LDLR

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LDLR

A gene on chromosome 19p13.2 that encodes a cell surface protein involved in receptor-mediated endocytosis of low-density lipoprotein (LDL), the major cholesterol-carrying lipoprotein of plasma, which it transports into cells by endocytosis. Internalisation of the receptor-ligand complex requires clustering into clathrin-coated pits.
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Praluent inhibits the binding of PCSK9 (proprotein convertase subtilisin/kexin type 9) to the LDL receptor and thereby increases the number of available LDL receptors on the surface of liver cells, which lowers LDL-C levels in the blood.
According to the companies, Praluent inhibits the binding of PCSK9 (proprotein convertase subtilisin/kexin type 9) to the LDL receptor and increases the number of available LDL receptors on the surface of liver cells, which lowers LDL-C levels in the blood.
Promoter of the LDL receptor gene contains a thyroid hormone responsive element (TRE) that allows the triiodothyronine (T3) to upregulate the gene expression of the LDL receptor (Bakker et al.
14 As a polymorphic protein, ApoE is the ligand of LDL receptor and that of chylomicron particle receptor in hepatocytes.
Activation of the hepatic LDL receptor promoter by thyroid hormone.
These drugs are antibodies directed at the PCSK9 protein, which regulates LDL receptor recycling.
LDLs containing only apoB-100 were shown to bind to cell-surface receptors on fibroblasts, known as the LDL receptor (LDLR) (11).
The team notes that trials specifically investigating how PCSK9 inhibitors affect cardiovascular outcomes have yet to be completed, so data for these drugs to date were assessed separately and compared with data for therapies that increase LDL receptor expression.
7] It binds to the LDL receptor (LDL-R) and promotes its intracellular lysosomal degradation via uptake into the hepatocytes.
LDL is surrounded by a single copy of apolipoprotein B-100 (ApoB100) [2] which binds the LDL receptor on the cell surface of target tissues [1].
Evolocumab and alirocumab are human monoclonal antibodies that lower LDL-C by binding to and inactivating proprotein convertase subtilisin kexin type 9 (PCSK9), which regulates the LDL receptor.