Search Results - "Harwood, H. James"

Acetyl-CoA carboxylase inhibition by ND-630 reduces hepatic steatosis, improves insulin sensitivity, and modulates dyslipidemia in rats by Harriman, Geraldine, Greenwood, Jeremy, Bhat, Sathesh, Huang, Xinyi, Wang, Ruiying, Paul, Debamita, Tong, Liang, Saha, Asish K., Westlin, William F., Kapeller, Rosana, Harwood, H. James

“…Simultaneous inhibition of the acetyl-CoA carboxylase (ACC) isozymes ACC1 and ACC2 results in concomitant inhibition of fatty acid synthesis and stimulation of…”
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Inhibition of acetyl-CoA carboxylase suppresses fatty acid synthesis and tumor growth of non-small-cell lung cancer in preclinical models by Svensson, Robert U, Parker, Seth J, Eichner, Lillian J, Kolar, Matthew J, Wallace, Martina, Brun, Sonja N, Lombardo, Portia S, Van Nostrand, Jeanine L, Hutchins, Amanda, Vera, Lilliana, Gerken, Laurie, Greenwood, Jeremy, Bhat, Sathesh, Harriman, Geraldine, Westlin, William F, Harwood, H James, Saghatelian, Alan, Kapeller, Rosana, Metallo, Christian M, Shaw, Reuben J

“…An allosteric inhibitor of acetyl-CoA carboxylase reveals a metabolic liability of non-small-cell lung cancer and slows tumor growth alone and in combination…”
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An allosteric mechanism for potent inhibition of human ATP-citrate lyase by Wei, Jia, Leit, Silvana, Kuai, Jun, Therrien, Eric, Rafi, Salma, Harwood, H. James, DeLaBarre, Byron, Tong, Liang

“…ATP-citrate lyase (ACLY) is a central metabolic enzyme and catalyses the ATP-dependent conversion of citrate and coenzyme A (CoA) to oxaloacetate and…”
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Acetyl‐coenzyme A carboxylase inhibition reduces de novo lipogenesis in overweight male subjects: A randomized, double‐blind, crossover study by Stiede, Kathryn, Miao, Wenyan, Blanchette, Heather S., Beysen, Carine, Harriman, Geraldine, Harwood, H. James, Kelley, Heather, Kapeller, Rosana, Schmalbach, Tess, Westlin, William F.

“…NDI‐010976, an allosteric inhibitor of acetyl‐coenzyme A carboxylases (ACC) ACC1 and ACC2, reduces hepatic de novo lipogenesis (DNL) and favorably affects…”
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The adipocyte as an endocrine organ in the regulation of metabolic homeostasis by Harwood, H. James

“…Over the past decade and a half it has become increasingly clear that adipose tissue is a much more complex organ than was initially considered and that its…”
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Acetyl-coenzyme A carboxylases: Versatile targets for drug discovery by Tong, Liang, Harwood Jr, H. James

“…Acetyl‐coenzyme A carboxylases (ACCs) have crucial roles in fatty acid metabolism in humans and most other living organisms. They are attractive targets for…”
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Pharmacologic inhibition of site 1 protease activity inhibits sterol regulatory element-binding protein processing and reduces lipogenic enzyme gene expression and lipid synthesis in cultured cells and experimental animals by Hawkins, Julie L, Robbins, Michael D, Warren, Laurie C, Xia, Donghui, Petras, Stephen F, Valentine, James J, Varghese, Alison H, Wang, Ing-Kae, Subashi, Timothy A, Shelly, Lorraine D, Hay, Bruce A, Landschulz, Katherine T, Geoghegan, Kieran F, Harwood, Jr, H James

“…Sterol regulatory element-binding proteins (SREBPs) are major transcriptional regulators of cholesterol, fatty acid, and glucose metabolism. Genetic disruption…”
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Nonhuman primates and other animal models in diabetes research by Harwood, Jr, H James, Listrani, Paul, Wagner, Janice D

“…Animal models are important for determining the pathogenesis of and potential treatments for obesity and diabetes. Nonhuman primates (NHPs) are particularly…”
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Treating the metabolic syndrome: acetyl-CoA carboxylase inhibition by Harwood, Jr, H James

“…Metabolic syndrome is defined as a clustering of cardiovascular risk factors (abdominal obesity, hyperinsulinaemia, atherogenic dislipidaemia, hypertension,…”
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class of selective antibacterials derived from a protein kinase inhibitor pharmacophore by Miller, J. Richard, Dunham, Steve, Mochalkin, Igor, Banotai, Craig, Bowman, Matthew, Buist, Susan, Dunkle, Bill, Hanna, Debra, Harwood, H. James, Huband, Michael D, Karnovsky, Alla, Kuhn, Michael, Limberakis, Chris, Liu, Jia Y, Mehrens, Shawn, Mueller, W. Thomas, Narasimhan, Lakshmi, Ogden, Adam, Ohren, Jeff, Prasad, J.V.N. Vara, Shelly, John A, Skerlos, Laura, Sulavik, Mark, Thomas, V. Hayden, VanderRoest, Steve, Wang, LiAnn, Wang, Zhigang, Whitton, Amy, Zhu, Tong, Stover, C. Kendall

“…As the need for novel antibiotic classes to combat bacterial drug resistance increases, the paucity of leads resulting from target-based antibacterial…”
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CP-346086: an MTP inhibitor that lowers plasma cholesterol and triglycerides in experimental animals and in humans by Chandler, Charles E, Wilder, Donald E, Pettini, Judith L, Savoy, Yvette E, Petras, Stephen F, Chang, George, Vincent, John, Harwood, Jr, H James

“…A microsomal triglyceride transfer protein (MTP) inhibitor, CP-346086, was identified that inhibited both human and rodent MTP activity [concentration giving…”
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Discovery of small molecule isozyme non-specific inhibitors of mammalian acetyl-CoA carboxylase 1 and 2 by Corbett, Jeffrey W., Freeman-Cook, Kevin D., Elliott, Richard, Vajdos, Felix, Rajamohan, Francis, Kohls, Darcy, Marr, Eric, Zhang, Hailong, Tong, Liang, Tu, Meihua, Murdande, Sharad, Doran, Shawn D., Houser, Janet A., Song, Wei, Jones, Christopher J., Coffey, Steven B., Buzon, Leanne, Minich, Martha L., Dirico, Kenneth J., Tapley, Susan, Kirk McPherson, R., Sugarman, Eliot, James Harwood, H., Esler, William

“…The discovery and SAR of the isozyme non-selective acetyl-CoA carboxylase 1 and 2 inhibitor 59 is described. Screening Pfizer’s compound library resulted in…”
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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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Old World nonhuman primate models of type 2 diabetes mellitus by Wagner, J.D, Kavanagh, K, Ward, G.M, Auerbach, B.J, Harwood, H.J. Jr, Kaplan, J.R

“…Type 2 diabetes mellitus is a major health problem of increasing incidence. To better study the pathogenesis and potential therapeutic agents for this disease,…”
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A selective peroxisome proliferator-activated receptor alpha agonist, CP-900691, improves plasma lipids, lipoproteins, and glycemic control in diabetic monkeys by Wagner, Janice D, Shadoan, Melanie K, Zhang, Li, Ward, Gina M, Royer, Lori J, Kavanagh, Kylie, Francone, Omar L, Auerbach, Bruce J, Harwood, Jr, H James

“…Peroxisome proliferator-activated receptors (PPARs) are involved in the regulation of lipid and glucose metabolism. PPARgamma agonists improve insulin…”
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A selective cannabinoid-1 receptor antagonist, PF-95453, reduces body weight and body fat to a greater extent than pair-fed controls in obese monkeys by Wagner, Janice D, Zhang, Li, Kavanagh, Kylie, Ward, Gina M, Chin, Janice E, Hadcock, John R, Auerbach, Bruce J, Harwood, Jr, H James

“…Cannabinoid-1 (CB(1)) receptor antagonists exhibit pharmacological properties favorable to treatment of obesity, caused by both centrally mediated effects on…”
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Aminopyrrolidineamide inhibitors of site-1 protease by Hay, Bruce A., Abrams, Barbara, Zumbrunn, Allice Y., Valentine, James J., Warren, Laurie C., Petras, Stephen F., Shelly, Lorraine D., Xia, Angela, Varghese, Alison H., Hawkins, Julie L., Van Camp, Jennifer A., Robbins, Michael D., Landschulz, Katherine, Harwood, H. James

“…A series of aminopyrrolidineamide inhibitors of sterol regulatory element binding protein site-1 protease was identified. The discovery and efficacy of a…”
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Short-term hyperglycemia increases arterial superoxide production and iron dysregulation in atherosclerotic monkeys by Rowe, Patrick A, Kavanagh, Kylie, Zhang, Li, Harwood, H. James, Wagner, Janice D

“…Abstract The incidence and severity of atherosclerotic vascular disease are increased in diabetic patients, in part because of increased production of reactive…”
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Three-Dimensional Quantitative Structure-Activity Relationship Analysis of Human CYP51 Inhibitors by EKINS, Sean, MANKOWSKI, Dayna C, HOOVER, Dennis J, LAWTON, Michael P, TREADWAY, Judith L, HARWOOD, H. James

“…CYP51 fulfills an essential requirement for all cells, by catalyzing three sequential mono-oxidations within the cholesterol biosynthesis cascade. Inhibition…”
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Inhibition of Acetyl-CoA Carboxylase by Phosphorylation or the Inhibitor ND-654 Suppresses Lipogenesis and Hepatocellular Carcinoma by Lally, James S.V., Ghoshal, Sarani, DePeralta, Danielle K., Moaven, Omeed, Wei, Lan, Masia, Ricard, Erstad, Derek J., Fujiwara, Naoto, Leong, Vivian, Houde, Vanessa P., Anagnostopoulos, Alexander E., Wang, Alice, Broadfield, Lindsay A., Ford, Rebecca J., Foster, Robert A., Bates, Jamie, Sun, Hailing, Wang, Ting, Liu, Henry, Ray, Adrian S., Saha, Asish K., Greenwood, Jeremy, Bhat, Sathesh, Harriman, Geraldine, Miao, Wenyan, Rocnik, Jennifer L., Westlin, William F., Muti, Paola, Tsakiridis, Theodoros, Harwood, H. James, Kapeller, Rosana, Hoshida, Yujin, Tanabe, Kenneth K., Steinberg, Gregory R., Fuchs, Bryan C.

“…The incidence of hepatocellular carcinoma (HCC) is rapidly increasing due to the prevalence of obesity and non-alcoholic fatty liver disease, but the molecular…”
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