english, 2007

Discovery of 1-{2-[(1 S )-(3-Dimethylamino-propionyl)amino-2-methylpropyl]-4-methyl-phenyl}-4-[(2 R )-methyl-3-(4-chlorophenyl)-propionyl]piperazine as an Orally Active Antagonist of the Melanocortin-4 Receptor for the Potential Treatment of Cachexia

Chen,, Jiang, Wanlong, Tucci, Fabio, Tran, Joe A., Fleck, Beth A., Hoare, Sam R., Joppa, Margaret, Markison, Stacy, Wen, Jenny, Sai, Yang, Johns, Michael, Madan, Ajay, Chen, Takung, Chen, Caroline W.

Journal:

Journal of Medicinal Chemistry

Année:

2007

Langue:

english

Fichier:

PDF, 67 KB

english, 2007

Molecular Interactions of Nonpeptide Agonists and Antagonists with the Melanocortin-4 Receptor

Fleck, Beth A., Chen,, Yang, Weidong, Huntley, Rajesh, Markison, Stacy, Nickolls, Sarah A., Foster, Alan C., Hoare, Sam R. J.

Journal:

Biochemistry

Année:

2005

Langue:

english

Fichier:

PDF, 381 KB

english, 2005

The distribution of triclosan and methyl-triclosan in marine sediments of Barker Inlet, South Australia

Fernandes, Milena, Shareef, Ali, Kookana, Rai, Gaylard, Sam, Hoare, Sonja, Kildea, Tim

Journal:

Journal of Environmental Monitoring

Année:

2011

Langue:

english

Fichier:

PDF, 197 KB

english, 2011

Analytical method for simultaneously measuring ex vivo drug receptor occupancy and dissociation rate: Application to (R)-dimethindene occupancy of central histamine H 1 receptors

Malany, Siobhan, Hernandez, Lisa M., Smith, William F., Crowe, Paul D., Hoare, Sam R. J.

Journal:

Journal of Receptor and Signal Transduction Research

Année:

2009

Langue:

english

Fichier:

PDF, 979 KB

english, 2009

Allosteric Modulators of Class B G-Protein-Coupled Receptors

Hoare, Sam

Journal:

Current Neuropharmacology

Année:

2007

Langue:

english

Fichier:

PDF, 536 KB

english, 2007

Evaluating the Ligand Specificity of Zebrafish Parathyroid Hormone (PTH) Receptors: Comparison of PTH, PTH-Related Protein, and Tuberoinfundibular Peptide of 39 Residues

Hoare, Sam R. J., Rubin, David A., Jüppner, Harald, Usdin, Ted B.

Journal:

Endocrinology

Année:

2000

Langue:

english

Fichier:

PDF, 168 KB

english, 2000

The Regulation of Feeding and Metabolic Rate and the Prevention of Murine Cancer Cachexia with a Small-Molecule Melanocortin-4 Receptor Antagonist

Markison, Stacy, Foster, Alan C., Chen, Chen, Brookhart, Gregor B., Hesse, Amy, Hoare, Sam R. J., Fleck, Beth A., Brown, Brock T., Marks, Daniel L.

Journal:

Endocrinology

Année:

2005

Langue:

english

Fichier:

PDF, 243 KB

english, 2005

Pharmacologic Characterization of Valbenazine (NBI-98854) and Its Metabolites

Grigoriadis, Dimitri E., Smith, Evan, Hoare, Sam R.J., Madan, Ajay, Bozigian, Haig

Journal:

Journal of Pharmacology and Experimental Therapeutics

Année:

2017

Langue:

english

Fichier:

PDF, 665 KB

english, 2017

666. VMAT2 Inhibition: A Novel Mechanism for Maintained Efficacy at Lowered Antipsychotic Doses

Grigoriadis, Dimitri, Hoare, Sam, Kudwa, Andrea, Boikess, Steve

Journal:

Biological Psychiatry

Année:

2017

Langue:

english

Fichier:

PDF, 59 KB

english, 2017

664. Selectivity of Valbenazine (NBI-98854) and Its Major Metabolites on Presynaptic Monoamine Transport

Harriott, Nicole, Hoare, Sam, Grigoriadis, Dimitri

Journal:

Biological Psychiatry

Année:

2017

Langue:

english

Fichier:

PDF, 43 KB

english, 2017

Sa1207 - Prospective Observational Cohort Study of Rapid Ionization Mass Spectrometry (Reims) for Near-Real Time Diagnosis and Stratification of Colorectal Cancer

Mason, Sam, Alexander, James L., White, Emma, Bodai, Zsolt, Manoli, Eftychios, Paizs, Petra, Scott, Alasdair, Adebesin, Afeez, Hoare, Jonathan, Goldin, Robert, Darzi, Ara, Takats, Zoltan, Kinross, Jam

Journal:

Gastroenterology

Année:

2018

Langue:

english

Fichier:

PDF, 1.02 MB

english, 2018

The importance of target binding kinetics for measuring target binding affinity in drug discovery: a case study from a CRF1 receptor antagonist program

Hoare, Sam R.J., Fleck, Beth A., Williams, John P., Grigoriadis, Dimitri E.

Journal:

Drug Discovery Today

Année:

2019

Langue:

english

Fichier:

PDF, 614 KB

english, 2019

The importance of target binding kinetics for measuring target binding affinity in drug discovery: a case study from a CRF1 receptor antagonist program

Hoare, Sam R.J., Fleck, Beth A., Williams, John P., Grigoriadis, Dimitri E.

Journal:

Drug Discovery Today

Année:

2019

Fichier:

PDF, 614 KB

2019

A kinetic method for measuring agonist efficacy and ligand bias using high resolution biosensors and a kinetic data analysis framework

Hoare, Sam R. J., Tewson, Paul H., Quinn, Anne Marie, Hughes, Thomas E.

Journal:

Scientific Reports

Année:

2020

Langue:

english

Fichier:

PDF, 2.68 MB

english, 2020

Analyzing kinetic signaling data for G-protein-coupled receptors

Hoare, Sam R. J., Tewson, Paul H., Quinn, Anne Marie, Hughes, Thomas E., Bridge, Lloyd J.

Journal:

Scientific Reports

Année:

2020

Fichier:

PDF, 2.97 MB

2020

Association of Child and Adolescent Mental Health With Adolescent Health Behaviors in the UK Millennium Cohort

Hoare, Erin, Werneck, Andre O., Stubbs, Brendon, Firth, Joseph, Collins, Sam, Corder, Kirsten, van Sluijs, Esther M. F.

Journal:

JAMA Network Open

Année:

2020

Fichier:

PDF, 746 KB

2020

Pharmacological characterisation of novel adenosine A3 receptor antagonists

Barkan, Kerry, Lagarias, Panagiotis, Stampelou, Margarita, Stamatis, Dimitrios, Hoare, Sam, Safitri, Dewi, Klotz, Karl-Norbert, Vrontaki, Eleni, Kolocouris, Antonios, Ladds, Graham

Journal:

Scientific Reports

Année:

2020

Fichier:

PDF, 2.92 MB

2020