Bioorganic and Medicinal Chemistry Letters p. 180 - 186 (2017)
Update date:2022-08-10
Topics:
Wang, Juan
Zang, Wenwen
Liu, Jiajia
Zheng, Weiping
In the current study, bivalent compounds 1–17 constructed by covalently linking the ?-amino group of lysine in a tripeptidic scaffold to a functionality via a linker were prepared and examined for their inhibitory potencies against SIRT1, a prototypical member of the β-nicotinamide adenine dinucleotide (β-NAD+)-dependent sirtuin family of protein Nε-acyl-lysine deacylases. A few of them were found to be stronger SIRT1 inhibitors than the N?-acetyl-lysine-containing monovalent counterparts 18 and 19. As exemplified with compounds 6 and 18, a bivalent SIRT1 inhibitor could exhibit a greater degree of inhibitory selectivity among SIRT1/2/3 than the corresponding monovalent counterpart. This study has laid a foundation for the future development of superior bivalent inhibitors against the (patho)physiologically and therapeutically important sirtuin family of deacylase enzymes.
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Doi:10.1021/j100458a019
(1980)Doi:10.1016/S0040-4039(01)98863-X
(1968)Doi:10.1021/jacs.6b07826
(2016)Doi:10.1016/j.ica.2015.08.016
(2015)Doi:10.1039/c4sm02239d
(2015)Doi:10.1055/s-2005-861830
(2005)