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Literature summary for 3.4.21.61 extracted from

  • Kourimate, S.; Chetiveaux, M.; Jarnoux, A.L.; Lalanne, F.; Costet, P.
    Cellular and secreted pro-protein convertase subtilisin/kexin type 9 catalytic activity in hepatocytes (2009), Atherosclerosis, 206, 134-140.
    View publication on PubMed
Search for more literature for 3.4.21.61

Application

Application Comment Organism
drug development PCSK9 is a highly promising therapeutic target to lower low density lipoprotein-cholesterol and therefore prevent or reduce atherosclerosis Homo sapiens

Cloned(Commentary)

Cloned (Comment) Organism
wild-type PCSK9 with a V5 epitope flag inserted into pcDNA3.1. PCSK9 mutants expressed in primary hepatocytes derived from PCSK9-/- mice Homo sapiens

Protein Variants

Protein Variants Comment Organism
D374Y naturally occurring gain-of-function mutation, associated to hypercholesterolemia and premature atherosclerosisias. Has less effect on processing (49% maturation) Homo sapiens
F216L naturally occurring gain-of-function mutation, associated to hypercholesterolemia and premature atherosclerosisias. Is matured to the same extent than the wild type (67% maturation) Homo sapiens
S127R naturally occurring gain-of-function mutation, associated to hypercholesterolemia and premature atherosclerosisias. Strongly diminishes processing (21% maturation) Homo sapiens
S386A catalytically inactive, strongly diminishes processing (8% maturation) Homo sapiens

Organism

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

Purification (Commentary)

Purification (Comment) Organism
-
 Mus musculus
-
 Homo sapiens

Source Tissue

Source Tissue Comment Organism Textmining
blood plasma
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 Mus musculus
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HEK-293 cell
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 Homo sapiens
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hepatocyte
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 Mus musculus
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hepatocyte
-
 Homo sapiens
-

Synonyms

Synonyms Comment Organism
PCSK9
-
 Mus musculus
PCSK9
-
 Homo sapiens
pro-protein convertase subtilisin/kexin type 9
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 Mus musculus
pro-protein convertase subtilisin/kexin type 9
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 Homo sapiens

Expression

Organism Comment Expression
Homo sapiens knockdown of PCSK9 expression in immortalized human hepatocytes using specific siRNA which results in a 38% and 53% decrease in PCSK9 protein quantity, respectively in cell lysates and culture media compared with controls down

General Information

General Information Comment Organism
malfunction at t = 585 min, PCSK9-/- hepatocytes exhibit 90% less activity than wild-type Mus musculus
malfunction cells with lower PCSK9 expression and secretion have a low density lipoprotein binding activity augmented by 200% Homo sapiens
physiological function high level of activity in wild-type PCSK9+/+ hepatocytes. At t = 585 min, the activity of 20 microg of total hepatocyte lysates is 360% higher than that of 10 microg of purified protein Mus musculus