Publications by authors named "Sam R Hoare"

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Binding kinetics redefine the antagonist pharmacology of the corticotropin-releasing factor type 1 receptor.
Beth A Fleck, Sam R J Hoare, Rebecca R Pick, Margaret J Bradbury, Dimitri E Grigoriadis

J Pharmacol Exp Ther· May 2012

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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, Sam R J Hoare

Bioorg Med Chem Lett· December 2010

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Analytical method for simultaneously measuring ex vivo drug receptor occupancy and dissociation rate: application to (R)-dimethindene occupancy of central histamine H1 receptors.
Siobhan Malany, Lisa M Hernandez, William F Smith, Paul D Crowe, Sam R J Hoare

J Recept Signal Transduct Res· August 2009

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Allosteric ligands for the corticotropin releasing factor type 1 receptor modulate conformational states involved in receptor activation.
Sam R J Hoare, Beth A Fleck, Raymond S Gross, Paul D Crowe, John P Williams

Mol Pharmacol· May 2008

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Pharmacological and pharmacokinetic characterization of 2-piperazine-alpha-isopropyl benzylamine derivatives as melanocortin-4 receptor antagonists.
Chen Chen, Fabio C Tucci, Wanlong Jiang, Joe A Tran, Beth A Fleck, Sam R Hoare

Bioorg Med Chem· May 2008

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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, Sam R Hoare

Bioorg Med Chem Lett· January 2008

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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

Bioorg Med Chem Lett· December 2007

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Design, synthesis, in vitro, and in vivo characterization of phenylpiperazines and pyridinylpiperazines as potent and selective antagonists of the melanocortin-4 receptor.
Joe A Tran, Wanlong Jiang, Fabio C Tucci, Beth A Fleck, Jenny Wen, Sam R Hoare

J Med Chem· December 2007

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Discovery of 1-[2-[(1S)-(3-dimethylaminopropionyl)amino-2-methylpropyl]-4-methylphenyl]-4-[(2R)-methyl-3-(4-chlorophenyl)-propionyl]piperazine as an orally active antagonist of the melanocortin-4 receptor for the potential treatment of cachexia.
Chen Chen, Wanlong Jiang, Fabio Tucci, Joe A Tran, Beth A Fleck, Sam R Hoare

J Med Chem· November 2007

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Pyrrolidinones as potent functional antagonists of the human melanocortin-4 receptor.
Wanlong Jiang, Fabio C Tucci, Joe A Tran, Beth A Fleck, Jenny Wen, Sam R Hoare

Bioorg Med Chem Lett· October 2007

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Allosteric modulators of class B G-protein-coupled receptors.
Sam R J Hoare

Curr Neuropharmacol· September 2007

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Pyrrolidinones as orally bioavailable antagonists of the human melanocortin-4 receptor with anti-cachectic activity.
Joe A Tran, Fabio C Tucci, Wanlong Jiang, Dragan Marinkovic, Caroline W Chen, Sam R Hoare

Bioorg Med Chem· August 2007

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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

Biochem Pharmacol· September 2006

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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

Biochem Pharmacol· July 2006

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Molecular interactions of nonpeptide agonists and antagonists with the melanocortin-4 receptor.
Beth A Fleck, Chen Chen, Weidong Yang, Rajesh Huntley, Stacy Markison, Sam R J Hoare

Biochemistry· November 2005

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Design and synthesis of tricyclic corticotropin-releasing factor-1 antagonists.
Raymond S Gross, Zhiqiang Guo, Brian Dyck, Tim Coon, Charles Q Huang, Sam R J Hoare

J Med Chem· September 2005

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Functional selectivity of melanocortin 4 receptor peptide and nonpeptide agonists: evidence for ligand-specific conformational states.
Sarah A Nickolls, Beth Fleck, Sam R J Hoare, Rich A Maki

J Pharmacol Exp Ther· June 2005

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The regulation of feeding and metabolic rate and the prevention of murine cancer cachexia with a small-molecule melanocortin-4 receptor antagonist.
Stacy Markison, Alan C Foster, Chen Chen, Gregor B Brookhart, Amy Hesse, Sam R J Hoare

Endocrinology· June 2005

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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, Sam R J Hoare

Bioorg Med Chem Lett· May 2005

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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

Peptides· March 2005

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Distinct conformations of the corticotropin releasing factor type 1 receptor adopted following agonist and antagonist binding are differentially regulated.
Stephen J Perry, Sachiko Junger, Trudy A Kohout, Sam R J Hoare, R Scott Struthers

J Biol Chem· March 2005

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Mechanisms of peptide and nonpeptide ligand binding to Class B G-protein-coupled receptors.
Sam R J Hoare

Drug Discov Today· March 2005

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Phenylguanidines as selective nonpeptide melanocortin-5 receptor antagonists.
Chen Chen, Jinghua Yu, Beth A Fleck, Sam R J Hoare, John Saunders

J Med Chem· July 2004

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Ligand affinity for amino-terminal and juxtamembrane domains of the corticotropin releasing factor type I receptor: regulation by G-protein and nonpeptide antagonists.
Sam R J Hoare, Sue K Sullivan, David A Schwarz, Nicholas Ling, Wylie W Vale

Biochemistry· April 2004

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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

Peptides· December 2003

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