Journal
FUTURE MEDICINAL CHEMISTRY
Volume 10, Issue 8, Pages 907-934Publisher
FUTURE SCI LTD
DOI: 10.4155/fmc-2017-0207
Keywords
inhibitors; progress; SIRT1; SIRT2; sirtuins
Categories
Funding
- Natural Science Foundation of Jiangsu Province [BK20161458]
- 'Six Talent Peaks' Project of Jiangsu Province [2016-YY-042]
- Postgraduate Research & Practice Innovation Program of Jiangsu Province [KYCX17_0721]
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Sirtuins (SIRT) are coenzyme NAD(+)-dependent histone deacetylases for the transfer of modified acetyl groups. Sirtuins are widely involved in various physiological processes and therefore associated with cardiovascular disease, diabetes, Parkinson's disease, cancer and beyond. Consequently, the development of modulators for sirtuins has considerable clinical value. To date, a variety of SIRT1/2 inhibitors have been reported and none has been approved for the market. This review summarizes the recent progress in the discovery and development of SIRT1/2 inhibitors including their inhibitory potency, structure-activity relationship and binding mode analysis as well as discusses the perspective for the future development of SIRT1/2 inhibitors.
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