TY  - JOUR
PY  - 2020//
TI  - Unexpected small molecules as novel SIRT2 suicide inhibitors
JO  - Bioorganic and medicinal chemistry
A1  - Chen, Xiaoxue
A1  - Zou, Yefang
A1  - Wang, Jie
A1  - Cao, Zhuoxian
A1  - Liu, Jingzi
A1  - Li, Yan
A1  - Zhao, Yonglong
A1  - He, Bin
SP  - e115353
EP  - e115353
VL  - 28
IS  - 6
N2  - A series of sirtuin inhibitor candidates were assembled based on an intermediate ester (1a) our accidently discovered. After screening and evaluation, several SIRT2 selective inhibitors were identified, which can inhibit all the deacetylation, defatty-acylation and debenzoylation of SIRT2. Among these inhibitors, compound 1e was the best SIRT2 selective inhibitors. The primary study on the inhibitory mechanism indicated that compound 1e may be a suicide inhibitor acting as an irreversible way. Given almost all reported sirtuin inhibitors are non-covalent, sirtuin covalent inhibitors are still need to be developed. These findings will facilitate for further development of SIRT2 selective and suicide inhibitors.<p /> <p>Language: en</p>
LA  - en
SN  - 0968-0896
UR  - http://dx.doi.org/10.1016/j.bmc.2020.115353
ID  - ref1
ER  -