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Cholesterol-binding proteins (CBPs) represent a broad functional class of proteins that specifically interact with cholesterol to regulate its transport, intracellular distribution, and signaling. This category encompasses several distinct protein families, including the Niemann-Pick C (NPC) proteins, sterol carrier proteins (SCPs), oxysterol-binding proteins (OSBPs), and caveolins. For instance, NPC1 and NPC1L1 are critical for the movement of cholesterol across lysosomal and intestinal membranes, respectively, while proteins like CETP facilitate the exchange of lipids between lipoproteins in the plasma. Due to their central role in maintaining lipid homeostasis, these proteins are significant therapeutic targets for treating hypercholesterolemia and atherosclerosis. Drugs such as ezetimibe target specific members of this class to lower blood cholesterol levels, while various CETP inhibitors have been investigated for their potential to raise high-density lipoprotein (HDL) levels and reduce cardiovascular events.
Inhibition of cholesterol absorption (NPC1L1), inhibition of cholesterol ester transfer (CETP), modulation of lysosomal cholesterol egress (NPC1), or direct binding and sequestration of cholesterol.
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