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Applications: Great for screening small molecular inhibitors for drug discovery and HTS applications.
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: The PCSK9(D374T)-LDLR TR-FRET Assay Kit is designed to measure the inhibition of the high affinity PCSK9 mutant (D374T) binding to LDLR in a homogeneous 384 reaction format. This FRET-based assay requires no time-consuming washing steps, making it especially suitable for high throughput screening applications. The assay procedure is straightforward and simple; a sample containing europium-labeled (Eu) LDLR ectodomain, dye-labeled acceptor, biotin-labeled PCSK9(D374T), and an inhibitor is incubated for two hours. Then, the fluorescence intensity is measured using a fluorescence reader.
Storage Stability: At least 6 months from date of receipt when stored as directed.
Supplied As: Kit comes in a convenient format with biotinylated PCSK9, Eu-labeled LDLR, dye-labeled acceptor, assay buffer and microtiter plate to perform 384 reactions.
Uniprot: Q8NBP7
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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