Highly fluorescent and HDAC6 selective scriptaid analogues

Fleming, Cassandra L.; Natoli, Anthony; Schreuders, Jeannette; Devlin, Mark; Yoganantharajah, Prusothman; Gibert, Yann; Leslie, Kathryn G.; New, Elizabeth J.; Ashton, Trent D.; Pfeffer, Frederick M.

doi:10.1016/j.ejmech.2018.11.020

Cited by 22 publications

(17 citation statements)

References 81 publications

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“…Scriptaid, M344, BML281, and SAHA are pan-HDAC inhibitors that are known to inhibit both nuclear and cytoplasmic HDACs [6,47,48,49,50] (Table 1). Depending on the subcellular localization, HDAC enzymes can be divided into three classes [51].…”

Section: Resultsmentioning

confidence: 99%

Pan-HDAC Inhibitors Promote Tau Aggregation by Increasing the Level of Acetylated Tau

Jeong

Shin

Lee

et al. 2019

IJMS

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Epigenetic remodeling via histone acetylation has become a popular therapeutic strategy to treat Alzheimer’s disease (AD). In particular, histone deacetylase (HDAC) inhibitors including M344 and SAHA have been elucidated to be new drug candidates for AD, improving cognitive abilities impaired in AD mouse models. Although emerged as a promising target for AD, most of the HDAC inhibitors are poorly selective and could cause unwanted side effects. Here we show that tau is one of the cytosolic substrates of HDAC and the treatment of HDAC inhibitors such as Scriptaid, M344, BML281, and SAHA could increase the level of acetylated tau, resulting in the activation of tau pathology.

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Section: Resultsmentioning

confidence: 99%

Pan-HDAC Inhibitors Promote Tau Aggregation by Increasing the Level of Acetylated Tau

Jeong

Shin

Lee

et al. 2019

IJMS

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“…Histone deacetylase inhibitors (HDACIs), as an important class of antitumor drugs, were capable of either altering gene transcription or inhibiting HDAC activity, and thereby affecting the cell growth inhibition, differentiation, apoptosis, and tumor angiogenesis. [44][45][46] Previous studies have shown that HDACIs not only induce histone H3 hyperacetylation (Ac-histone H3), but also up-regulate expression of p21 gene. 47 Thus, the expressions of Ac-histone H3 and p21 proteins in MDA-MB-231 cells were evaluated by western blot assay.…”

Section: Cc5 Induced Apoptotic Cell Death and Western Blot Analysismentioning

confidence: 99%

A light-controlled multi-step drug release nanosystem targeting tumor hypoxia for synergistic cancer therapy

Zhang

Zhou

et al. 2021

Chem. Sci.

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“…Fleming et al reported fluorescent scriptaid derivatives as novel HDAC6-specific binders. Compound 9 had high potency affinity of HDAC6 (IC 50 = 3.5 nM), outstanding selectivity (>100-7000 fold over other HDACs), along with ideal fluorescent parameters, warranting its application as a useful HDAC6-specific probe for in vitro cellular imaging and in vivo zebrafish imaging [68].…”

Section: Fatty Hydroxamic Acid-derived Hdac6 Inhibitorsmentioning

confidence: 99%

Recent Advances in Small Molecular Modulators Targeting Histone Deacetylase 6

Xiao

Zhang

2020

Future Drug. Discov.

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Histone deacetylase 6 (HDAC6) is a unique isozyme in the HDAC family with various distinguished characters. HDAC6 is predominantly localized in the cytoplasm and has several specific nonhistone substrates, such as α-tubulin, cortactin, Hsp90, tau and peroxiredoxins. Accumulating evidence reveals that targeting HDAC6 may serve as a promising therapeutic strategy for the treatment of cancers, neurological disorders and immune diseases, making the development of HDAC6 inhibitors particularly attractive. Recently, multitarget drug design and proteolysis targeting chimera technology have also been applied in the discovery of novel small molecular modulators targeting HDAC6. In this review, we briefly describe the structural features and biological functions of HDAC6 and discuss the recent advances in HDAC6 modulators, including selective inhibitors, chimeric inhibitors and proteolysis targeting chimeras for multiple therapeutic purposes.

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Highly fluorescent and HDAC6 selective scriptaid analogues

Cited by 22 publications

References 81 publications

Pan-HDAC Inhibitors Promote Tau Aggregation by Increasing the Level of Acetylated Tau

Pan-HDAC Inhibitors Promote Tau Aggregation by Increasing the Level of Acetylated Tau

A light-controlled multi-step drug release nanosystem targeting tumor hypoxia for synergistic cancer therapy

Recent Advances in Small Molecular Modulators Targeting Histone Deacetylase 6

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