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Literature summary extracted from

  • 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 (2008), J. Lipid Res., 49, 399-409.
    View publication on PubMed

Activating Compound

EC Number Activating Compound Comment Organism Structure
3.4.21.61 lovastatin suppresses endogenous synthesis of sterols, increases both the proteins and mRNAs for PCSK9. 10 mM can reverse the increase of PCSK9 expression by lovastatin Homo sapiens
3.4.21.61 additional information depletion of sterols induces PCSK9 in a time-dependent manner Homo sapiens
3.4.21.61 additional information PCSK9 protein and mRNA are increased by refeeding after fasting. Supplementation with 2% cholesterol in the diet prevents the increase in PCSK9 Mus musculus
3.4.21.61 sodium mevalonate suppresses endogenous synthesis of sterols, PCSK9 is further increased Homo sapiens
3.4.21.61 sterol-regulatory element binding protein-1 dramatically increases the promoter activity of PCSK9 Homo sapiens
3.4.21.61 sterol-regulatory element binding protein-2 dramatically increases the promoter activity of PCSK9 Homo sapiens
3.4.21.61 sterol-regulatory element binding protein-2 predominantly mediates sterol-dependent regulation of PCSK9 in vivo Mus musculus

Application

EC Number Application Comment Organism
3.4.21.61 additional information expression of PCSK9 is regulated by sterol at the transcriptional level in HepG2 cells and that both SREBP-1 and SREBP-2 can transcriptionally activate PCSK9 via sterol-regulatory element in its proximal promoter region in vitro Homo sapiens

Cloned(Commentary)

EC Number Cloned (Comment) Organism
3.4.21.61 into vector pET-21a(+) Homo sapiens
3.4.21.61 ligated into vector pCR2.1-Topo and subcloned into vector pET-21a(+) Mus musculus

Inhibitors

EC Number Inhibitors Comment Organism Structure
3.4.21.61 additional information PCSK9 protein and mRNA are decreased significantly by fasting Mus musculus
3.4.21.61 sterol completely blocks increase in PCSK9 mRNA by lovastatin Homo sapiens

Organism

EC Number Organism UniProt Comment Textmining
3.4.21.61 Homo sapiens
-
-
-
3.4.21.61 Mus musculus
-
 male C57B/6 mice
-

Source Tissue

EC Number Source Tissue Comment Organism Textmining
3.4.21.61 Hep-G2 cell
-
 Homo sapiens
-
3.4.21.61 liver
-
 Mus musculus
-

Synonyms

EC Number Synonyms Comment Organism
3.4.21.61 PCSK9
-
 Mus musculus
3.4.21.61 PCSK9
-
 Homo sapiens
3.4.21.61 proprotein convertase subtilisin/kexin type 9
-
 Mus musculus
3.4.21.61 proprotein convertase subtilisin/kexin type 9
-
 Homo sapiens