Regulation of proprotein convertase subtilisin/kexin type 9: Therapeutical perspectives

Atherosclerosis

Volumn 217, Issue 1, 2011, Pages 77-79

  Chan, Dick C ^a  

^a UNIVERSITY OF WESTERN AUSTRALIA   (Australia)

Author keywords

Hypercholesterolaemia; LDL metabolism; PCSk9 and lipid regulating therapy

Indexed keywords

ANTISENSE OLIGONUCLEOTIDE; ATORVASTATIN; BEZAFIBRATE; FENOFIBRATE; FURIN; GEMFIBROZIL; HYDROXYMETHYLGLUTARYL COENZYME A REDUCTASE INHIBITOR; LOW DENSITY LIPOPROTEIN RECEPTOR; MONOCLONAL ANTIBODY; PEROXISOME PROLIFERATOR ACTIVATED RECEPTOR ALPHA AGONIST; PROPROTEIN CONVERTASE SUBTILISIN KEXIN TYPE 9; ROSUVASTATIN; SERINE PROTEINASE; SMALL INTERFERING RNA; STEROL REGULATORY ELEMENT BINDING PROTEIN 2; UNCLASSIFIED DRUG;

ABSORPTION; CHOLESTEROL SYNTHESIS; DYSLIPIDEMIA; HUMAN; HYPERCHOLESTEROLEMIA; HYPERLIPIDEMIA; IMPAIRED GLUCOSE TOLERANCE; INSULIN RESISTANCE; LIFESTYLE MODIFICATION; LIPOPROTEIN METABOLISM; NON INSULIN DEPENDENT DIABETES MELLITUS; NONHUMAN; NOTE; PRIORITY JOURNAL; PROTEIN EXPRESSION; REGULATORY MECHANISM; SAMPLE SIZE; TREATMENT DURATION; UPREGULATION;

ADIPOKINES; BEZAFIBRATE; FEMALE; FENOFIBRATE; HUMANS; MALE; PROPROTEIN CONVERTASES; SERINE ENDOPEPTIDASES;

EID: 79960270412     PISSN: 00219150     EISSN: 18791484     Source Type: Journal    
DOI: 10.1016/j.atherosclerosis.2011.02.040     Document Type: Note

References (26)

1. Goldstein J.L., Brown M.S. The LDL receptor. Arterioscler Thromb Vasc Biol 2009, 29:431-438.
2. Marsh J.B., Welty F.K., Lichtenstein A.H., Lamon-Fava S., Schaefer E.J. Apolipoprotein B metabolism in humans: studies with stable isotope-labeled amino acid precursors. Atherosclerosis 2002, 162:227-244.
3. Lambert G., Charlton F., Rye K.A., Piper D.E. Molecular basis of PCSK9 function. Atherosclerosis 2009, 203:1-7.
4. Horton J.D., Cohen J.C., Hobbs H.H. PCSK9: a convertase that coordinates LDL catabolism. J Lipid Res 2009, 50:172-177.
5. Abifadel M., Varret M., Rabes J.P., et al. Mutations in PCSK9 cause autosomal dominant hypercholesterolemia. Nat Genet 2003, 34:154-156.
6. Cohen J.C., Boerwinkle E., Mosley T.H., Hobbs H.H. Sequence Variations in PCSK9, low LDL, and protection against coronary heart disease. N Engl J Med 2006, 354:1264-1272.
7. Chan D.C., Lambert G., Barrett P.H.R., Rye K.A., Ooi E.M.M., Watts G.F. Plasma proprotein convertase subtilisin/kexin type 9: a marker of LDL apolipoprotein B-100 catabolism?. Clin Chem 2009, 55:2049-2052.
8. Cariou B., Ouguerram K., Zaïr Y., et al. PCSK9 dominant negative mutant results in increased LDL catabolic rate and familial hypobetalipoproteinemia. Arterioscler Thromb Vasc Biol 2009, 29:2191-2197.
9. Noguchi T, Kobayashi J, Yagi K, et al. Comparison of the effects of bezafibrate and fenofibrate on circulating proprotein convertase subtilisin/kexin type 9 and adipocytokine levels in dyslipidemic subjects with impaired glucose tolerance or type 2 diabetes mellitus: results from a crossover study. Atherosclerosis, in press. doi:10.1016/j.atherosclerosis.2011.02.012.
10. Mayne J., Dewpura T., Raymond A., et al. Plasma PCSK9 levels are significantly modified by statins and fibrates in humans. Lipids Health Dis 2008, 7:22.
11. Troutt J.S., Alborn W.E., Cao G., Konrad R.J. Fenofibrate treatment increases human serum proprotein convertase subtilisin kexin type 9 levels. J Lipid Res 2010, 51:345-351.
12. Lambert G., Ancellin N., Charlton F., et al. Plasma PCSK9 concentrations correlate with LDL and total cholesterol in diabetic patients and are decreased by fenofibrate treatment. Clin Chem 2008, 54:1038-1045.
13. Chan D.C., Hamilton S.J., Rye K.A., et al. Fenofibrate concomitantly decreases serum proprotein convertase subtilisin/kexin type 9 and very-low-density lipoprotein particle concentrations in statin-treated type 2 diabetic patients. Diabetes Obes Metab 2010, 12:752-756.
14. Jeong H.J., Lee H.S., Kim K.S., Kim Y.K., Yoon D., Park S.W. Sterol-dependent regulation of proprotein convertase subtilisin/kexin type 9 expression by sterol-regulatory element binding protein-2. J Lipid Res 2008, 49:399-409.
15. Careskey H.E., Davis R.A., Alborn W.E., Troutt J.S., Cao G., Konrad R.J. Atorvastatin increases human serum levels of proprotein convertase subtilisin/kexin type 9. J Lipid Res 2008, 49:394-398.
16. Welder G., Zineh I., Pacanowski M.A., et al. High-dose atorvastatin causes a rapid sustained increase in human serum PCSK9 and disrupts its correlation with LDL cholesterol. J Lipid Res 2010, 51:2714-2721.
17. Schneider A., Strange E.F., Ditschuneit H.H., Ditschuneit H. Fenofibrate treatment inhibits HMG-CoA reductase activity in mononuclear cells from hyperlipoproteinemic patients. Atherosclerosis 1985, 56:257-262.
18. Kourimate S., Le May C., Langhi C., et al. Dual mechanisms for the fibrate-mediated repression of proprotein convertase subtilisin/kexin type 9. J Biol Chem 2008, 283:9666-9673.
19. Essalmani R., Susan-Resiga D., Chamberland A., et al. In vivo evidence that furin from hepatocytes inactivates PCSK9. J Biol Chem 2011, 286:4257-4263.
20. Costet P., Hoffmann M.M., Cariou B., Guyomarc'h Delasalle G., Konrad T., Winkler K. Plasma PCSK9 is increased by fenofibrate and atorvastatin in a non-additive fashion in diabetic patients. Atherosclerosis 2010, 212:246-251.
21. Steinberg D., Witztum J.L. Inhibition of PCSK9: a powerful weapon for achieving ideal LDL cholesterol levels. Proc Natl Acad Sci USA 2009, 106:9546-9547.
22. Frank-Kamenetsky M., Grefhorst A., Anderson N.N., et al. Therapeutic RNAi targeting PCSK9 acutely lowers plasma cholesterol in rodents and LDL cholesterol in nonhuman primates. Proc Natl Acad Sci USA 2008, 105:11915-11920.
23. Graham M.J., Lemonidis K.M., Whipple C.P., et al. Antisense inhibition of proprotein convertase subtilisin/kexin type 9 reduces serum LDL in hyperlipidemic mice. J Lipid Res 2007, 48:763-767.
24. Chan J.C.Y., Piper D.E., Cao Q., et al. A proprotein convertase subtilisin/kexin type 9 neutralizing antibody reduces serum cholesterol in mice and nonhuman primates. Proc Natl Acad Sci USA 2009, 106:9820-9825.
25. Ason B., Tep S., Davis H.R., et al. Improved efficacy for ezetimibe and rosuvastatin by attenuating the induction of PCSK9. J Lipid Res 2011, 10.1194/jlr.M013664.
26. Le May C., Kourimate S., Langhi C., et al. Proprotein convertase subtilisin kexin type 9 null mice are protected from postprandial triglyceridemia. Arterioscler Thromb Vasc Biol 2009, 29:684-690.