Cell based in vitro and ex vivo models in metabolic disease drug discovery: nice to have or critical path?

Bibliography

• Kennedy SP, Bormann BJ. Effective partnering of academic and physician scientists with the pharmaceutical drug development industry. Exp Biol Med 2006;231(11):1690-4
   Web of Science ®Google Scholar
• Kola I, Landis J. Can the pharmaceutical industry reduce attrition rates? Nat Rev Drug Disc 2004;3(8):711-16
   PubMed Web of Science ®Google Scholar
• Sams-Dodd F. Target-based drug discovery: is something wrong? Drug Discov Today 2005;10(2):139-147
   Web of Science ®Google Scholar
• Korner J, Aronne LJ. Pharmacological approaches to weight reduction: Therapeutic targets. J Clin Endocrinol Metab 2004;89(6):2616-21
   PubMed Web of Science ®Google Scholar
• Zhang Y, Proenca R, Maffei M, et al. Positional cloning of the mouse obese gene and its human homologue. Nat 1994;372:425-32
   Google Scholar
• Rankinen T, Zuberi A, Chagnon YC, et al. The human obesity gene map: The 2005 update. Obesity 2006;14(4):529-644
   PubMed Web of Science ®Google Scholar
• Powell DR. Obesity drugs and their targets: correlation of mouse knockout phenotypes with drug effects in vivo. Obes Rev 2006;7(1):89-108
   PubMed Web of Science ®Google Scholar
• Cefalu WT. Pharmacotherapy for the treatment of patients with type 2 diabetes mellitus: rationale and specific agents. Clin Pharmacol Ther 2007;81(5):636-49
   PubMed Web of Science ®Google Scholar
• Speakman J, Hambly C, Mitchell S, et al. Animal models of obesity. Obes Rev 2007;8(s1):55-61
   PubMed Web of Science ®Google Scholar
• Rodbell M. Metabolism of isolated fat cells. I. Effects of hormones on glucose metabolism and lipolysis. J Biol Chem 1964;239(2):375-80
   PubMed Web of Science ®Google Scholar
• Cushman SW. structure-function relationships in the adipose cell: I. Ultrastructure of the isolated adipose cell. J Cell Biol 1970;46(2):326-41
   PubMed Web of Science ®Google Scholar
• Ruan H, Zarnowski M, Cushman SW, et al. Standard isolation of primary adipose cells from mouse epididymal fat pads induces inflammatory mediators and down-regulates adipocyte genes. J Biol Chem 2003;278(48):47585-93
   PubMed Web of Science ®Google Scholar
• Brüning JC, Michael MD, Winnay JN, et al. A muscle-specific insulin receptor knockout exhibits features of the metabolic syndrome of NIDDM without altering glucose tolerance. Mol Cell 1998;2(5):559-69
   PubMed Web of Science ®Google Scholar
• Ukropcova B, McNeil M, Sereda O, et al. Dynamic changes in fat oxidation in human primary myocytes mirror metabolic characteristics of the donor. J Clin Invest 2005;115(7):1934-41
   PubMed Web of Science ®Google Scholar
• Gaster M, Rustan AC, Aas V, et al. Reduced lipid oxidation in skeletal muscle from type 2 diabetic subjects may be of genetic origin: evidence from cultured myotubes. Diab 2004;53(3):542-8
   PubMed Web of Science ®Google Scholar
• Higaki Y, Wojtaszewski JFP, Hirshman MF, et al. Insulin receptor substrate-2 is not necessary for insulin- and exercise-stimulated glucose transport in skeletal muscle. J Biol Chem 1999;274(30):20791-5
   PubMed Web of Science ®Google Scholar
• Hayashi T, Hirshman MF, Kurth EJ, et al. Evidence for 5′ AMP-activated protein kinase mediation of the effect of muscle contraction on glucose transport. Diab 1998;47(8):1369-73
   PubMed Web of Science ®Google Scholar
• Curtin NA, Clapham JC, Barclay CJ. Excess recovery heat production by isolated muscles from mice overexpressing uncoupling protein-3. J Physiol 2002;542(1):231-5
   PubMed Web of Science ®Google Scholar
• Weissman A, Keefer J, Miagkov A, et al. Cell-based screening assays. 2007;617-46
   Google Scholar
• Loechel F, Bjørn S, Linde V, et al. High content translocation assays for pathway profiling. In: High Content Screening, Humana Press, Totowa, NJ, USA 2006;(29):401-14
   Google Scholar
• Ferrick DA, Neilson A, Beeson C. Advances in measuring cellular bioenergetics using extracellular flux. Drug Discov Today 2008;13(5-6):268-74
   PubMed Web of Science ®Google Scholar
• Gnaiger E. Bioenergetics at low oxygen: dependence of respiration and phosphorylation on oxygen and adenosine diphosphate supply. Respir Physiol 2001;128(3):277-97
   PubMedGoogle Scholar
• Marroquin LD, Hynes J, Dykens JA, et al. Circumventing the Crabtree effect: replacing media glucose with galactose increases susceptibility of HepG2 cells to mitochondrial toxicants. Toxicol Sci 2007;97(2):539-47
   PubMed Web of Science ®Google Scholar
• Wang X, Wang R, Nemcek TA, et al. A self-contained 48-well fatty acid oxidation assay. ASSAY Drug DevTechnol 2004;2(1):63-9
   PubMed Web of Science ®Google Scholar
• Wensaas AJ, Rustan AC, Lovstedt K, et al. Cell-based multiwell assays for the detection of substrate accumulation and oxidation. J Lipid Res 2007;48(4):961-7
   PubMed Web of Science ®Google Scholar
• Kajstura J, Fiordaliso F, Andreoli AM, et al. IGF-1 overexpression inhibits the development of diabetic cardiomyopathy and angiotensin II-mediated oxidative stress. Diab 2001;50(6):1414-24
   PubMed Web of Science ®Google Scholar
• Kangas L, Grönroos M, Nieminen AL. Bioluminescence of cellular ATP: a new method for evaluating cytotoxic agents in vitro. Med Biol 1984;62(6):338-43
   PubMedGoogle Scholar
• Lundin A, Hasenson M, Persson J, et al. Estimation of biomass in growing cell lines by adenosine triphosphate assay. Meth Enzymol 1986;133:27-42
   Google Scholar
• Smiley ST, Reers M, Mottola-Hartshorn C, et al. Intracellular heterogeneity in mitochondrial membrane potentials revealed by a J-aggregate-forming lipophilic cation JC-1. Proc Natl Acad Sci USA 2008;88(9):3671-5
   Google Scholar
• Horrobin DF. Modern biomedical research: an internally self-consistent universe with little contact with medical reality? Nat Rev Drug Disc 2003;2(2):151-4
   Web of Science ®Google Scholar
• Olsavsky KM, Page JL, Johnson MC, et al. Gene expression profiling and differentiation assessment in primary human hepatocyte cultures, established hepatoma cell lines, and human liver tissues. Toxicol Appl Pharmacol 2007;222(1):42-56
   PubMed Web of Science ®Google Scholar
• Youdim KA, Tyman CA, Jones BC, et al. Induction of cytochrome P450: assessment in an immortalized human hepatocyte cell line (Fa2N4) using a novel higher throughput cocktail assay. Drug Metab Dispos 2007;35(2):275-82
   PubMed Web of Science ®Google Scholar
• Macpherson PCD, Suhr ST, Goldman D. Activity-dependent gene regulation in conditionally-immortalized muscle precursor cell lines. J Cell Biochem 2008;91(4):821-39
   Google Scholar
• Morganstein DL, Christian M, Turner JJO, et al. Conditionally immortalized white preadipocytes: a novel adipocyte model. J Lipid Res 2008;49(3):679-85
   PubMed Web of Science ®Google Scholar
• Lim PLK, Tan W, Latchoumycandane C, et al. Molecular and functional characterization of drug-metabolizing enzymes and transporter expression in the novel spontaneously immortalized human hepatocyte line HC-04. Toxicol in Vitro 2007;21(8):1390-401
   PubMed Web of Science ®Google Scholar
• Valtueña S, Salas-Salvadó J, Lorda PG. The respiratory quotient as a prognostic factor in weight-loss rebound. Int J Obes Relat Metab Disord 1997;21(9):811-7
   PubMed Web of Science ®Google Scholar
• Lou P, Hansen BS, Olsen PH, et al. Mitochondrial uncouplers with an extraordinary dynamic range. Biochem J 2007;407(1):129-40
   PubMed Web of Science ®Google Scholar
• Cutting WC, Mehrtens HG, Tainter ML. Action and uses of dinitrophenol. JAMA 1933;101(1):193-5
   Google Scholar
• Blaikie F, Brown S, Samuelsson L, et al. Targeting dinitrophenol to mitochondria: limitations to the development of a self-limiting mitochondrial protonophore. Biosci Rep 2006;26(3):231-43
   PubMed Web of Science ®Google Scholar
• Masaaki S, Hiroshi H. Recent developments in the design of orally bioavailable ß3-adrenergic receptor agonists. Curr Med Chem 2008;13(1):25-37
   Web of Science ®Google Scholar
• Savkur RS, Miller AR. Investigational PPAR-γ agonists for the treatment of Type 2 diabetes. Expert Opin Investig Drugs 2006;15(7):763-78
   PubMedGoogle Scholar
• Olefsky JM. Treatment of insulin resistance with peroxisome proliferator-activated receptor γ agonists. J Clin Invest 2000;106(4):467-72
   PubMed Web of Science ®Google Scholar
• Wilson-Fritch L, Burkart A, Bell G, et al. Mitochondrial biogenesis and remodeling during adipogenesis and in response to the insulin sensitizer rosiglitazone. Mol Cell Biol 2003;23(3):1085-94
   PubMed Web of Science ®Google Scholar
• Wilson-Fritch L, Nicoloro S, Chouinard M, et al. Mitochondrial remodeling in adipose tissue associated with obesity and treatment with rosiglitazone. J Clin Invest 2004;114(9):1281-9
   PubMed Web of Science ®Google Scholar
• Rong JX, Qiu Y, Hansen MK, et al. Adipose mitochondrial biogenesis is suppressed in db/db and high-fat diet-fed mice and improved by rosiglitazone. Diab 2007;56(7):1751-60
   PubMed Web of Science ®Google Scholar
• Bogacka I, Ukropcova B, McNeil M, et al. Structural and functional consequences of mitochondrial biogenesis in human adipocytes in vitro. J Clin Endocrinol Metab 2005;90(12):6650-6
   PubMed Web of Science ®Google Scholar
• Boden G, Homko C, Mozzoli M, et al. Thiazolidinediones upregulate fatty acid uptake and oxidation in adipose tissue of diabetic patients. Diab 2005;54(3):880-5
   PubMed Web of Science ®Google Scholar
• Grønn M, Christensen E, Hagve TA, et al. Effects of clofibrate feeding on essential fatty acid desaturation and oxidation in isolated rat liver cells. Biochimica et Biophys Acta (BBA) - Lipids and Lipid Metab 1992;1123(2):170-6
   PubMed Web of Science ®Google Scholar
• Amacher DE, Beck R, Schomaker SJ, et al. Hepatic microsomal enzyme induction, β-oxidation, and cell proliferation following administration of clofibrate, gemfibrozil, or bezafibrate in the CD Rat. Toxicol Appl Pharmacol 1997;142(1):143-50
   PubMed Web of Science ®Google Scholar
• Kaikaus RM, Chan WK, Lysenko N, et al. Induction of peroxisomal fatty acid beta-oxidation and liver fatty acid-binding protein by peroxisome proliferators. Mediation via the cytochrome P-450IVA1 omega-hydroxylase pathway. J Biol Chem 1993;268(13):9593-603
   PubMed Web of Science ®Google Scholar
• Lanne B, Dahllöf B, Lindahl C, et al. PPARα and PPARγ regulation of liver and adipose proteins in obese and dyslipidemic rodents. J Proteome Res 2006;5(8):1850-9
   PubMed Web of Science ®Google Scholar
• Edvardsson U, Ljungberg A, Linden D, et al. PPARα activation increases triglyceride mass and adipose differentiation-related protein in hepatocytes. J Lipid Res 2006;47(2):329-40
   PubMed Web of Science ®Google Scholar
• Dimopoulos N, Watson M, Green C, et al. The PPARδ agonist, GW501516, promotes fatty acid oxidation but has no direct effect on glucose utilisation or insulin sensitivity in rat L6 skeletal muscle cells. FEBS Lett 2007;581(24):4743-8
   PubMed Web of Science ®Google Scholar
• Krämer DK, A1 Khalili L, Guigas B, et al. Role of AMP kinase and PPARδ in the regulation of lipid and glucose metabolism in human skeletal muscle. J Biol Chem 2007;282(27):19313-20
   PubMed Web of Science ®Google Scholar
• Lee C, Olson P, Hevener A, et al. PPARδ regulates glucose metabolism and insulin sensitivity. Proc Natl Acad Sci USA 2006;103(9):3444-9
   PubMed Web of Science ®Google Scholar
• Narkar VA, Downes M, Yu RT, et al. AMPK and PPARδ agonists are exercise mimetics. Cell 2008;134(3):405-15
   PubMed Web of Science ®Google Scholar
• Riserus U, Sprecher D, Johnson T, et al. Activation of peroxisome proliferator-activated receptor (PPAR)δ promotes reversal of multiple metabolic abnormalities, reduces oxidative stress, and increases fatty acid oxidation in moderately obese men. Diab 2008;57(2):332-9
   PubMed Web of Science ®Google Scholar
• Vincent MF, Marangos PJ, Gruber HE, et al. Inhibition by AICA riboside of gluconeogenesis in isolated rat hepatocytes. Diab 1991;40(10):1259-66
   PubMed Web of Science ®Google Scholar
• Bergeron R, Russell RR III, Young LH, et al. Effect of AMPK activation on muscle glucose metabolism in conscious rats. Am J Physiol - Endocrinol Metab 1999;276(5):E938-44
   PubMed Web of Science ®Google Scholar
• Boon H, Bosselaar M, Praet S, et al. Intravenous AICAR administration reduces hepatic glucose output and inhibits whole body lipolysis in type 2 diabetic patients. Diabetologia 2008;51(10):1893-900
   PubMed Web of Science ®Google Scholar
• Zhou G, Myers R, Li Y, et al. Role of AMP-activated protein kinase in mechanism of metformin action. J Clin Invest 2001;108(8):1167-74
   PubMed Web of Science ®Google Scholar
• Choi CS, Savage DB, Abu-Elheiga L, et al. Continuous fat oxidation in acetyl–CoA carboxylase 2 knockout mice increases total energy expenditure, reduces fat mass, and improves insulin sensitivity. Proc Natl Acad Sci USA 2007;104(42):16480-5
   PubMed Web of Science ®Google Scholar
• Abu-Elheiga L, Matzuk MM, Abo-Hashema KA, et al. Continuous fatty acid oxidation and reduced fat storage in mice lacking acetyl-CoA carboxylase 2. Sci 2001;291(5513):2613-16
   Web of Science ®Google Scholar
• Tong L, Harwood HJ Jr. Acetyl-coenzyme a carboxylases: versatile targets for drug discovery. J Cell Biochem 2006;99(6):1476-88
   PubMed Web of Science ®Google Scholar
• Gu YG, Weitzberg M, Clark RF, et al. Synthesis and structure-activity relationships of N-{3-[2-(4-Alkoxyphenoxy)thiazol-5-yl]-1-methylprop-2-ynyl}carboxy derivatives as selective acetyl-CoA carboxylase 2 inhibitors. J Med Chem 2006;49(13):3770-3
   PubMed Web of Science ®Google Scholar
• Harwood HJ Jr, Petras SF,Shelly LD, et al. 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. J Biol Chem 2003;278:37099-111
   PubMed Web of Science ®Google Scholar
• Ferraro L, Tanganelli S, O'Connor WT, et al. γ-Hydroxybutyrate modulation of glutamate levels in the hippocampus: an in vivo and in vitro study. J Neurochem 2008;78(5):929-39
   Google Scholar
• Osei-Hyiaman D, DePetrillo M, Pacher P, et al. Endocannabinoid activation at hepatic CB1 receptors stimulates fatty acid synthesis and contributes to diet-induced obesity. J Clin Invest 2005;115(5):1298-305
   PubMed Web of Science ®Google Scholar
• Teixeira-Clerc F, Julien B, Grenard P, et al. CB1 cannabinoid receptor antagonism: a new strategy for the treatment of liver fibrosis. Nat Med 2006;12(6):671-6
   PubMed Web of Science ®Google Scholar
• Hansen DL, Toubro S, Stock MJ, et al. Thermogenic effects of sibutramine in humans. Am J Clin Nutr 1998;68(6):1180-6
   PubMed Web of Science ®Google Scholar
• Walsh WM, Leen E, Lean MEJ. The effect of sibutramine on resting energy expenditure and adrenaline-induced thermogenesis in obese females. Int J Obes Relat Metab Disord 1999;23(10):1009-15
   PubMed Web of Science ®Google Scholar
• Wagner BK, Kitami T, Gilbert TJ, et al. Large-scale chemical dissection of mitochondrial function. Nat Biotech 2008;26(3):343-51
   PubMed Web of Science ®Google Scholar
• Griffith LG, Swartz MA. Capturing complex 3D tissue physiology in vitro. Nat Rev Mol Cell Biol 2006;7(3):211-24
   PubMed Web of Science ®Google Scholar
• Khetani SR, Bhatia SN. Engineering tissues for in vitro applications. Curr Opin Biotechnol 2006;17(5):524-31
   PubMed Web of Science ®Google Scholar
• Kroehne V, Heschel I, Schügner F, et al. Use of a novel collagen matrix with oriented pore structure for muscle cell differentiation in cell culture and in grafts. J Cell Mol Med 2008;12(5a):1640-8
   Web of Science ®Google Scholar
• Fraker CA, Álvarez S, Papadopoulos P, et al. Enhanced oxygenation promotes -cell differentiation in vitro. Stem Cells 2007;25(12):3155-64
   Web of Science ®Google Scholar
• Leeson PD, Springthorpe B. The influence of drug-like concepts on decision-making in medicinal chemistry. Nat Rev Drug Disc 2007;6(11):881-90
   PubMed Web of Science ®Google Scholar
• Sproull DH. A comparison of sodium salicylate and 2:4-dinitrophenol as metabolic stimulants in vitro. Biochem J 1957;66(3):527-32
   PubMed Web of Science ®Google Scholar
• Harvey DG. On the metabolism of some aromatic nitro compounds by different species of animal. III. The toxicity of the dinitrophenols, with a note on the effects of high environmental temperatures. J Pharm Pharmacol 1959;11462-474
   Google Scholar
• Tainter ML, Cutting WC, Stockton AB. Use of dinitrophenol in nutritional disorders : a critical survey of clinical results. Am J Public Health Nations Health 1934;24(10):1045-53
   PubMedGoogle Scholar
• Fediuc S, Pimenta AS, Gaidhu MP, et al. Activation of AMP-activated protein kinase, inhibition of pyruvate dehydrogenase activity, and redistribution of substrate partitioning mediate the acute insulin-sensitizing effects of troglitazone in skeletal muscle cells. J Cell Physiol 2008;215(2):392-400
   PubMed Web of Science ®Google Scholar
• Cha BS, Ciaraldi TP, Park KS, et al. Impaired fatty acid metabolism in type 2 diabetic skeletal muscle cells is reversed by PPARγ agonists. Am J Physiol - Endocrinol Metab 2005;289(1):E151-9
   PubMed Web of Science ®Google Scholar
• Lazarow PB, De Duve C. A fatty acyl-CoA oxidizing system in rat liver peroxisomes; enhancement by clofibrate, a hypolipidemic drug. Proc Natl Acad Sci USA 1976;73(6):2043-6
   PubMed Web of Science ®Google Scholar
• Otto M, Breinholt J, Westergaard N. Metformin inhibits glycogen synthesis and gluconeogenesis in cultured rat hepatocytes. Diab, Obes and Metab 2008;5(3):189-94
   Google Scholar
• Kumar N, Dey CS. Metformin enhances insulin signalling in insulin-dependent and -independent pathways in insulin resistant muscle cells. Br J Pharmacol 2002;137(3):329-36
   PubMed Web of Science ®Google Scholar
• Hundal HS, Ramlal T, Reyes R, et al. Cellular mechanism of metformin action involves glucose transporter translocation from an intracellular pool to the plasma membrane in L6 muscle cells. Endocrinol 1992;131(3):1165-73
   PubMed Web of Science ®Google Scholar
• Cleasby ME, Dzamko N, Hegarty BD, et al. Metformin prevents the development of acute lipid-induced insulin resistance in the rat through altered hepatic signaling mechanisms. Diab 2004;53(12):3258-66
   PubMed Web of Science ®Google Scholar
• Stumvoll M, Nurjhan N, Perriello G, et al. Metabolic effects of metformin in non-insulin-dependent diabetes mellitus. N Engl J Med 1995;333(9):550-4
   PubMed Web of Science ®Google Scholar
• Gerondaes P, Alberti KG, Agius L. Interactions of inhibitors of carnitine palmitoyltransferase I and fibrates in cultured hepatocytes. Biochem J 1988;253(1):169-73
   PubMed Web of Science ®Google Scholar
• Oakes ND, Cooney GJ, Camilleri S, et al. Mechanisms of liver and muscle insulin resistance induced by chronic high-fat feeding. Diab 1997;46(11):1768-74
   PubMed Web of Science ®Google Scholar
• Hinderling VB, Schrauwen P, Langhans W, et al. The effect of etomoxir on 24-h substrate oxidation and satiety in humans. Am J Clin Nutr 2002;76(1):141-7
   PubMed Web of Science ®Google Scholar