Mechanisms of antidiabetic drugs and cholesterol efflux: A clinical perspective

Drug Discov Today. 2022 Jun;27(6):1679-1688. doi: 10.1016/j.drudis.2022.02.006. Epub 2022 Feb 16.

Abstract

Reverse cholesterol transport (RCT) is a physiological process that reduces excess cholesterol in the body. Cholesterol efflux (CE), an important step in RCT, is mainly mediated by ATP-binding cassette transporters A1 and G1 and has a significant role in atheroprotection. Moreover, impairments in CE can lead to the development of diabetes and fatty liver disease. In this review, we summarize the possible effects of hypoglycemic agents on CE and how this might influence atherosclerosis and dyslipidemia-related pathologies. Newer antidiabetic agents could have significant potential for targeting CE and preventing or alleviating atherosclerosis, obesity, and liver steatosis, and simultaneously improving insulin secretion. However, more research is warranted to interpret the clinical relevance of these data.

Keywords: Atherosclerosis; Cholesterol efflux, reverse cholesterol transport; Diabetes; Nonalcoholic fatty liver disease.

Publication types

  • Review
  • Research Support, Non-U.S. Gov't

MeSH terms

  • ATP Binding Cassette Transporter, Subfamily G, Member 1
  • ATP-Binding Cassette Transporters / metabolism
  • Atherosclerosis*
  • Biological Transport
  • Cholesterol
  • Humans
  • Hypoglycemic Agents* / pharmacology
  • Hypoglycemic Agents* / therapeutic use

Substances

  • ATP Binding Cassette Transporter, Subfamily G, Member 1
  • ATP-Binding Cassette Transporters
  • Hypoglycemic Agents
  • Cholesterol