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Applications: Useful for the study of enzyme kinetics, binding studies, screening inhibitors, and selectivity profiling.
Assay Conditions: Reaction was performed using PCSK9(D374T)-LDLR TR-FRET Assay Kit (Cat. #72011). Briefly, 5 ng of europium-labeled LDLR were mixed withvarying amounts of PCSK9(D374T) and dye labeled acceptor in PCSK9 TR-FRET assay buffer and incubated at RT for 2 hr. Donor emission was read at 620 nm followed by acceptor emission at 665 nm.
Background: PCSK9 is a crucial player in the regulation of plasma cholesterol homeostasis. It binds to the ectodomain of hepatic low-density lipid receptor family members: low density lipoprotein receptor (LDLR), very low density lipoprotein receptor (VLDLR), apolipoprotein E receptor (LRP1/APOER) and apolipoprotein receptor 2 (LRP8/APOER2), and promotes their degradation. PCSK9 acts via a non-proteolytic mechanism to enhance the degradation of the hepatic LDLR through a clathrin LDLRAP1/ARH-mediated pathway. May prevent the recycling of LDLR from endosomes to the cell surface or direct it to lysosomes for degradation. The D374T mutation results in higher affinity of PCSK9 for LDLR.
Description: Human proprotein convertasesubtilisin/kexin type 9 (PCSK9), also known as FH3, HCHOLA3, and PC9, GenBank Accession No. NM_174936, a.a. 31-692(end), with C-terminal His- and Avi-tagsand a D374T mutation, MW=73.8 kDa, expressed in an HEK293 cell expression system and enzymatically biotinylated using Avitag™ technology. PCSK9 is autocleavedto the ~14 kDa prodomain (a.a. 31-152) and the ~60 kDa mature form (a.a. 153-692), which run at higher MW by SDS-PAGE.
Format: Aqueous buffer solution
Formulation: 40 mM Tris-HCl, pH 8.0, 110 mM NaCl, 2.2 mM KCl, 20% glycerol
Genbank: NM_174936
Storage Stability: At least 6 months at -80°C.
Tags: C-terminal His, Avi-tags
Uniprot: Q8NBP7
Warnings: Avoidfreeze/thaw cycles. Storing dilutedenzyme is not recommended, ifnecessary, use carrier protein (BSA 0.1- 0.5%).
Biosafety Level: Not applicable (BSL-1)
References: 1. Chan, J.C. et al. (2009). Proc. Natl. Acad. Sci. USA, 106: 9820-9825.
2. Liang, H., et al. (2012). J. Pharmacol. Exp. Ther. 340: 2289-236.
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