The novel cholesterol-lowering drug SR-12813 inhibits cholesterol synthesis via an increased degradation of 3-hydroxy-3-methylglutaryl-coenzyme A reductase

Journal of Biological Chemistry

Volumn 271, Issue 24, 1996, Pages 14376-14382

  Berkhout, Theo A ^a   Simon, Helen M ^a   Patel, Dilip D ^b   Bentzen, Craig ^c   Niesor, Eric ^c   Jackson, Brian ^d   Suckling, Keith E ^a  

^a GLAXOSMITHKLINE   (United Kingdom)

^b HAMMERSMITH HOSPITAL   (United Kingdom)

^c Symphar SA   (Switzerland)

^d NONE

Author keywords

[No Author keywords available]

Indexed keywords

2 (3,5 DI TERT BUTYL 4 HYDROXYPHENYL)ETHENYL 1,1 BISPHOSPHONIC ACID; 25 HYDROXYCHOLESTEROL; HYDROXYMETHYLGLUTARYL COENZYME A REDUCTASE; HYPOCHOLESTEROLEMIC AGENT; LOW DENSITY LIPOPROTEIN RECEPTOR; MESSENGER RNA; MEVALONIC ACID; MEVINOLIN; SR 12813; UNCLASSIFIED DRUG;

ARTICLE; CHOLESTEROL BLOOD LEVEL; CHOLESTEROL SYNTHESIS; CONTROLLED STUDY; DRUG MECHANISM; ENZYME ACTIVITY; ENZYME DEGRADATION; HALF LIFE TIME; HEP 2 CELL; HUMAN; HUMAN CELL; PRIORITY JOURNAL; TRANSCRIPTION REGULATION;

ACETATES; ANTICHOLESTEREMIC AGENTS; BLOTTING, WESTERN; CARCINOMA, HEPATOCELLULAR; CELL LINE; CHOLESTEROL; DIPHOSPHONATES; HUMANS; HYDROXYCHOLESTEROLS; HYDROXYMETHYLGLUTARYL COA REDUCTASES; KINETICS; LANOSTEROL; LIPOPROTEINS, LDL; LIVER NEOPLASMS; LOVASTATIN; RECEPTORS, LDL; RNA, MESSENGER; TRANSCRIPTION, GENETIC; TRITIUM; TUMOR CELLS, CULTURED;

EID: 15844402429     PISSN: 00219258     EISSN: None     Source Type: Journal    
DOI: 10.1074/jbc.271.24.14376     Document Type: Article

References (48)

1. Suckling, K. E., Kerns, W. D., Jackson, B., Gee, A. N., Hickman, S. E., Nguyen, L., Niesor, E., and Bentzen, C. L. (1994) Atherosclerosis 109, 166-167
2. Gherardi, E., Thomas, K., Le Cras, T. D., Fitzsimmons, C., Moorby, C. D., and Bowyer, D. E. (1992) J. Cell Sci. 103, 531-539
3. Erickson, S. K., and Fielding, P. E. (1986) J. Lipid Res. 27, 875-883
4. Javitt, N. B. (1990) FASEB J. 4, 161-168
5. Rodwell, V. W., Nordstrom, J. L., and Mitchselen, J. J. (1916) Adv. Lipid Res. 14, 1-74
6. Goldstein, J. L., and Brown, M. S. (1984) J. Lipid Res. 25, 1450-1461
7. Nakanishi, M., Goldstein, J. L., and Brown, M. S. (1988) J. Biol. Chem. 263, 8929-8937
8. Peffley, D., and Sinensky, M. (1985) J. Biol. Chem. 260, 9949-9952
9. Goldstein, J. L., and Brown, M. S. (1990) Nature 343, 425-430
10. Roitelman, J., and Simoni, R. D. (1992) J. Biol. Chem. 267, 25264-25273
11. Giron, M. D., Havel, C. M., and Watson, J. A. (1994) Proc. Natl. Acad. Sci. U. S. A. 91, 6398-6402
12. Trzaskos, J. M., Favata, M. F., Fischer, R. T., and Stam, S. H. (1987) J. Biol. Chem. 262, 12261-12268
13. Trzaskos, J. M., Magolda, R. L., Favata, M. F., Fischer, R. T., Johnson, P. R., Chen, H. W., Ko, S. S., Leonard, D. A., and Gaylor, J. L. (1993) J. Biol. Chem. 268, 22591-22599
14. Mayer, R. J., Adams, J. L., Bossard, M. J., and Berkhout, T. A. (1991) J. Biol. Chem. 266, 20070-20078
15. Panini, S. R., Delate, T. A., and Sinensky, M. (1992) J. Biol. Chem. 267, 12647-12654
16. Clarke, P. R., and Hardie, D. G. (1990) EMBO J. 9, 2439-2446
17. Ness, G. C., McCreery, M. J., Sample, C. E., Smith, M., and Pendleton, L. C. (1985) J. Biol. Chem. 260, 16395-16399
18. Omkumar, R. V., and Ramasarma, T. (1993) Biochim. Biophys. Acta 1156, 267-274
19. von Gunten, C. F., and Sinensky, M. (1989) Biochim. Biophys. Acta 1001, 218-224
20. Harwood, H. J., Jr., Alvarez, I. M., Noyes, W. D., and Stacpoole, P. W. (1991) J. Lipid Res. 32, 1237-1252
21. Gil, G., Faust, J. R., Chin, D. J., Goldstein, J. L., and Brown, M. S. (1985) Cell 41, 249-258
22. Chun, K. T., and Simoni, R. D. (1992) J. Biol. Chem. 267, 4236-4246
23. Knight, B. L., Patel, D. D., Gavigan, S. J. P., and Soutar, A. K. (1988) Eur. J. Biochem. 178, 555-561
24. Berkhout, T. A., Havekes, L. M., Pearce, N. J., and Groot, P. H. (1990) Biochem. J. 272, 181-186
25. Bligh, E. G., and Dyer, W. J. (1959) Can. J. Biochem. 8, 911-917
26. Goldstein, J. L., Basu, S. K., and Brown, M. S. (1983) Methods Enzymol. 98, 241-260
27. Kennelly, P. J., and Rodwell, V. W. (1985) J. Lipid Res. 26, 903-914
28. van Driel, I. R., Davis, G. D., Goldstein, J. L., and Brown, M. S. (1987) J. Biol. Chem. 262, 16127-16134
29. Laemmli, U. K. (1970) Nature 227, 680-685
30. Hardeman, E. C., Jenke, H. S., and Simoni, R. D. (1983) J. Biol. Chem. 80, 1516-1520
31. Edwards, P. A., Lan, S. F., Tanaka, R. D., and Fogelman, A. M. (1983) J. Biol. Chem. 258, 7272-7275
32. Gillespie, J. G., and Hardie, D. G. (1992) FEBS Lett. 306, 59-62
33. Wilkins, G. M., and Leake, D. S. (1994) Biochim. Biophys. Acta 1211, 69-78
34. Albrightson, C. R., Bugelski, P. J., Berkhout, T. A., Jackson, B., Kerns, W. D., Organ, A. J., and Badger, A. M. (1995) J. Pharmacol. Exp. Ther. 272, 689-698
35. Molowa, D. T., and Cimis, G. M. (1989) Biochem. J. 260, 731-736
36. Cohen, L. H., and Griffioen, M. (1988) Biochem. J. 255, 61-67
37. Berkhout, T. A., Simon, H., Niesor, E., Bentzen, C. L., and Suckling, K. E. (1994) Atherosclerosis 109, 167
38. Beg, Z. H., Stonik, J. A., and Brewer, H. B., Jr. (1987) Metabolism 36, 900-917
39. Parker, R. A., Miller, S. J., and Gibson, D. M. (1989) J. Biol. Chem. 264, 4877-4887
40. Niesor, E., Maechler, P., Lolli, D., Villemin, P., Gee, A., Suckling, K. E., Kerns, W. D., and Bentzen, C. L. (1994) Atherosclerosis 109, 167
41. Sinensky, M., and Logel, J. (1983) J. Biol. Chem. 268, 8547-8549
42. Correll, C. C., and Edwards, P. A. (1994) J. Biol. Chem. 269, 633-638
43. Peffley, D. M. (1992) Somatic Cell Mol. Genet. 18, 19-32
44. Parker, R. A., Pearce, B. C., Clark, R. W., Gordon, D. A., and Wright, J. J. (1993) J. Biol. Chem. 268, 11230-11238
45. Bradfute, D. L., and Simoni, R. D. (1994) J. Biol. Chem. 269, 6645-6650
46. Correll, C. C., Ng, L., and Edwards, P. A. (1994) J. Biol. Chem. 269, 17390-17393
47. Inoue, S., Bar-Nun, S., Roitelman, J., and Simoni, R. D. (1991) J. Biol. Chem. 266, 13311-13317
48. Kito, M., and Urade, R. (1995) Proc. Jpn. Acad. Ser. B Phys. Biol. Sci. 71, 189-192