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Literature summary extracted from

  • Chan, J.C.; Piper, D.E.; Cao, Q.; Liu, D.; King, C.; Wang, W.; Tang, J.; Liu, Q.; Higbee, J.; Xia, Z.; Di, Y.; Shetterly, S.; Arimura, Z.; Salomonis, H.; Romanow, W.G.; Thibault, S.T.; Zhang, R.; Cao, P.; Yang, X.P.; Yu, T.; Lu, M.; Retter, M.W.; Kwon, G.; Henne, K.; Pan, O.; Tsai, M.M.; Fuchslocher, B.; Yang, E.; Z, Z.h.
    A proprotein convertase subtilisin/kexin type 9 neutralizing antibody reduces serum cholesterol in mice and nonhuman primates (2009), Proc. Natl. Acad. Sci. USA, 106, 9820-9825.
    View publication on PubMedView publication on EuropePMC

Application

EC Number Application Comment Organism
3.4.21.61 drug development anti-PCSK9 antibodies may be effective therapeutics for treating hypercholesterolemia Mus musculus
3.4.21.61 drug development anti-PCSK9 antibodies may be effective therapeutics for treating hypercholesterolemia Macaca fascicularis
3.4.21.61 drug development anti-PCSK9 antibodies may be effective therapeutics for treating hypercholesterolemia Homo sapiens

Protein Variants

EC Number Protein Variants Comment Organism
3.4.21.61 D374Y gain-of-function mutant, human monoclonal antibody mAb1 also blocks binding of PCSK9 to low density lipoprotein receptor in the mutant Homo sapiens

Inhibitors

EC Number Inhibitors Comment Organism Structure
3.4.21.61 additional information human monoclonal antibody against PCSK9, mAb1, inhibits PCSK9 binding to the low density lipoprotein receptor and attenuates PCSK9-mediated reduction in low density lipoprotein receptor protein levels, thereby increasing low density lipoprotein uptake. A combination of mAb1 with a statin increases low density lipoprotein receptor levels in Hep-G2 cells more than either treatment alone Homo sapiens
3.4.21.61 additional information human monoclonal antibody against PCSK9, mAb1, inhibits PCSK9 binding to the low density lipoprotein receptor and attenuates PCSK9-mediated reduction in low density lipoprotein receptor protein levels, thereby increasing low density lipoprotein uptake. A single injection of mAb1 reduces serum LDL-C by 80%, and a significant decrease is maintained for 10 days Macaca fascicularis
3.4.21.61 additional information human monoclonal antibody against PCSK9, mAb1, inhibits PCSK9 binding to the low density lipoprotein receptor and attenuates PCSK9-mediated reduction in low density lipoprotein receptor protein levels, thereby increasing low density lipoprotein uptake. In wild-type mice, mAb1 increases hepatic low density lipoprotein receptor protein levels ca. 2fold and lowers total serum cholesterol by up to 36% Mus musculus

Organism

EC Number Organism UniProt Comment Textmining
3.4.21.61 Homo sapiens Q8NBP7
-
-
3.4.21.61 Macaca fascicularis
-
-
-
3.4.21.61 Mus musculus
-
-
-

Source Tissue

EC Number Source Tissue Comment Organism Textmining

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
3.4.21.61 low density lipoprotein receptor + H2O
-
 Mus musculus ?
-
 ?
3.4.21.61 low density lipoprotein receptor + H2O
-
 Macaca fascicularis ?
-
 ?
3.4.21.61 low density lipoprotein receptor + H2O
-
 Homo sapiens ?
-
 ?

Synonyms

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