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Cyclic tripeptide-based potent human SIRT7 inhibitors.
- Source :
-
Bioorganic & Medicinal Chemistry Letters . Feb2019, Vol. 29 Issue 3, p461-465. 5p. - Publication Year :
- 2019
-
Abstract
- Graphical abstract Highlights • Two first examples of potent (low μM) inhibitors against the tRNA-activated human SIRT7 deacetylase activity were found. • The two inhibitors are cyclic tripeptides each harboring a catalytic mechanism-based sirtuin inhibitory warhead. • The two inhibitors also exhibited potent (low μM) inhibition against the deacylase activities of human SIRT1/2/3/6. • Our finding could facilitate the future development of more potent and selective human SIRT7 inhibitors. Abstract In the current study, two cyclic tripeptides respectively harboring a thiourea-type and a carboxamide-type of catalytic mechanism-based sirtuin inhibitory warheads as the central residue were found to behave as potent (low μM level) inhibitors against the tRNA-activated human SIRT7 deacetylase activity. Despite exhibiting a potent pan-inhibition against the deacylase activities of the five tested human sirtuins (i.e. SIRT1/2/3/6/7), these two compounds represent the first examples of potent SIRT7 inhibitors ever identified thus far, and their identification could facilitate the future development of more potent and selective SIRT7 inhibitors. [ABSTRACT FROM AUTHOR]
- Subjects :
- *DEACETYLASES
*TRIPEPTIDES
*CHEMICAL inhibitors
*DEACETYLATION
*MECHANICAL movements
Subjects
Details
- Language :
- English
- ISSN :
- 0960894X
- Volume :
- 29
- Issue :
- 3
- Database :
- Academic Search Index
- Journal :
- Bioorganic & Medicinal Chemistry Letters
- Publication Type :
- Academic Journal
- Accession number :
- 134253294
- Full Text :
- https://doi.org/10.1016/j.bmcl.2018.12.023