Recent advances in the screening methods of NPC1L1 inhibitors.

NPC1L1 is a crucial protein involved in sterol lipid absorption and has been shown to play an important role in intestinal cholesterol absorption. Hypercholesterolemia is a significant risk factor for cardiovascular diseases such as coronary heart disease. Screening of NPC1L1 inhibitors is critical for gaining a full understanding of lipid metabolism, developing new cholesterol-lowering medicines, and treating cardiovascular diseases. This work summarized existing methodologies for screening NPC1L1 inhibitors and evaluated their challenges, and will assist the development of novel cholesterol-lowering medications and therapeutic strategies for hypercholesterolemia and other cholesterol-related metabolic disorders.