Recent advances in the development of histone deacylase SIRT2 inhibitors. Issue 61 (9th October 2020)

• Record Type: Journal Article
• Authors: Yang, Wenyu; Chen, Wei; Su, Huilin; Li, Rong; Song, Chen; Wang, Zhouyu; Yang, Lingling
• Is Part Of: RSC advances. Volume 10:Issue 61(2020)
• Page Start: 37382
• Page End: 37390
• Publication Date: 2020-10-09
• Subjects: Chemistry -- Periodicals; 540.5
• DOI: 10.1039/d0ra06316a
• Languages: English
• ISSNs: 2046-2069

Abstract

Abstract : This review presents a systematic summarization of nine chemotypes of small-molecule SIRT2 inhibitors, which will be useful for future efforts to develop new inhibitors targeting SIRT2 and associated target proteins. Abstract : Sirtuin 2 (SIRT2) is an important and special member of the atypical histone deacetylase Sirtuin (SIRT) family. Due to its extensive catalytic effects, SIRT2 can regulate autophagy, myelination, immunity, inflammation and other physiological processes. Recent evidence revealed that dysregulation of human SIRT2 activity is associated with the pathogenesis and prognosis of cancers, Parkinson's disease and other disorders; thus SIRT2 is a promising target for potential therapeutic intervention. This review presents a systematic summary of nine chemotypes of small-molecule SIRT2 inhibitors, particularly including the discovery and structural optimization strategies, which will be useful for future efforts to develop new inhibitors targeting SIRT2 and associated target proteins.