PCSK9 Assay Service
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Target
PCSK9
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Description
Screening and/or profiling inhibitor compounds against PCSK9 binding to LDLR in a biochemical assay.
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Synonyms
pcsk9, cholesterol, LDL, kexin
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Example Data
*Example only, final data may vary.
Assay Details
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Assay Format
TR-FRET
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Reference Compounds and IC50
Anti-PCSK9 Antibody, 0.01 μM
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Assay Principle
The PCSK9/LDLR TR-FRET Assay is designed to measure the inhibition of PCSK9 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, and an inhibitor is incubated for two hours. Then, the fluorescence intensity is measured using a fluorescence reader.
Target Details
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Protein Family
Cholesterol-Related
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UniProt
Q8NBP7
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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.
Delivery
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Estimated Turnaround
Two to three weeks following delivery of compounds
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Results
Extensive report with raw and analyzed data, graphs, and detailed protocols. Includes positive control for inhibition.
