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Literature summary 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

Application

EC Number Application Comment Organism
3.4.21.61 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)

EC Number Cloned (Comment) Organism
3.4.21.61 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

EC Number Protein Variants Comment Organism
3.4.21.61 D374Y naturally occurring gain-of-function mutation, associated to hypercholesterolemia and premature atherosclerosisias. Has less effect on processing (49% maturation) Homo sapiens
3.4.21.61 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
3.4.21.61 S127R naturally occurring gain-of-function mutation, associated to hypercholesterolemia and premature atherosclerosisias. Strongly diminishes processing (21% maturation) Homo sapiens
3.4.21.61 S386A catalytically inactive, strongly diminishes processing (8% maturation) Homo sapiens

Organism

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

Purification (Commentary)

EC Number Purification (Comment) Organism
3.4.21.61
-
 Mus musculus
3.4.21.61
-
 Homo sapiens

Source Tissue

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

Synonyms

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

Expression

EC Number Organism Comment Expression
3.4.21.61 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

EC Number General Information Comment Organism
3.4.21.61 malfunction at t = 585 min, PCSK9-/- hepatocytes exhibit 90% less activity than wild-type Mus musculus
3.4.21.61 malfunction cells with lower PCSK9 expression and secretion have a low density lipoprotein binding activity augmented by 200% Homo sapiens
3.4.21.61 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