A High-throughput two-phase partition assay to measure the activity of lipid-metabolizing enzymes

Analytical Biochemistry

Volumn 358, Issue 2, 2006, Pages 266-272

  Kristie, James ^a   Toth, Joshuaine G ^a   Silverstrim, Christine ^a   Pickett, Walter ^a   Landro, James A ^a  

^a BAYER CORPORATION   (United States)

Author keywords

Acetyl CoA carboxylase (EC 6.4.1.2); Fatty acid synthase (EC 2.3.1.85); High throughput screening; Lipid; Phase partition

Indexed keywords

ENZYMES; LIPIDS; SCINTILLATION; SOLVENT EXTRACTION;

ACETYL-COA CARBOXYLASE; ENZYMATIC REACTION; FATTY ACID SYNTHASE; HIGH THROUGHPUT SCREENING; KINETIC CHARACTERIZATION; PHASE PARTITION; REACTION SUBSTRATES; TWO-PHASE PARTITIONS;

FATTY ACIDS;

ACETYL COENZYME A; ENZYME; FATTY ACID SYNTHASE; LIPID; LIPID METABOLIZING ENZYME; UNCLASSIFIED DRUG;

ANIMAL CELL; AQUEOUS SOLUTION; ARTICLE; CONTROLLED STUDY; ENZYME ACTIVITY; ENZYME ASSAY; ENZYME KINETICS; ENZYME MECHANISM; ENZYME SUBSTRATE; HIGH THROUGHPUT SCREENING; ISOTOPE LABELING; LIPID METABOLISM; NONHUMAN; PHASE PARTITIONING; PHASE SEPARATION; PRIORITY JOURNAL; RAT; SEPARATION TECHNIQUE;

EID: 33750034182     PISSN: 00032697     EISSN: 10960309     Source Type: Journal    
DOI: 10.1016/j.ab.2006.07.036     Document Type: Article

References (42)

1. Harwood Jr. H.J. Acetyl-CoA carboxylase inhibtion for the treatment of metabolic syndrome. Curr. Opin. Invest. Drugs 5 (2004) 283-289
2. Kuhajda F.P. Fatty acid synthase and human cancer: new perspectives on its role in tumor biology. Nutrition 16 (2000) 202-208
3. Baron A., Migita T., Tang D., and Loda M. Fatty acid synthase: a metabolic oncogene in prostate cancer?. J. Cell. Biochem. 91 (2004) 47-53
4. Reaven G.M. Banting lecture 1988. Role of insulin resistance in human disease. Diabetes 37 (1988) 1595-1607
5. Ford E.S., Giles W.H., and Dietz W.H. Prevalence of the metabolic syndrome among US adults: findings from the third national health and nutritional examination survey. J. Am. Med. Assoc. 287 (2002) 356-359
6. Isomaa B., Almgren P., Tuomi T., Forsen B., Lahti K., Nissen M., Taskinen M.-R., and Groop L. Cardiovascular morbidity and mortality associated with the metabolic syndrome. Diabetes Care 24 (2001) 683-689
7. McGarry J.D., and Brown N.F. The mitochondrial carnitine transport system. From concept to molecular analysis. Eur. J. Biochem. 244 (1997) 1-14
8. Rasmussen B.B., Holmback U.C., Volpi E., Morio-Liondore B., Paddon-Jones D., and Wolfe R.R. Malonyl coenzyme A and the regulation of functional carntine palmitoyltransferase-1 activity and fat oxidation in human skeletal muscle. J. Clin. Invest. 110 (2002) 1687-1693
9. Abu-Elheiga L., Oh W., Kordari P., and Wakil S.J. Acetyl-CoA carboxylase 2 mutant mice are protected against obesity and diabetes induced by high-fat/high-carbohydrate diets. Proc. Natl. Acad. Sci. USA 100 (2003) 10207-10212
10. Harwood Jr. H.J., Petras S.F., Shelly L.D., Zaccaro L.M., Perry D.A., Makowski M.R., Hargrove D.M., Martin K.A., Tracey W.R., Martin W.H., Mularski C.J., and Eisenbeis S.A. 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 hepatocytes and in expreimental animals. J. Biol. Chem. 278 (2003) 37099-37111
11. Pizer E.S., Jackisch C., Wood F.D., Pasternack G.R., Davidson N.E., and Kuhajda F.P. Inhibition of fatty acid synthesis induces programmed cell death in human breast cancer cells. Cancer Res. 56 (1996) 2745-2747
12. Pizer E.S., Chrest F.J., DiGiuseppe J.A., and Han W.F. Pharmacological inhibitors of mammalian fatty acid synthase suppress DNA replication and induce apoptosis in tumor cell lines. Cancer Res. 58 (1998) 4611-4615
13. De Schrijver E., Brusselmans K., Heyns W., Verhoeven G., and Swinnen J.V. RNA interference-mediated silencing of the fatty acid synthase gene attenuates growth and induces morphological changes and apoptosis of LNCaP prostate cancer cells. Cancer Res. 63 (2003) 3799-3804
14. Pizer E.S., Wood F.D., Heine H.S., Romantsev F.E., Pasternack G.R., and Kuhajda F.P. Inhibition of fatty acid synthesis delays disease progression in a xenograft model of ovarian cancer. Cancer Res. 56 (1996) 1189-1193
15. Wakil S.J. A malonic acid derivative as an intermediate in fatty acid synthesis. J. Am. Chem. Soc. 80 (1958) 6465
16. Martin D.B., Horning M.G., and Vagelos P.R. Fatty acid synthesis in adipose tissue. I. Purification and properties of a long chain fatty acid synthesizing system. J. Biol. Chem. 263 (1961) 663-668
17. Jayakumar A., Huang W.-Y., Raetz B., Chirala S.S., and Wakil S.J. Cloning and expression of the multifunctional human fatty acid synthase and its subdomains in Escherichia coli. Proc. Natl. Acad. Sci. USA 93 (1996) 14509-14514
18. Abu-Elheiga L., Jayakumar A., Baldini A., Chirala S.S., and Wakil S.J. Human acetyl-CoA carboxylase: characterization, molecular cloning, and evidence for two isoforms. Proc. Natl. Acad. Sci. USA 92 (1995) 4011-4015
19. Ha J., Lee J.-K., Kim K.-S., Witters L.A., and Kim K.-H. Cloning of human acetyl-CoA carboxylase-β and its unique features. Proc. Natl. Acad. Sci. USA 93 (1996) 11466-11470
20. Menendez J.A., Vellon L., Mehmi I., Oza B.P., Ropero S., Colomer R., and Lupu R. Inhibition of fatty acid synthase (FAS) suppresses HER2/neu (erbB-2) oncogene overexpression in cancer cells. Proc. Natl. Acad. Sci. USA 101 (2004) 10715-10720
21. Schmid B., Rippmann J.F., Tadayyon M., and Hamilton B.S. Inhibition of fatty acid synthase prevents preadipocyte differentiation. Biophys. Res. Commun. 328 (2005) 1073-1082
22. Thampy K.G., and Wakil S.J. Activation of acetyl-CoA carboxylase. Purification and properties of manganese(2+)-dependent phosphatase. J. Biol. Chem. 260 (1985) 6318-6323
23. Herbert D., Price L.J., Alban C., Dehaye L., Job D., Cole D.J., Pallett K.E., and Harwood J.L. Kinetic studies on two isoforms of acetyl-CoA carboxylase from maize leaves. Biochem. J. 318 (1996) 997-1006
24. Wada H., Shintani D., and Ohlrogge J. Why do mitochondria synthesize fatty acids? Evidence for involvement in lipoic acid production. Proc. Natl. Acad. Sci. USA 94 (1997) 1591-1596
25. Hsu R.Y., Wasson G., and Porter J.W. The purification and properties of the fatty acid synthetase of pigeon liver. J. Biol. Chem. 240 (1965) 3736-3746
26. Witters L.A., and Vogt B. A new method for the isolation of rat liver acetyl-CoA carboxylase. J. Lipid Res. 22 (1981) 364-369
27. Tong L. Acetyl-coenzyme A carboxylase: crucial metabolic enzyme and attractive target for drug discovery. Cell. Mol. Life Sci. 62 (2005) 1784-1803
28. McClure W.R. A kinetic analysis of coupled enzyme assays. Biochemistry 8 (1969) 2782-2786
29. Duggleby R.G. Determination of the kinetic properties of enzymes catalyzing coupled reaction sequences. Biochim. Biophys. Acta 744 (1983) 249-259
30. Easterby J.S. Coupled enzyme assays. General expression for the transient. Biochim. Biophys. Acta 293 (1973) 552-558
31. Hashimoto T., and Numa S. Kinetic Studies on the reaction mechanism and citrate activation of liver acetyl coenzyme A carboxylase. Eur. J. Biochem. 18 (1971) 319-331
32. Trumble G.E., Smith M.A., and Winder W.W. Purification and characterization of rat skeletal muscle acetyl-CoA carboxylase. Eur. J. Biochem. 231 (1995) 192-198
33. Shi Y., Luo W., Tian W.-X., Zhang T., and Zhou H.-M. Inactivation and conformational changes of fatty acid synthase from chicken liver during unfolding by sodium dodecyl sulfate. Int. J. Biochem. Cell Biol. 30 (1998) 1319-1330
34. Rangan V., and Smith S.S. Alteration of the substrate specificity of the malonyl-CoA/acetyl-CoA:acyl carrier protein S-acyltransferase domain of the multifunctional fatty acid synthase by mutation of a single arginine residue. J. Biol. Chem. 272 (1997) 11975-11978
35. Jayakumar A., Tai M.-H., Huang W.-Y., Al-feel W., Hsu M., Abu-Elheiga L., Chirala S.S., and Wakil S.J. Human fatty acid synthase: properties and molecular cloning. Proc. Natl. Acad. Sci. USA 92 (1995) 8695-8699
36. Zhang J.-H., Chung T.D.Y., and Oldenburg K.R. A simple statistical parameter for use in evaluation and validation of high throughput screening assays. J. Biomol. Screen 4 (1999) 67-73
37. Arslanian M.J., and Wakil S.J. Fatty acid synthase from chicken liver. Methods Enzymol. 35 (1975) 59-65
38. Singh N., Wakil S.J., and Stoops J.K. On the question of half- or full-site reactivity of animal fatty acid synthetase. J. Biol. Chem. 259 (1984) 3605-3611
39. Levert K., Lloyd L.R.B., and Waldrop G.L. Do cysteine 230 and lysine 238 of biotin carboxylase play a role in the activation of biotin?. Biochemistry 39 (2000) 4122-4128
40. Winder W.W., Holmes B.F., Rubink D.S., Jensen E.B., Chen M., and Holloszy J.O. Activation of AMP-activated protein kinase increases mitochondrial enzymes in skeletal muscle. J. Appl. Physiol. 88 (2000) 2219-2226
41. Weiss D.R., and Glickman J.F. Characterization of fatty acid synthase activity using scintillation proximity. ASSAY Drug Dev. Technol. 1 (2003) 161-166
42. Mintzer R.J., Appell K.C., Cole A., Johns A., Paglia R., Polokoff M.A., Tabas I., Snider M., and Meurer-Ogden J.A. A novel high-throughput screening format to identify inhibitors of secreted acid sphingomyelinase. J. Biomol. Screen. 10 (2005) 225-234