Thursday, 27 October 2016

PCSK9 inhibitors are monoclonal antibodies (MABs

Proprotein convertase subtilisin/kexin type 9 (PCSK9) is an enzyme encoded by the PCSK9 gene in humans on chromosome

It is ubiquitously expressed in many tissues and cell types.PCSK9 binds to the receptor for low-density lipoprotein (LDL) cholesterol (LDL-C). In the liver, the LDL receptor (LDLR) removes LDL-C from the blood. When PCSK9 binds to the LDLR, the receptor is broken down and can no longer remove LDL-C from the blood. If PCSK9 is blocked, more LDLRs will be present on the surface of the liver and will remove more LDL-C from the blood.Therefore, blocking PCSK9 can lower blood cholesterol levels. Similar genes (orthologs) are found across many species. PCSK9 is inactive when first synthesized, because a section of peptide chains blocks their activity; proprotein convertases remove that section to activate the enzyme.

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