Biomedicine & Pharmacotherapy (Nov 2022)

Recent advances in the screening methods of NPC1L1 inhibitors

  • Renshuai Zhang,
  • Wenjing Liu,
  • Jun Zeng,
  • Jingsen Meng,
  • Lingyu Shi,
  • Shanbo Yang,
  • Jing Chang,
  • Chao Wang,
  • Kunyue Xing,
  • Jialian Wen,
  • Ning Liu,
  • Bing Liang,
  • Dongming Xing

Journal volume & issue
Vol. 155
p. 113732

Abstract

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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.

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