4.7 Review

Mechanisms of antidiabetic drugs and cholesterol efflux: A clinical perspective

Journal

DRUG DISCOVERY TODAY
Volume 27, Issue 6, Pages 1679-1688

Publisher

ELSEVIER SCI LTD
DOI: 10.1016/j.drudis.2022.02.006

Keywords

Atherosclerosis; Nonalcoholic fatty liver disease; Diabetes; Cholesterol efflux; reverse cholesterol transport

Funding

  1. Russian Science Foundation [20-15-00264]
  2. Russian Science Foundation [20-15-00264] Funding Source: Russian Science Foundation

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This review summarizes the potential effects of hypoglycemic agents on cholesterol efflux (CE), a key step in reverse cholesterol transport (RCT), and how this may influence atherosclerosis and fatty liver disease. Newer antidiabetic agents have the potential to target CE and prevent or alleviate the development of related diseases, while also improving insulin secretion. However, further research is needed to interpret the clinical relevance of these findings.
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.

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