Proprotein convertase substilisin/kexin type 9 antagonism reduces low-density lipoprotein cholesterol in statin-treated hypercholesterolemic nonhuman primates.

@article{Liang2012ProproteinCS,
  title={Proprotein convertase substilisin/kexin type 9 antagonism reduces low-density lipoprotein cholesterol in statin-treated hypercholesterolemic nonhuman primates.},
  author={Hong Liang and Javier Chaparro-Riggers and Pavel Strop and Tao Geng and Janette E Sutton and Daniel Tsai and Lanfang Bai and Yasmina Noubia Abdiche and Jeanette Dilley and Jessica Yu and Si Wu and Sherman Michael Chin and Nicole A Lee and Andrea Rossi and John C Lin and Arvind Rajpal and Jaume Pons and David L. Shelton},
  journal={The Journal of pharmacology and experimental therapeutics},
  year={2012},
  volume={340 2},
  pages={228-36}
}
Proprotein convertase substilisin/kexin type 9 (PCSK9) promotes the degradation of low-density lipoprotein (LDL) receptor (LDLR) and thereby increases serum LDL-cholesterol (LDL-C). We have developed a humanized monoclonal antibody that recognizes the LDLR binding domain of PCSK9. This antibody, J16, and its precursor mouse antibody, J10, potently inhibit PCSK9 binding to the LDLR extracellular domain and PCSK9-mediated down-regulation of LDLR in vitro. In vivo, J10 effectively reduces serum… CONTINUE READING
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