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The proprotein convertase subtilisin kexin 9 (PCSK9) is a key regulator in plasma cholesterol metabolism. It binds to a number of low-density lipid receptor family members: LDLR, VLDLR, LRP1/APOER, and LRP8/APOER2. PCSK9 regulates the levels of LDL receptors, plasma membrane glycoproteins that remove cholesterol-rich LDL particles from the plasma. The removal of LDL receptors involves internalization of the PCSK9-LDL complex and then fusion with an acidic endosome. With its key role in cholesterol homeostasis, PCSK9 can be a drug target. Drugs that block PCSK9 can lower low-density lipoprotein cholesterol (LDL-C), and may improve outcomes in heart disease.... |
