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Review

Recent developments in ghrelin receptor (GHS-R1a) agonists and antagonists

Pages 1599-1618 | Published online: 25 Feb 2005

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Philip A Carpino & Guyu Ho. (2008) Modulators of the ghrelin system as potential treatments for obesity and diabetes. Expert Opinion on Therapeutic Patents 18:11, pages 1253-1263.
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Articles from other publishers (18)

N. Ceron-Romero, N. Taofeek, A. Thomas, E. Vroonland, K. Sanmartin, M. Verghese, E. Heinen & J.A. Vizcarra. (2021) Capromorelin, a ghrelin receptor agonist, increases feed intake and body weight gain in broiler chickens (Gallus gallus domesticus). Poultry Science 100:8, pages 101204.
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Dennis J. Worm, Sylvia Els‐Heindl & Annette G. Beck‐Sickinger. (2020) Targeting of peptide‐binding receptors on cancer cells with peptide‐drug conjugates. Peptide Science 112:3.
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Junichi Ishida, Masakazu Saitoh, Nicole Ebner, Jochen Springer, Stefan D. Anker & Stephan Haehling. (2020) Growth hormone secretagogues: history, mechanism of action, and clinical development. JCSM Rapid Communications 3:1, pages 25-37.
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Fabio Maria Sabbatini, Sergio Melotto, Giovanni Bernasconi, Steve M. Bromidge, Lucilla D'Adamo, Marilisa Rinaldi, Chiara Savoia, Claudia Mundi, Carla Di Francesco, Laura Zonzini, Vivian J. A. Costantini, Benedetta Perini, Enzo Valerio, Alfonso Pozzan, Elisabetta Perdonà, Filippo Visentini, Mauro Corsi & Romano Di Fabio. (2011) Azabicyclo[3.1.0]hexane-1-carbohydrazides as Potent and Selective GHSR1a Ligands Presenting a Specific in vivo Behavior. ChemMedChem 6:11, pages 1981-1985.
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Luca CostantinoDaniela Barlocco. (2009) Ghrelin receptor modulators and their therapeutic potential. Future Medicinal Chemistry 1:1, pages 157-177.
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Graeme L. Fraser, Hamid R. Hoveyda & Gloria Shaffer Tannenbaum. (2008) Pharmacological Demarcation of the Growth Hormone, Gut Motility and Feeding Effects of Ghrelin Using a Novel Ghrelin Receptor Agonist. Endocrinology 149:12, pages 6280-6288.
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Weixu Zhai, Neil Flynn, Daniel A. Longhi, Joseph A. Tino, Brian J. Murphy, Dorothy Slusarchyk, David A. Gordon, Anna Pendri, Shuhao Shi, Robert Stoffel, Baoqing Ma, Michael J. Sofia & Samuel W. Gerritz. (2008) Discovery and optimization of (R)-prolinol-derived agonists of the Growth Hormone Secretagogue receptor (GHSR). Bioorganic & Medicinal Chemistry Letters 18:18, pages 5083-5086.
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Andrés S. Hernández, Stephen G. Swartz, Dorothy Slusarchyk, Mujing Yan, R. Krishna Seethala, Paul Sleph, Gary Grover, Kenneth Dickinson, Leah Giupponi, Timothy W. Harper, W. Griffith Humphreys, Daniel A. Longhi, Neil Flynn, Brian J. Murphy, David A. Gordon, Scott A. Biller, Jeffrey A. Robl & Joseph A. Tino. (2008) Optimization of 1H-tetrazole-1-alkanenitriles as potent orally bioavailable growth hormone secretagogues. Bioorganic & Medicinal Chemistry Letters 18:6, pages 2067-2072.
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Tom D. Heightman, Jackie S. Scott, Mark Longley, Vincent Bordas, David K. Dean, Richard Elliott, Gail Hutley, Jason Witherington, Lee Abberley, Barry Passingham, Manuela Berlanga, Maite de los Frailes, Alan Wise, Ben Powney, Alison Muir, Fiona McKay, Sharon Butler, Kim Winborn, Christopher Gardner, Jill Darton, Colin Campbell & Gareth Sanger. (2007) Potent achiral agonists of the ghrelin (growth hormone secretagogue) receptor. Part I: Lead identification. Bioorganic & Medicinal Chemistry Letters 17:23, pages 6584-6587.
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Andrés S. Hernández, Peter T.W. Cheng, Christa M. Musial, Stephen G. Swartz, Rocco J. George, Gary Grover, Dorothy Slusarchyk, R. Krishna Seethala, Mark Smith, Kenneth Dickinson, Leah Giupponi, Daniel A. Longhi, Neil Flynn, Brian J. Murphy, David A. Gordon, Scott A. Biller, Jeffrey A. Robl & Joseph A. Tino. (2007) Discovery, synthesis, and structure–activity studies of tetrazole based growth hormone secretagogues. Bioorganic & Medicinal Chemistry Letters 17:21, pages 5928-5933.
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Jade S. Blakeney, Robert C. Reid, Giang T. Le & David P. Fairlie. (2007) Nonpeptidic Ligands for Peptide-Activated G Protein-Coupled Receptors. Chemical Reviews 107:7, pages 2960-3041.
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Britta Evers, Gerd Ruehter, Martina Berg, Jeffrey A. Dodge, Dirk Hankotius, Ulrike Hary, Louis N. Jungheim, Hans-Juergen Mest, Eva-Maria Martin de la Nava, Michael Mohr, Brian S. Muehl, Soenke Petersen, Birgit Sommer, Grit Riedel-Herold, Mark J. Tebbe, Kenneth J. Thrasher & Silke Voelkers. (2005) Structure activity studies of the serine-AIB dipeptide domain in 2,3-dihydroisothiazole based growth hormone secretagogues. Bioorganic & Medicinal Chemistry 13:24, pages 6748-6762.
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Hongyu Zhao. (2005) Growth hormone secretagogue receptor antagonists as potential therapeutic agents for obesity. Drug Development Research 65:2, pages 50-54.
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Teruhisa Tokunaga, W. Ewan Hume, Jun Nagamine, Tetsuya Kawamura, Mutsuo Taiji & Ryu Nagata. (2005) Structure–activity relationships of the oxindole growth hormone secretagogues. Bioorganic & Medicinal Chemistry Letters 15:7, pages 1789-1792.
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Hongyu Zhao, Zhili Xin, Gang Liu, Verlyn G. Schaefer, H. Douglas Falls, Wiweka Kaszubska, Christine A. Collins & Hing L. Sham. (2004) Discovery of Tetralin Carboxamide Growth Hormone Secretagogue Receptor Antagonists via Scaffold Manipulation. Journal of Medicinal Chemistry 47:27, pages 6655-6657.
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Charles W. Lugar, Michael P. Clay, Terry D. Lindstrom, Andrea L. Woodson, David Smiley, Mark L. Heiman & Jeffrey A. Dodge. (2004) Synthesis and biological evaluation of an orally active ghrelin agonist that stimulates food consumption and adiposity in rats. Bioorganic & Medicinal Chemistry Letters 14:23, pages 5873-5876.
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Jeffrey A. Dodge & Mark L. Heiman. 2003. 81 88 .
Iyassu Sebhat, Zhixiong Ye, Maria Bednarek, David Weinberg, Ravi Nargund & Tung M. Fong. 2003. 31 40 .

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