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Literature summary for 3.4.21.61 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

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

Protein Variants

Protein Variants Comment Organism
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

Inhibitors Comment Organism Structure
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
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
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

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

Source Tissue

Source Tissue Comment Organism Textmining

Substrates and Products (Substrate)

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

Synonyms

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