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Development of Thiazolidinedione-Based HDAC6 Inhibitors to Overcome Methamphetamine Addiction

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Author(s)
서지혜
Alternative Author(s)
Seo, Ji Hye
Issued Date
2019
Keyword
HDAC6 inhibitorsdrug addictionmethamphetaminethiazolidinedione
Abstract
Thiazolidinedione is a five-membered heterocycle that is widely used in drug discovery endeavors. In this study, we report the design, synthesis, and biological evaluation of a series of thiazolidinedione-based HDAC6 inhibitors. In particular, compound 6b exerts an excellent inhibitory activity against HDAC6 with an IC50 value of 21 nM, displaying a good HDAC6 selectivity over HDAC1. Compound 6b dose-dependently induces the acetylation level of α-tubulin via inhibition of HDAC6 in human neuroblastoma SH-SY5Y cell line. Moreover, compound 6b efficiently reverses methamphetamine-induced morphology changes of SH-SY5Y cells via regulating acetylation landscape of α-tubulin. Collectively, compound 6b represents a novel HDAC6-isoform selective inhibitor and demonstrates promising therapeutic potential for the treatment of methamphetamine addiction.
Department
Dept. of Biochemistry (생화학)
Publisher
School of Medicine (의과대학)
Citation
International journal of molecular sciences, Vol.20(24) : 6213-6213, 2019
Type
Article
ISSN
1422-0067
DOI
10.3390/ijms20246213
URI
http://kumel.medlib.dsmc.or.kr/handle/2015.oak/42634
Appears in Collections:
1. School of Medicine (의과대학) > Dept. of Biochemistry (생화학)
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