Molecular biology of PCSK9: its role in LDL metabolism - PMC
Proprotein convertase subtilisin-like kexin type 9 (PCSK9) is a newly discovered serine protease that destroys low density lipoprotein (LDL) receptors in liver and thereby controls the level of LDL in plasma.
PCSK9 Inhibitors: How They Manage Cholesterol and Side Effects
PCSK9 inhibitors are a cholesterol-lowering medicine. They work by decreasing your levels of low-density lipoprotein (LDL) cholesterol. Your provider may prescribe PCSK9 inhibitors if you have tried other medicines and still have high cholesterol.
PCSK9 and LDLR degradation: regulatory mechanisms in
Recent findings: Recent studies indicate that circulating PCSK9 binds to apolipoprotein B100 on LDL particles, which in turn inhibits PCSK9's ability to bind to cell surface LDLRs. Negative feedback of secreted PCSK9 activity by LDL could serve to increase plasma excursion of triglyceride-rich lipoproteins and monitor lipoprotein remodeling.
PCSK9 inhibition: A game changer in cholesterol management
Nov 20, 2015 · Proprotein convertase subtilisin/kexin type 9 serine protease (PCSK9) plays an important role in cholesterol metabolism by regulating LDL receptor degradation. Shortly after its discovery in 2001, the gene encoding PCSK9 was implicated in …
Regulation of PCSK9 Expression and Function: Mechanisms and …
Proprotein convertase subtilisin/kexin type 9 (PCSK9) promotes degradation of low-density lipoprotein receptor (LDLR) and plays a central role in regulating plasma levels of LDL cholesterol levels, lipoprotein (a) and triglyceride-rich lipoproteins, increasing the risk of …
Advances in targeting LDL cholesterol: PCSK9 inhibitors and beyond
PCSK9 (proprotein convertase subtilisin/kexin 9) is a hepatically-derived protein that regulates LDL-receptor expression. PCSK9 inhibition leads to an increase in LDL-receptor density on the liver surface, resulting in reduced serum LDL-C levels.
Chasing LDL cholesterol to the bottom — PCSK9 in perspective
Jun 15, 2022 · Like the LDL receptor, PCSK9 can block recycling of major histocompatibility antigen class I (MHC I) to the cell surface by chaperoning it to the lysosome.
Current and emerging PCSK9‐directed therapies to reduce LDL‐C …
Dec 16, 2024 · An appreciation for the role of PCSK9 in LDL-C regulation incited the pharmacologic development of subcutaneously delivered mAb therapies that specifically target PCSK9 and block its ability to facilitate LDL receptor degradation.
New PCSK9 Gets Cholesterol to Target if Statins Can't - Medscape
3 days ago · PCSK9 prevents LDL receptors from "recycling" to the surface of hepatocytes or liver cells where they remove LDL-C from circulation. PCSK9 inhibitors increase the density of the receptors on the ...
PCSK9 Inhibitors - StatPearls - NCBI Bookshelf
Feb 25, 2024 · In patients without clinical cardiovascular disease and with baseline LDL-C ≥190 mg/dL on a statin for primary prevention, if the LDL-C level on statin ≥100 mg/dL (≥2.59 mmol/L), a PCSK9 inhibitor may be considered.