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The low-density lipoprotein receptor family consists of structurally related cell-surface receptors that mediate the endocytosis of diverse extracellular ligands, particularly those involved in lipid, cholesterol, and proteinase turnover. Members include LDLR, VLDLR, LRP1, LRP2 (megalin), and others, all characterized by modular architectures with cysteine-rich LDL receptor-type A repeats, EGF-like domains, a transmembrane anchor, and cytoplasmic motifs for internalization and signaling. They are central to cholesterol homeostasis, removal of remnant lipoproteins, and regulation of vital signaling pathways in many tissues, including the brain, liver, and cardiovascular system. Dysfunction of these receptors is genetically and clinically linked to disorders such as familial hypercholesterolemia, atherosclerosis, and neurodegenerative diseases like Alzheimer’s disease. Their essential, multi-system role makes them central therapeutic targets for a range of metabolic and cardiovascular diseases
Enhancement of receptor-mediated endocytosis of LDL and other lipoproteins - Upregulation of receptor expression - Inhibition or modulation of downstream signaling pathways (e.g., Wnt pathway via LRP5/6)
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