Figure: Schematic representation of PCSK9 Binding Assay Kit which can be used to screen inhibitors of PCSK9 binding to the LDL receptor.
As discussed in a previous blog post, inhibiting PCSK9 from binding to the LDL receptor results in lower LDL cholesterol levels in the bloodstream. Research on PCSK9 has explored how it can be targeted in treatments for hypercholesterolemia (high cholesterol) and other cardiovascular diseases1.
This blog post will catch you up on the two biggest areas of research into treatments for high cholesterol that target PCSK9. And why there is so much news coverage. http://www.fiercebiotech.com/tags/pcsk9-drugs
Antibodies are proteins that can specifically bind to another protein called an antigen. Many antibodies bind to antigens to target them for destruction. Monoclonal antibodies are antibodies that are derived from an identical cell line2. When PCSK9 is bound by a monoclonal antibody, PCSK9 cannot bind the LDL receptor3. The inhibition of PCSK9 from binding to LDL receptors results in an increase in the number of LDL receptors. Consequently, the level of LDL cholesterol in the bloodstream is lowered.
RNA can be divided into two types: coding and non-coding RNA. Coding RNA, also termed mRNA, contains the genetic information for a protein to be produced. siRNA is a type of non-coding RNA that can bind to mRNA and prevent the protein specific to that mRNA from being produced4. The use of a siRNA specific to the mRNA that codes for PCSK9 is being explored as a way to lower PCSK9 production5. By lowering PCSK9 production, the level of cholesterol in the bloodstream can be lowered.
MBL International offers a variety of PCSK9 products including PCSK9 antibodies and PCSK9 ELISA kits. With our PCSK9 ELISA kits, you will be able to measure levels of PCSK9 and further your research into the regulation of cholesterol.
1. Farnier M. PCSK9: From discovery to therapeutic applications. Arch Cardiovasc Dis. 2014;107(1):58-66.
2. "Monoclonal Antibodies to Treat Cancer." American Cancer Society. American Cancer Society, 8 Dec. 2014. Web. 02 June 2015.
3. Poirier S, Mayer G. The biology of PCSK9 from the endoplasmic reticulum to lysosomes: new and emerging therapeutics to control low-density lipoprotein cholesterol. Drug Des Devel Ther. 2013;7:1135-48.
4. Tang G. siRNA and miRNA: an insight into RISCs. Trends Biochem Sci. 2005;30(2):106-14.
5. Frank-kamenetsky M, Grefhorst A, Anderson NN, et al. Therapeutic RNAi targeting PCSK9 acutely lowers plasma cholesterol in rodents and LDL cholesterol in nonhuman primates. Proc Natl Acad Sci USA. 2008;105(33):11915-20.