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Low-density lipoprotein (LDL)

Target
LDL
Molecular classification
Other (Lipoprotein, Macromolecular complex)
01

Overview

Low-density lipoprotein (LDL) is a complex nanoparticle composed primarily of lipids and a single apolipoprotein B-100 molecule that serves as both a structural scaffold and ligand for receptor-mediated endocytosis[1][5]. LDL is the principal carrier of cholesterol in plasma, transporting it to peripheral tissues. The particle consists of a hydrophobic core of cholesteryl esters and triglycerides surrounded by a monolayer of phospholipids, free cholesterol, and apolipoprotein B-100[1][2][5]. Elevated levels of circulating LDL are associated with the development and progression of atherosclerosis, a leading cause of cardiovascular disease[1][4][5]. Although LDL is not a drug target in the conventional sense (i.e., not a receptor, enzyme, or protein therapeutic target), its concentration in blood is a major clinical biomarker, and modulation of its levels is central to therapies such as statins or PCSK9 inhibitors, which indirectly reduce LDL by upregulating LDL receptor expression or function[5][7][9]. Notes: - **is_incorrect**: true. The listed target is not a single molecule but a particle consisting of many molecules (lipids and one protein, apoB-100). The typical therapeutic target in context of LDL is the "Low-density lipoprotein receptor" (LDLR), not LDL itself. - **interacting_drugs/mechanism_of_action**: Direct drugs do not target LDL as a structure but rather its metabolism (e.g., HMG-CoA reductase inhibition to reduce LDL synthesis, PCSK9 inhibition to increase LDLR-mediated clearance)[9]. No drugs directly "bind" or act on LDL as a therapeutic mechanism. For research on LDL as a direct molecular or pharmacological target, the answer is: LDL itself is best described as a biomarker and a lipid carrier; the actual common therapeutic target is the LDL receptor (LDLR). If seeking structured drug target data, "Low-density lipoprotein receptor (LDLR)" is more appropriate. If you wish to map LDL as a clinical analyte (biomarker), "Low-density lipoprotein cholesterol" is the common analyte.

Other names
LDLβ-lipoprotein
02

Mechanism of action

Acts as a carrier; not a direct drug target for therapeutic intervention. Drugs affecting LDL levels typically target its metabolism or receptor-mediated clearance, e.g., HMG-CoA reductase inhibitors, PCSK9 inhibitors.

03

Biological functions

Lipid transportCholesterol transportEnergy deliveryLipid/cholesterol metabolism
04

Disease associations

Cardiovascular diseaseAtherosclerosisHyperlipidemiaMetabolic syndrome
05

Safety considerations

High LDL-C is a recognized risk factor for atherosclerosis, coronary artery disease, and related cardiovascular morbidity/mortality
06

Biomarkers

LDL cholesterol (LDL-C) concentration is a major clinical biomarker for cardiovascular risk

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