Niemann-Pick C1-like 1 cholesterol transporter (NPC1L1)

Niemann-Pick C1-like 1 cholesterol transporter (NPC1L1) is a multispan transmembrane protein highly expressed in the intestinal epithelium and hepatocytes, where it mediates the uptake of dietary and biliary cholesterol. NPC1L1 is the primary target of the drug ezetimibe, which selectively inhibits its activity to reduce cholesterol absorption and plasma LDL cholesterol levels. In addition to its established role in cholesterol transport and cardiovascular disease risk, recent research suggests NPC1L1 is implicated in cancer biology, with altered expression linked to prognosis and tumor progression in colorectal, hepatocellular, and pancreatic cancers. Polymorphisms in the NPC1L1 gene can affect responsiveness to cholesterol-lowering therapies. Safety concerns regarding cancer risk have not been substantiated in larger meta-analyses. NPC1L1 is part of the solute carrier family (SLC65A2), shares homology with NPC1, and mediates cholesterol internalization via endocytosis[1][2][3][4].

Other names

Niemann–Pick C1-like 1NPC1 like intracellular cholesterol transporter 1SLC65A2LDLCQ7NPC11L1NPC1-like 1

Inhibition of cholesterol absorption: Ezetimibe binds to NPC1L1 and blocks intestinal and hepatic cholesterol uptake, leading to reduced plasma cholesterol levels[1][3].