PCSK9
Alpha Lifetech can provide PCSK9 corresponding products, help each customer's research and development.
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Introduction To PCSK9
Drug targets a biomolecule that can directly bind to drugs and then react. Generally, the target refers to a protein related to the cause of disease. The focus of the target began with focusing on tumors and then began to spread to various fields. The introduction of PCSK9 protein is a common target in medicine.
PCSK 9, the ninth member of the lysin family of subtilis of proprotein convertases, is a serine protease encoded by the PCSK 9 gene, which is expressed in various cells throughout the body and is produced mainly in liver cells.
Function of Target PCSK9
PCSK 9 has important biological functions in the regulation of cholesterol metabolism, tissue expression, and function, its relationship with disease, and clinical application. The PCSK 9 protein can participate in the degradation process of LDLR. In the physiological state, LDLR on the cell surface binds free LDL-C in the blood and mediates its endocytosis into the cell, further degraded in intracellular metabolism, while LDLR is transported back to the cell membrane for recycling. Elevated intracellular cholesterol concentrations can upregulate the expression levels of the PCSK 9 precursor protein. Extracellular, PCSK 9 molecules bind to LDLR through the catalytic subunit to form the PCSK 9-LDLR-LDL-C complex, which will be transported to the lysosome for degradation, thus blocking the process of LDLR return to the cell membrane. Thus, overexpression or hyperactivation of PCSK 9 in FH patients with acquired function mutations of the PCSK 9 gene will induce rapid endocytosis and degradation of LDLR at the cell membrane, inhibiting the clearance of LDL-C by cells, and causing abnormal increase of LDL-C levels in the blood.
Gene Pathway of Target PCSK9
PCSK9 directly or indirectly upregulates Snail 1 and then downregulates E-cadherin expression, but N-cadherin and MMP 9 levels, which thereafter induce epithelial-mesenchymal transition (EMT) in colon cancer cells, and activates PI3K / AKT signaling. However, PCSK 9 overexpression has opposite effects on colon cancer cells. Knockdown of PCSK 9 expression inhibited M2 macrophage polarization but also promoted M1 macrophage polarization by reducing lactate, protein rectification, and macrophage migration inhibitory factor (MIF) levels. PCSK 9 triggers mitochondrial DNA damage and activates the cGAS-STING pathway in the DN, thereby leading to a cascade of inflammatory cascades. PCSK 9 targeted intervention can effectively reduce DN inflammation and delay its progression. Moreover, inhibition of STING significantly abolished the inflammation triggered by HGPA in HK-2 cells.
Fig 1: PCSK9 Gene Pathway. (Reference source: Lambert G, Sjouke B, Choque B, Kastelein JJ, Hovingh GK. The PCSK9 decade. J Lipid Res. 2012 Dec;53(12):2515-24.)
Alpha Lifetech Can Provide
At present, various drugs targeting PCSK9 are constantly under development, and taking drugs alone or together with other products to treat diseases has become a new method and remarkable achievements have been made. PCSK9 protein has shown important research value and application prospects in tumor biology, and drug research and development. With further research and technological advances, PCSK9 protein products are also essential. Alpha Lifetech can provide LPCSK9 with corresponding products and help each customer's research and development. Alpha Lifetech provides end-to-end biotechnology development solutions, from upstream cell culture optimization to downstream purification scale. Our process is validated through analytical techniques such as HPLC, SDS-PAGE, and mass spectrometry to ensure product consistency and regulatory compliance. By combining cutting-edge biotechnology expertise with flexible service models, we help clients accelerate project research progress and ensure smooth experimentation.
| Catalog Number | Product Name | Product Sizes |
|---|---|---|
| ADT1190 | 100ug,1mg,5mg | |
| ADT1466 | 100ug,1mg,5mg | |
| ADT1539 | 100ug,1mg,5mg | |
| ADT1023 | 1mg,5mg | |
| ADT1231 | 100ug,1mg,5mg | |
| ADT1257 | 100ug,1mg,5mg | |
| ADT1367 | 100ug,1mg,5mg | |
| ADT1620 | 100ug,1mg,5mg | |
| ADT1102 | 100ug,1mg,5mg | |
| ADT1532 | 100ug,1mg,5mg | |
Reference
[1] Hummelgaard S, Vilstrup JP, Gustafsen C, Glerup S, Weyer K. Targeting PCSK9 to tackle cardiovascular disease. Pharmacol Ther. 2023 Sep;249:108480.
[2] Lambert G, Sjouke B, Choque B, Kastelein JJ, Hovingh GK. The PCSK9 decade. J Lipid Res. 2012 Dec;53(12):2515-24.
[3] Ding Z, Pothineni NVK, Goel A, Lüscher TF, Mehta JL. PCSK9 and inflammation: role of shear stress, pro-inflammatory cytokines, and LOX-1. Cardiovasc Res. 2020 Apr 1;116(5):908-915.
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2018-07-16
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