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Development of Thiazolidinedione-Based HDAC6 Inhibitors to Overcome Methamphetamine Addiction

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Author(s)
Chiranjeev SharmaYong Jin OhByoungduck ParkSooyeun LeeChul-Ho JeongSangkil LeeJi Hae SeoYoung Ho Seo
Keimyung Author(s)
Seo, Ji Hye
Department
Dept. of Biochemistry (생화학)
Journal Title
International journal of molecular sciences
Issued Date
2019
Volume
20
Issue
24
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.
Keimyung Author(s)(Kor)
서지혜
Publisher
School of Medicine (의과대학)
Citation
Chiranjeev Sharma et al. (2019). Development of Thiazolidinedione-Based HDAC6 Inhibitors to Overcome Methamphetamine Addiction. International journal of molecular sciences, 20(24), 6213–6213. doi: 10.3390/ijms20246213
Type
Article
ISSN
1422-0067
Source
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6940941/
DOI
10.3390/ijms20246213
URI
https://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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