A highly sensitive high-throughput luminescence assay for malonyl-CoA decarboxylase

Analytical Biochemistry

Volumn 376, Issue 1, 2008, Pages 122-130

  Lo, Mei Chu ^a   Wang, Minghan ^a   Kim, Ki Won ^a   Busby, James ^a   Yamane, Harvey ^a   Zondlo, James ^a   Yuan, Chester ^a   Young, Stephen W ^a   Xiao, Shou Hua ^a  

^a AMGEN INC   (United States)

Author keywords

Coupled assay; High throughput screening; IC50; Inhibitor; kcat; Km; Luminescence assay; Malonyl CoA decarboxylase

Indexed keywords

ENZYMES; FLUORESCENCE; MITOCHONDRIA; OXIDATION;

DECARBOXYLASES; HIGH THROUGHPUT SCREENING; IC50; INHIBITOR; KCAT; LUMINESCENCE ASSAY;

FATTY ACIDS;

MALONYL COENZYME A DECARBOXYLASE;

ARTICLE; AUTOMATION; ENZYME ACTIVITY; ENZYME ASSAY; HIGH THROUGHPUT SCREENING; LUMINESCENCE; PRIORITY JOURNAL; SENSITIVITY AND SPECIFICITY;

EID: 41549085203     PISSN: 00032697     EISSN: 10960309     Source Type: Journal    
DOI: 10.1016/j.ab.2008.01.033     Document Type: Article

References (21)

1. Stanley W.C., Lopaschuk G.D., Hall J.L., and McCormack J.G. Regulation of myocardial carbohydrate metabolism under normal and ischaemic conditions. Potential for pharmacological interventions. Cardiovasc. Res. 33 (1997) 243-257
2. McGarry J.D., and Brown N.F. The mitochondrial carnitine palmitoyltransferase system. From concept to molecular analysis. Eur. J. Biochem. 244 (1997) 1-14
3. Dyck J.R., and Lopaschuk G.D. Malonyl CoA control of fatty acid oxidation in the ischemic heart. J. Mol. Cell. Cardiol. 34 (2002) 1099-1109
4. Lopaschuk G.D., Collins-Nakai R., Olley P.M., Montague T.J., McNeil G., Gayle M., Penkoske P., and Finegan B.A. Plasma fatty acid levels in infants and adults after myocardial ischemia. Am. Heart J. 128 (1994) 61-67
5. Kudo N., Barr A.J., Barr R.L., Desai S., and Lopaschuk G.D. High rates of fatty acid oxidation during reperfusion of ischemic hearts are associated with a decrease in malonyl-CoA levels due to an increase in 5'-AMP-activated protein kinase inhibition of acetyl-CoA carboxylase. J. Biol. Chem. 270 (1995) 17513-17520
6. Stanley W.C., and Sabbah H.N. Metabolic therapy for ischemic heart disease: the rationale for inhibition of fatty acid oxidation. Heart Fail. Rev. 10 (2005) 275-279
7. Folmes C.D., and Lopaschuk G.D. Role of malonyl-CoA in heart disease and the hypothalamic control of obesity. Cardiovasc. Res. 73 (2007) 278-287
8. Lopaschuk G.D., and Stanley W.C. Malonyl-CoA decarboxylase inhibition as a novel approach to treat ischemic heart disease. Cardiovasc. Drugs Ther. 20 (2006) 433-439
9. Cheng J.F., Chen M., Wallace D., Tith S., Haramura M., Liu B., Mak C.C., Arrhenius T., Reily S., Brown S., Thorn V., Harmon C., Barr R., Dyck J.R., Lopaschuk G.D., and Nadzan A.M. Synthesis and structure-activity relationship of small-molecule malonyl coenzyme A decarboxylase inhibitors. J. Med. Chem. 49 (2006) 1517-1525
10. Cheng J.F., Huang Y., Penuliar R., Nishimoto M., Liu L., Arrhenius T., Yang G., O'leary E., Barbosa M., Barr R., Dyck J.R., Lopaschuk G.D., and Nadzan A.M. Discovery of potent and orally available malonyl-CoA decarboxylase inhibitors as cardioprotective agents. J. Med. Chem. 49 (2006) 4055-4058
11. Wallace D.M., Haramura M., Cheng J.F., Arrhenius T., and Nadzan A.M. Novel trifluoroacetophenone derivatives as malonyl-CoA decarboxylase inhibitors. Bioorg. Med. Chem. Lett. 17 (2007) 1127-1130
12. Dyck J.R., Cheng J.F., Stanley W.C., Barr R., Chandler M.P., Brown S., Wallace D., Arrhenius T., Harmon C., Yang G., Nadzan A.M., and Lopaschuk G.D. Malonyl coenzyme A decarboxylase inhibition protects the ischemic heart by inhibiting fatty acid oxidation and stimulating glucose oxidation. Circ. Res. 94 (2004) e78-e84
13. Kim Y.S., and Kolattukudy P.E. Purification and properties of malonyl- CoA decarboxylase from rat liver mitochondria and its immunological comparison with the enzymes from rat brain, heart, and mammary gland. Arch. Biochem. Biophys. 190 (1978) 234-246
14. Zhou D., Yuen P., Chu D., Thon V., McConnell S., Brown S., Tsang A., Pena M., Russell A., Cheng J.F., Nadzan A.M., Barbosa M.S., Dyck J.R., Lopaschuk G.D., and Yang G. Expression, purification, and characterization of human malonyl-CoA decarboxylase. Protein Expr. Purif. 34 (2004) 261-269
15. Studier F.W., and Moffatt B.A. Use of bacteriophage T7 RNA polymerase to direct selective high-level expression of cloned genes. J. Mol. Biol. 189 (1986) 113-130
16. Zhang J.H., Chung T.D., 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
17. Kim K.W., Yamane H., Zondlo J., Busby J., and Wang M. Expression, purification, and characterization of human acetyl-CoA carboxylase 2. Protein Expr. Purif. 53 (2007) 16-23
18. Gao J., Waber L., Bennett M.J., Gibson K.M., and Cohen J.C. Cloning and mutational analysis of human malonyl-coenzyme A decarboxylase. J. Lipid Res. 40 (1999) 178-182
19. Fan F., and Wood K.V. Bioluminescent assays for high-throughput screening. Assay Drug Dev. Technol. 5 (2007) 127-136
20. Lee G.Y., Bahk Y.Y., and Kim Y.S. Rat malonyl-CoA decarboxylase; cloning, expression in E. coli and its biochemical characterization. J. Biochem. Mol. Biol. 35 (2002) 213-219
21. Sacksteder K.A., Morrell J.C., Wanders R.J., Matalon R., and Gould S.J. MCD encodes peroxisomal and cytoplasmic forms of malonyl-CoA decarboxylase and is mutated in malonyl-CoA decarboxylase deficiency. J. Biol. Chem. 274 (1999) 24461-24468