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Members of the low-density lipoprotein receptor family are single-pass transmembrane receptors involved in the endocytosis of cholesterol and various ligands, as well as in regulation of extracellular matrix, cell adhesion, signal transduction, and growth factor response. These receptors, including LDLR and LRPs, are expressed in tumor cells and the tumor microenvironment and display altered expression and function in several cancers, influencing tumor growth, invasion, and recurrence-free survival. Their complex role includes both tumor-suppressive and pro-tumorigenic activities, depending on the context and malignancy state, making them a multifaceted target in cancer biology.
Inhibition of cholesterol uptake (reduces cell proliferation, induces cell death); Modulation of Wnt/β-catenin pathway (especially for LRP5/6 inhibitors); Interference with growth factor signaling (EGFR/MAPK, TGF-β, PDGF, etc.).
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