The crystal structure of PCSK9: a regulator of plasma LDL-cholesterol

Structure. 2007 May;15(5):545-52. doi: 10.1016/j.str.2007.04.004.

Abstract

Proprotein convertase subtilisin kexin type 9 (PCSK9) has been shown to be involved in the regulation of extracellular levels of the low-density lipoprotien receptor (LDLR). Although PCSK9 is a subtilase, it has not been shown to degrade the LDLR, and its LDLR-lowering mechanism remains uncertain. Here we report the crystal structure of human PCSK9 at 2.3 A resolution. PCSK9 has subtilisin-like pro- and catalytic domains, and the stable interaction between these domains prevents access to PCSK9's catalytic site. The C-terminal domain of PCSK9 has a novel protein fold and may mediate protein-protein interactions. The structure of PCSK9 provides insight into its biochemical characteristics and biological function.

MeSH terms

  • Cholesterol, LDL / antagonists & inhibitors
  • Cholesterol, LDL / blood*
  • Crystallography, X-Ray
  • Humans
  • Peptide Fragments / chemistry
  • Peptide Fragments / physiology
  • Proprotein Convertase 9
  • Proprotein Convertases
  • Protein Folding
  • Protein Interaction Mapping
  • Serine Endopeptidases / chemistry*
  • Serine Endopeptidases / physiology*

Substances

  • Cholesterol, LDL
  • Peptide Fragments
  • PCSK9 protein, human
  • Proprotein Convertase 9
  • Proprotein Convertases
  • Serine Endopeptidases

Associated data

  • PDB/2PMW