|ZFIN ID: ZDB-PUB-181119-5|
Highly fluorescent and HDAC6 selective scriptaid analogues
Fleming, C.L., Natoli, A., Schreuders, J., Devlin, M., Yoganantharajah, P., Gibert, Y., Leslie, K.G., New, E.J., Ashton, T.D., Pfeffer, F.M.
|Source:||European Journal of Medicinal Chemistry 162: 321-333 (Journal)|
|Registered Authors:||Gibert, Yann|
|Keywords:||4MS, Fluorescence, HDAC, Imaging, Naphthalimide, Scriptaid, Zebrafish|
|PubMed:||30448419 Full text @ Eur. J. Med. Chem.|
Fleming, C.L., Natoli, A., Schreuders, J., Devlin, M., Yoganantharajah, P., Gibert, Y., Leslie, K.G., New, E.J., Ashton, T.D., Pfeffer, F.M. (2018) Highly fluorescent and HDAC6 selective scriptaid analogues. European Journal of Medicinal Chemistry. 162:321-333.
ABSTRACTFluorescent scriptaid analogues with excellent HDAC6 selectivity (HDAC1/6 > 500) and potency (HDAC6 IC50 < 5 nM) have been synthesised and evaluated. The highly fluorescent nature of the compounds (up to ΦF = 0.83 in DMSO and 0.38 in aqueous buffer) makes them ideally suited for cellular imaging and visualisation of their cytoplasmic localisation was readily accomplished. Whole organism imaging in zebrafish confirmed both the vascular localisation of the new inhibitors and the impact of HDAC6 inhibition on in vivo development.
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