Search Results - "HARGROVE, Diane M"

Additive effect of simultaneous continuous administration of degarelix and TAK-448 on LH suppression in a castrated rat model by Stalewski, Jacek, Hargrove, Diane M., Wolfe, Monica, Kohout, Trudy A., Kamal, Adeela

“…Gonadotropin releasing hormone (GnRH) analogs have long been used in androgen deprivation therapy (ADT) in the treatment of prostate cancer. Chronic…”
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Isozyme-nonselective N-Substituted Bipiperidylcarboxamide Acetyl-CoA Carboxylase Inhibitors Reduce Tissue Malonyl-CoA Concentrations, Inhibit Fatty Acid Synthesis, and Increase Fatty Acid Oxidation in Cultured Cells and in Experimental Animals by Harwood, H.James, Petras, Stephen F., Shelly, Lorraine D., Zaccaro, Lawrence M., Perry, David A., Makowski, Michael R., Hargrove, Diane M., Martin, Kelly A., Tracey, W.Ross, Chapman, Justin G., Magee, William P., Dalvie, Deepak K., Soliman, Victor F., Martin, William H., Mularski, Christian J., Eisenbeis, Shane A.

“…Inhibition of acetyl-CoA carboxylase (ACC), with its resultant inhibition of fatty acid synthesis and stimulation of fatty acid oxidation, has the potential to…”
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Pharmacological Characterization of Apraglutide, a Novel Long-Acting Peptidic Glucagon-Like Peptide-2 Agonist, for the Treatment of Short Bowel Syndrome by Hargrove, Diane M, Alagarsamy, Sudarkodi, Croston, Glenn, Laporte, Régent, Qi, Steve, Srinivasan, Karthik, Sueiras-Diaz, Javier, Wiśniewski, Kazimierz, Hartwig, Jennifer, Lu, Mark, Posch, Alexander P, Wiśniewska, Halina, Schteingart, Claudio D, Rivière, Pierre J-M, Dimitriadou, Violetta

“…Glucagon-like peptide-2 (GLP-2) agonists have therapeutic potential in clinical indications in which the integrity or absorptive function of the intestinal…”
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Biological activity of AC3174, a peptide analog of exendin-4 by Hargrove, Diane M., Kendall, Eric S., Reynolds, James M., Lwin, Aung N., Herich, John P., Smith, Pamela A., Gedulin, Bronislava R., Flanagan, Shawn D., Jodka, Carolyn M., Hoyt, Julie A., McCowen, Kevin M., Parkes, David G., Anderson, Christen M.

“…Exenatide, the active ingredient of BYETTA® (exenatide injection), is an incretin mimetic that has been developed for the treatment of patients with type 2…”
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Discovery of Potent, Selective, and Short-Acting Peptidic V 2 Receptor Agonists by Wiśniewski, Kazimierz, Qi, Steve, Kraus, John, Ly, Brian, Srinivasan, Karthik, Tariga, Hiroe, Croston, Glenn, La, Erin, Wiśniewska, Halina, Ortiz, Carlos, Laporte, Régent, Rivière, Pierre J-M, Neyer, Gebhard, Hargrove, Diane M, Schteingart, Claudio D

“…The vasopressin analogue desmopressin (desamino-d-arginine vasopressin, dDAVP, 1) is a potent vasopressin 2 (V ) receptor (V R) agonist approved in many…”
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Discovery of potent and orally bioavailable heterocycle-based β3-adrenergic receptor agonists, potential therapeutics for the treatment of obesity by LAFONTAINE, Jennifer A, DAY, Robert F, DASILVA-JARDINE, Paul, DIBRINO, Joe, HADCOCK, John R, HARGROVE, Diane M, LINHARES, Michael, MARTIN, Kelly A, MAURER, Tristan S, NARDONE, Nancy A, TESS, David A

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Discovery of Potent, Nonsteroidal, and Highly Selective Glucocorticoid Receptor Antagonists by Morgan, Bradley P, Swick, Andrew G, Hargrove, Diane M, LaFlamme, Janet A, Moynihan, Melinda S, Carroll, Richard S, Martin, Kelly A, Lee, Eunsun, Decosta, Debra, Bordner, Jon

“…An approach to the computer-assisted, pharmacophore design of nonsteroidal templates for the glucocorticoid receptor (GR) that contained an element of…”
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Exenatide does not evoke pancreatitis and attenuates chemically induced pancreatitis in normal and diabetic rodents by Tatarkiewicz, Krystyna, Smith, Pamela A, Sablan, Emmanuel J, Polizzi, Clara J, Aumann, Donald E, Villescaz, Christiane, Hargrove, Diane M, Gedulin, Bronislava R, Lu, Melissa G W, Adams, Lisa, Whisenant, Tina, Roy, Denis, Parkes, David G

“…The risk of developing pancreatitis is elevated in type 2 diabetes and obesity. Cases of pancreatitis have been reported in type 2 diabetes patients treated…”
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GLUT4 Overexpression in db/db Mice Dose-Dependently Ameliorates Diabetes But Is Not a Lifelong Cure by BROZINICK, Joseph T, MCCOID, Scott C, REYNOLDS, Thomas H, NARDONE, Nancy A, HARGROVE, Diane M, STEVENSON, Ralph W, CUSHMAN, Samuel W, GIBBS, E. Michael

“…GLUT4 Overexpression in db/db Mice Dose-Dependently Ameliorates Diabetes But Is Not a Lifelong Cure Joseph T. Brozinick, Jr. 1 , Scott C. McCoid 2 , Thomas H…”
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Discovery of Potent, Selective, and Short-Acting Peptidic V2 Receptor Agonists by Wiśniewski, Kazimierz, Qi, Steve, Kraus, John, Ly, Brian, Srinivasan, Karthik, Tariga, Hiroe, Croston, Glenn, La, Erin, Wiśniewska, Halina, Ortiz, Carlos, Laporte, Régent, Rivière, Pierre J.-M, Neyer, Gebhard, Hargrove, Diane M, Schteingart, Claudio D

“…The vasopressin analogue desmopressin (desamino-d-arginine8 vasopressin, dDAVP, 1) is a potent vasopressin 2 (V2) receptor (V2R) agonist approved in many…”
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Synthesis and Pharmacological Characterization of Novel Glucagon-like Peptide‑2 (GLP-2) Analogues with Low Systemic Clearance by Wiśniewski, Kazimierz, Sueiras-Diaz, Javier, Jiang, Guangcheng, Galyean, Robert, Lu, Mark, Thompson, Dorain, Wang, Yung-Chih, Croston, Glenn, Posch, Alexander, Hargrove, Diane M, Wiśniewska, Halina, Laporte, Régent, Dwyer, John J, Qi, Steve, Srinivasan, Karthik, Hartwig, Jennifer, Ferdyan, Nicky, Mares, Monica, Kraus, John, Alagarsamy, Sudarkodi, Rivière, Pierre J. M, Schteingart, Claudio D

“…Glucagon-like peptide-2 receptor agonists have therapeutic potential for the treatment of intestinal diseases. The native hGLP-2, a 33 amino acid…”
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Discovery and evaluation of pyrazolo[1,5- a]pyrimidines as neuropeptide Y1 receptor antagonists by Griffith, David A., Hargrove, Diane M., Maurer, Tristan S., Blum, Charles A., De Lombaert, Stéphane, Inthavongsay, John K., Klade, Lee E., Mack, Christine M., Rose, Colin R., Sanders, Martin J., Carpino, Philip A.

“…A novel series of pyrazolo[1,5- a]pyrimidine derivatives was synthesized and evaluated as NPY Y1R antagonists. Oral administration of 2f resulted in modest…”
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In vitro and in vivo pharmacology of CP-945,598, a potent and selective cannabinoid CB1 receptor antagonist for the management of obesity by Hadcock, John R., Griffith, David A., Iredale, Phillip A., Carpino, Phillip A., Dow, Robert L., Black, Shawn C., O’Connor, Rebecca, Gautreau, Denise, Lizano, Jeffrey S., Ward, Karen, Hargrove, Diane M., Kelly-Sullivan, Dawn, Scott, Dennis O.

“…Cannabinoid CB1 receptor antagonists exhibit pharmacologic properties favorable for the treatment of metabolic disease. CP-945,598…”
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Discovery of N-benzyl-2-[(4S)-4-(1H-indol-3-ylmethyl)-5-oxo-1-phenyl-4,5-dihydro-6H-[1,2,4]triazolo[4,3-a][1,5]benzodiazepin-6-yl]-N-isopropylacetamide, an orally active, gut-selective CCK1 receptor agonist for the potential treatment of obesity by Elliott, Richard L., Cameron, Kimberly O., Chin, Janice E., Bartlett, Jeremy A., Beretta, Elena E., Chen, Yue, Jardine, Paul Da Silva, Dubins, Jeffrey S., Gillaspy, Melissa L., Hargrove, Diane M., Kalgutkar, Amit S., LaFlamme, Janet A., Lame, Mary E., Martin, Kelly A., Maurer, Tristan S., Nardone, Nancy A., Oliver, Robert M., Scott, Dennis O., Sun, Dexue, Swick, Andrew G., Trebino, Catherine E., Zhang, Yingxin

“…We report the design, synthesis, and SAR of triazolobenzodiazepinone CCK1 receptor agonists. Compound 4a is a potent, selective CCK1 receptor agonist which…”
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Pharmacological Characterization of FE 203799, a Novel Long Acting Peptide Analog of Glucagon-Like Peptide-2 (GLP-2) by Hargrove, Diane M, Alagarsamy, Sudar, Qi, Steve, Srinivasan, Karthik, Croston, Glenn, Laporte, Regent, Sueiras-Diaz, Javier, Wisniewski, Kazimierz, Hartwig, Jennifer, Wisniewska, Halina T, Lu, Mark, Posch, Alexander P, Schteingart, Claudio D, Rivière, Pierre J

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Discovery of a novel series of 6-azauracil-based thyroid hormone receptor ligands: potent, TRβ subtype-selective thyromimetics by Dow, Robert L., Schneider, Steven R., Paight, Ernest S., Hank, Richard F., Chiang, Phoebe, Cornelius, Peter, Lee, Eunsun, Newsome, William P., Swick, Andrew G., Spitzer, Josephine, Hargrove, Diane M., Patterson, Terrell A., Pandit, Jayvardhan, Chrunyk, Boris A., LeMotte, Peter K., Danley, Dennis E., Rosner, Michele H., Ammirati, Mark J., Simons, Samuel P., Schulte, Gayle K., Tate, Bonnie F., DaSilva-Jardine, Paul

“…In this communication, we wish to describe the discovery of a novel series of 6-azauracil-based thyromimetics that possess up to 100-fold selectivities for…”
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Potent and selective, sulfamide-based human β3-adrenergic receptor agonists by DOW, Robert L, PAIGHT, Ernest S, SCHNEIDER, Steven R, HADCOCK, John R, HARGROVE, Diane M, MARTIN, Kelly A, MAURER, Tristan S, NARDONE, Nancy A, TESS, David A, DASILVA-JARDINE, Paul

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In Vitro and in Vivo Characterization of 3-{2-[6-(2-tert-Butoxyethoxy)pyridin-3-yl]-1H-imidazol-4-yl}benzonitrile Hydrochloride Salt, a Potent and Selective NPY5 Receptor Antagonist by Elliott, Richard L, Oliver, Robert M, Hammond, Marlys, Patterson, Terrell A, She, Li, Hargrove, Diane M, Martin, Kelly A, Maurer, Tristan S, Kalvass, J. Cory, Morgan, Bradley P, DaSilva-Jardine, Paul A, Stevenson, Ralph W, Mack, Christine M, Cassella, James V

“…To investigate the anorectic potential of NPY5 receptor antagonists, we have profiled the in vitro and in vivo properties of…”
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P2.45: Apraglutide Has an Extended Duration and Induces a Greater Intestinotrophic Effect Compared with Teduglutide, Glepaglutide and Elsiglutide by Dimitriadou, Violetta, Hargrove, Diane M, Laporte, Regent, Posch, Alexander, Riviere, Pierre, Porter, Richard, Meyer, Christian, Santarelli, Luca

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Glucose Transport-Enhancing and Hypoglycemic Activity of 2-Methyl-2-phenoxy-3-phenylpropanoic Acids by Sarges, Reinhard, Hank, Richard F, Blake, James F, Bordner, Jon, Bussolotti, Donald L, Hargrove, Diane M, Treadway, Judith L, Gibbs, E. Michael

“…A series of 2-phenoxy-3-phenylpropanoic acids has been prepared which contains many potent hypoglycemic agents as demonstrated by assessing glucose lowering in…”
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