What's PCSK9?
PCSK9 (also known as neural apoptosis-regulated convertase, NARC-1) is an extracellular protein
expressed primarily in the kidneys, liver and intestines. Genetic observations mapped PCSK9 as the third gene
(along with LDLR and APOB) to cause autosomal dominant hypercholesterolemia (ADH). These studies suggested that
gain of function mutations increase plasma levels of LDL-c, whereas loss-of-function mutations lead to a reduction
of plasma levels of LDL-c and a decrease in the risk of coronary heart disease (CHD) (1).
Recent studies
showed the secreted form of PCSK9 binding directly to the LDLR and resulting in degradation of the receptor.
Zhang et al. localized the binding site of PCSK9 in the LDLR to the first epidermal growth factor-like repeat (EGF-A) of
the extracellular domain and showed that PCSK9 binding to this site is required for LDLR degradation(2).
PCSK9 would seem to be an attractive drug target for lowering LDL-c(3).
References
1. Cohen J. C., et al., N. Engl. J. Med. 354, 1264-1272 (2006)
2. Zhang D. W., et al., J. Biol. Chem. 282, 18602-18612 (2007)
3. Kourimate S., et al., Atherosclerosis, 206, 134-140 (2009)
PCSK9 Related Products
PCSK9 Kit
- CY-8079Human PCSK9 ELISA Kit( 96 Assay )
- This kit is used for the quantitative measurement of Human PCSK9 in serum, plasma, cell culture medium and other biological media.
- Product Publication Reference
- (1) Cellular and secreted pro-protein convertase subtilisin/kexin type 9 catalytic activity in hepatocytes Kourimate S, Chétiveaux M, Jarnoux AL, Lalanne F and Costet P. Atherosclerosis, 206, 134-140 (2009)
- (2) The E32K variant of PCSK9 exacerbates the phenotype of familial hypercholesterolaemia by increasing PCSK9 function and concentration in the circulation Noguchi T, Katsuda S, Kawashiri M, Tada H, Nohara A, Inazu A, Yamagishi M, Kobayashi J and Mabuchi H. Atherosclerosis, in Press
- CY-8078Mouse/Rat PCSK9 ELISA Kit( 96 Assay )
- This kit is used for the quantitative measurement of Mouse PCSK9 in serum, plasma, cell culture medium and other biological media and can be done for Rat PCSK9 also.
- CY-8150PCSK9-LDLR in vitro Binding Assay Kit( 96 Assay )
- This kit is primarily designed for the rapid and sensitive screening and evaluation of inhibitor candidates as well as characterization of PCSK9-LDLR interaction in vitro.
PCSK9 Antibody
- CY-M1032Anti-Human PCSK9 Prodomain Clone KS-2C8( 100ug )
- CY-M1033Anti-Human PCSK9 Clone KS-4H12( 100ug )
- CY-P1037Anti-Human PCSK9( 100ug )
Recombinant PCSK9 (WT, Mutant) & LDLR Proteins
- CY-R2310PCSK9 Wild Type in culture medium( 50ug )
- CY-R2311PCSK9 D374Y in culture medium( 50ug )
- CY-R2320PCSK9 Wild Type/Δ53 in culture medium( 20ug )
- CY-R2321PCSK9 D374Y/Δ53 in culture medium( 10ug )
- CY-R2330PCSK9 Wild Type( 50ug )
- CY-R2331PCSK9 D374Y( 10ug )
- CY-R2333PCSK9 R194A( 20ug )
- CY-R2340LDLR EGF-AB domain( 50ug )
- CY-R2341LDLR EGF-AB domain, Myc-tagged( 50ug )