References
- Brown MS, Goldstein JL. The SREBP pathway: regulation of cholesterol metabolism by proteolysis of a membrane‑bound transcription factor. Cell 89(3), 331–340 (1997).
- Poirier S, Mayer G, Benjannet S et al. The proprotein convertase PCSK9 induces the degradation of low density lipoprotein receptor (LDLR) and its closest family members VLDLR and ApoER2. J. Biol Chem. 283(4), 2363–2372 (2008).
- Seidah NG, Prat A. The biology and therapeutic targeting of the proprotein convertases. Nat. Rev. Drug Discov. 11(5), 367–383 (2012).
- Cohen JC, Boerwinkle E, Mosley TH Jr, Hobbs HH. Sequence variations in PCSK9, low LDL, and protection against coronary heart disease. N. Engl. J. Med. 354(12), 1264–1272 (2006).
- Graham MJ, Lemonidis KM, Whipple CP et al. Antisense inhibition of proprotein convertase subtilisin/kexin type 9 reduces serum LDL in hyperlipidemic mice. J. Lipid Res. 48(4), 763–767 (2007).
- Frank‑Kamenetsky M, Grefhorst A, Anderson NN et al. Therapeutic RNAi targeting PCSK9 acutely lowers plasma cholesterol in rodents and LDL cholesterol in nonhuman primates. Proc. Natl Acad. Sci. USA 105(33), 11915–11920 (2008).
- Stein EA, Mellis S, Yancopoulos GD. Effect of a monoclonal antibody to PCSK9 on LDL cholesterol. N. Engl. J. Med. 366(12), 1108–1118 (2012).
- McKenney JM, Koren MJ, Kereiakes DJ, Hanotin C, Ferrand AC, Stein EA. Safety and efficacy of a monoclonal antibody to proprotein convertase subtilisin/kexin type 9 serine protease, SAR236553/REGN727, in patients with primary hypercholesterolemia receiving ongoing stable atorvastatin therapy. J. Am. Coll. Cardiol. 59(25), 2344–2353 (2012).
- Tavori H, Fazio S, Linton MF. PCSK9: a novel target for LDL lowering: promise and progress. Clin. Lipidol. 7(6), 611–615 (2012).
- Stein EA, Gipe D, Bergeron J et al. Effect of a monoclonal antibody to PCSK9, REGN727/SAR236553, to reduce lowdensity lipoprotein cholesterol in patients with heterozygous familial hypercholesterolaemia on stable statin dose with or without ezetimibe therapy: a Phase 2 randomised controlled trial. Lancet 380(9836), 29–36 (2012).
- Rhainds D, Arsenault BJ, Tardif J‑C. PCSK9 inhibition and LDL cholesterol lowering: the biology of an attractive therapeutic target and critical review of the latest clinical trials. Clin. Lipidol. 7(6), 621–640 (2012).
- Gusarova V, Howard VG, Okamoto H. Reduction of LDL‑C by a monoclonal antibody to PCSK9 in rodents and nonhuman primates. Clin. Lipidol. 7(6), 737–743 (2012).