Search Results - "GIBBS, E. Michael"

Acute Effects of Atypical Antipsychotics on Whole-Body Insulin Resistance in Rats: Implications for Adverse Metabolic Effects by HOUSEKNECHT, Karen L, ROBERTSON, Alan S, ZAVADOSKI, William, GIBBS, E. Michael, JOHNSON, David E, ROLLEMA, Hans

“…Although it is generally accepted that atypical antipsychotics differ in their risk for diabetic side effects, the underlying pharmacological mechanisms are…”
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The discovery of potent, selective, and orally bioavailable PDE9 inhibitors as potential hypoglycemic agents by DeNinno, Michael P., Andrews, Melissa, Bell, Andrew S., Chen, Yue, Eller-Zarbo, Cynthia, Eshelby, Nan, Etienne, John B., Moore, Dianna E., Palmer, Michael J., Visser, Michael S., Yu, Li J., Zavadoski, William J., Michael Gibbs, E.

“…Starting from the non-selective lead 1, the sequential use of library and directed synthesis led to the optimized PDE9 inhibitor 13. Starting from a…”
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Identification of a novel glucose transporter-like protein-GLUT-12 by Rogers, Suzanne, Macheda, Maria L, Docherty, Susan E, Carty, Maynard D, Henderson, Michael A, Soeller, Walter C, Gibbs, E Michael, James, David E, Best, James D

“…Facilitative glucose transporters exhibit variable hexose affinity and tissue-specific expression. These characteristics contribute to specialized metabolic…”
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Defining the key pharmacophore elements of PF-04620110: Discovery of a potent, orally-active, neutral DGAT-1 inhibitor by Dow, Robert L., Andrews, Melissa P., Li, Jian-Cheng, Michael Gibbs, E., Guzman-Perez, Angel, LaPerle, Jennifer L., Li, Qifang, Mather, Dawn, Munchhof, Michael J., Niosi, Mark, Patel, Leena, Perreault, Christian, Tapley, Susan, Zavadoski, William J.

“…DGAT-1 is an enzyme that catalyzes the final step in triglyceride synthesis. mRNA knockout experiments in rodent models suggest that inhibitors of this enzyme…”
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Design and synthesis of potent, orally-active DGAT-1 inhibitors containing a dioxino[2,3- d]pyrimidine core by Dow, Robert L., Andrews, Melissa, Aspnes, Gary E., Balan, Gayatri, Michael Gibbs, E., Guzman-Perez, Angel, Karki, Kapil, LaPerle, Jennifer L., Li, Jian-Cheng, Litchfield, John, Munchhof, Michael J., Perreault, Christian, Patel, Leena

“…A novel series of potent DGAT-1 inhibitors was developed originating from the lactam-based clinical candidate PF-04620110. Incorporation of a dioxino[2,3-…”
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Modeling the mechanism of action of a DGAT1 inhibitor using a causal reasoning platform by Enayetallah, Ahmed E, Ziemek, Daniel, Leininger, Michael T, Randhawa, Ranjit, Yang, Jianxin, Manion, Tara B, Mather, Dawn E, Zavadoski, William J, Kuhn, Max, Treadway, Judith L, des Etages, Shelly Ann G, Gibbs, E Michael, Greene, Nigel, Steppan, Claire M

“…Triglyceride accumulation is associated with obesity and type 2 diabetes. Genetic disruption of diacylglycerol acyltransferase 1 (DGAT1), which catalyzes the…”
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Physiochemical drug properties associated with in vivo toxicological outcomes by Hughes, Jason D., Blagg, Julian, Price, David A., Bailey, Simon, DeCrescenzo, Gary A., Devraj, Rajesh V., Ellsworth, Edmund, Fobian, Yvette M., Gibbs, Michael E., Gilles, Richard W., Greene, Nigel, Huang, Enoch, Krieger-Burke, Teresa, Loesel, Jens, Wager, Travis, Whiteley, Larry, Zhang, Yao

“…Relationships between physicochemical drug properties and toxicity were inferred from a data set consisting of animal in vivo toleration (IVT) studies on 245…”
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Nitric oxide stimulates skeletal muscle glucose transport through a calcium/contraction- and phosphatidylinositol-3-kinase-independent pathway by ETGEN, G. J, FRYBURG, D. A, GIBBS, E. M

“…Recently published data have provided evidence that nitric oxide (NO) and cyclic guanosine monophosphate (cGMP) are signaling intermediates in the pathway…”
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Establishment of correlation between in vitro enzyme binding potency and in vivo pharmacological activity: application to liver glycogen phosphorylase a inhibitors by Yu, Li J, Chen, Yue, Treadway, Judith L, McPherson, R Kirk, McCoid, Scott C, Gibbs, E Michael, Hoover, Dennis J

“…In drug discovery, establishing a correlation between in vitro potency and in vivo activity is critical for the validation of the selected target and for…”
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Pharmacological inhibition to examine the role of DGAT1 in dietary lipid absorption in rodents and humans by Maciejewski, Benjamin S, LaPerle, Jennifer L, Chen, Danny, Ghosh, Avijit, Zavadoski, William J, McDonald, Thomas S, Manion, Tara B, Mather, Dawn, Patterson, Terrell A, Hanna, Maya, Watkins, Steven, Gibbs, E Michael, Calle, Roberto A, Steppan, Claire M

“…Alterations in fat metabolism, in particular elevated plasma concentrations of free fatty acids and triglycerides (TG), have been implicated in the…”
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Dual-action hypoglycemic and hypocholesterolemic agents that inhibit glycogen phosphorylase and lanosterol demethylase by Harwood, H. James, Petras, Stephen F., Hoover, Dennis J., Mankowski, Dayna C., Soliman, Victor F., Sugarman, Eliot D., Hulin, Bernard, Kwon, Younggil, Gibbs, E. Michael, Mayne, James T., Treadway, Judith L.

“…Diabetic dyslipidemia requires simultaneous treatment with hypoglycemic agents and lipid-modulating drugs. We recently described glycogen phosphorylase…”
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Altered metabolism causes cardiac dysfunction in perfused hearts from diabetic (db/db) mice by Belke, D D, Larsen, T S, Gibbs, E M, Severson, D L

“…Contractile function and substrate metabolism were characterized in perfused hearts from genetically diabetic C57BL/KsJ-lepr(db)/lepr(db) (db/db) mice and…”
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The PPAR-γ Agonist, Darglitazone, Restores Acute Inflammatory Responses to Cerebral Hypoxia–Ischemia in the Diabetic ob/ob Mouse by Kumari, Rashmi, Willing, Lisa B, Patel, Shyama D, Krady, J Kyle, Zavadoski, William J, Gibbs, E Michael, Vannucci, Susan J, Simpson, Ian A

“…Diabetes is an increased risk factor for stroke and results in increased brain damage in experimental animals and humans. The precise mechanisms are unclear,…”
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Discovery of PF-04620110, a Potent, Selective, and Orally Bioavailable Inhibitor of DGAT-1 by Dow, Robert L, Li, Jian-Cheng, Pence, Michael P, Gibbs, E. Michael, LaPerle, Jennifer L, Litchfield, John, Piotrowski, David W, Munchhof, Michael J, Manion, Tara B, Zavadoski, William J, Walker, Gregory S, McPherson, R. Kirk, Tapley, Susan, Sugarman, Eliot, Guzman-Perez, Angel, DaSilva-Jardine, Paul

“…Acyl-CoA:diacylglycerol acyltransferase-1 (DGAT-1) catalyzes the final committed step in the biosynthesis of triglycerides. DGAT-1 knockout mice have been…”
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Inhibitory effects of antipsychotics on carbachol-enhanced insulin secretion from perifused rat islets : Role of muscarinic antagonism in antipsychotic-induced diabetes and hyperglycemia by JOHNSON, David E, YAMAZAKI, Hanae, WARD, Karen M, SCHMIDT, Anne W, LEBEL, Wesley S, TREADWAY, Judith L, GIBBS, E. Michael, ZAWALICH, Walter S, ROLLEMA, Hans

“…Treatment with the atypical antipsychotics olanzapine and clozapine has been associated with an increased risk for deterioration of glucose homeostasis,…”
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Coat color and its effect on preference for the scent marks of opposite-sex conspecifics in the meadow vole Microtus pennsylvanicus by Vaughn, Ashlee A., Finger, Antedra A., Gibbs, Porshia E., Ferkin, Michael H.

“…Many mammal species can distinguish between opposite-sex conspecifics that differ in a certain trait. In that coat coloration is associated with differences in…”
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5-Chloroindoloyl glycine amide inhibitors of glycogen phosphorylase: synthesis, in vitro, in vivo, and X-ray crystallographic characterization by Wright, Stephen W., Rath, Virginia L., Genereux, Paul E., Hageman, David L., Levy, Carolyn B., McClure, Lester D., McCoid, Scott C., McPherson, R. Kirk, Schelhorn, Teresa M., Wilder, Donald E., Zavadoski, William J., Gibbs, E. Michael, Treadway, Judith L.

“…Glycine amide inhibitors of human liver glycogen phosphorylase A with improved potency in vivo are reported. The synthesis, in vitro, and in vivo biological…”
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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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Endogenous effectors of human liver glycogen phosphorylase modulate effects of indole-site inhibitors by Ercan-Fang, Nacide, Taylor, Miriam R, Treadway, Judith L, Levy, Carolyn B, Genereux, Paul E, Gibbs, E Michael, Rath, Virginia L, Kwon, Younggil, Gannon, Mary C, Nuttall, Frank Q

“…Phosphorylase is regulated by a number of small-molecular-weight effectors that bind to three sites on the enzyme. Recently, a fourth site referred to as the…”
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Glucose metabolism in perfused mouse hearts overexpressing human GLUT-4 glucose transporter by Belke, D D, Larsen, T S, Gibbs, E M, Severson, D L

“…Glucose and fatty acid metabolism was assessed in isolated working hearts from control C57BL/KsJ-m+/+db mice and transgenic mice overexpressing the human…”
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