Antiproliferation and Antiencystation Effect of Class II Histone Deacetylase Inhibitors on Acanthamoeba castellanii

2022 ◽  
Author(s):  
Ki-Back Chu ◽  
Hae-Ahm Lee ◽  
Marc Pflieger ◽  
Fabian Fischer ◽  
Yodita Asfaha ◽  
...  
Keyword(s):  
Histone Deacetylase ◽  
Histone Deacetylase Inhibitors ◽  
Acanthamoeba Castellanii ◽  
Class Ii

2-Trifluoroacetylthiophene oxadiazoles as potent and selective class II human histone deacetylase inhibitors

2008 ◽  
Vol 18 (23) ◽  
pp. 6083-6087 ◽  
Author(s):  
Ester Muraglia ◽  
Sergio Altamura ◽  
Danila Branca ◽  
Ottavia Cecchetti ◽  
Federica Ferrigno ◽  
...  
Keyword(s):  
Histone Deacetylase ◽  
Histone Deacetylase Inhibitors ◽  
Class Ii

Class II-selective histone deacetylase inhibitors. Part 2: Alignment-independent GRIND 3-D QSAR, homology and docking studies

2008 ◽  
Vol 43 (3) ◽  
pp. 621-632 ◽  
Author(s):  
Rino Ragno ◽  
Silvia Simeoni ◽  
Dante Rotili ◽  
Antonella Caroli ◽  
Giorgia Botta ◽  
...  
Keyword(s):  
Histone Deacetylase ◽  
Histone Deacetylase Inhibitors ◽  
Class Ii ◽  
Docking Studies

Class II (IIa)-Selective Histone Deacetylase Inhibitors. 1. Synthesis and Biological Evaluation of Novel (Aryloxopropenyl)pyrrolyl Hydroxyamides

2005 ◽  
Vol 48 (9) ◽  
pp. 3344-3353 ◽  
Author(s):  
Antonello Mai ◽  
Silvio Massa ◽  
Riccardo Pezzi ◽  
Silvia Simeoni ◽  
Dante Rotili ◽  
...  
Keyword(s):  
Histone Deacetylase ◽  
Histone Deacetylase Inhibitors ◽  
Class Ii ◽  
Biological Evaluation ◽  
Synthesis And Biological Evaluation

Class II-specific histone deacetylase inhibitors MC1568 and MC1575 suppress IL-8 expression in human melanoma cells

2013 ◽  
Vol 26 (2) ◽  
pp. 193-204 ◽  
Author(s):  
I. Venza ◽  
M. Visalli ◽  
R. Oteri ◽  
M. Cucinotta ◽  
D. Teti ◽  
...  
Keyword(s):  
Histone Deacetylase ◽  
Histone Deacetylase Inhibitors ◽  
Class Ii ◽  
Melanoma Cells ◽  
Human Melanoma ◽  
Human Melanoma Cells

scholarly journals Application of Histone Deacetylase Inhibitors MPK472 and KSK64 as a Potential Treatment Option for Acanthamoeba Keratitis

2020 ◽  
Vol 64 (12) ◽  
Author(s):  
Hae-Ahm Lee ◽  
So-Min Park ◽  
Ki-Back Chu ◽  
Fu-Shi Quan ◽  
Thomas Kurz ◽  
...  
Keyword(s):  
Histone Deacetylase ◽  
Histone Deacetylase Inhibitors ◽  
Apoptotic Cell ◽  
Therapeutic Option ◽  
Acanthamoeba Castellanii ◽  
Cyst Formation ◽  
Acanthamoeba Keratitis ◽  
Content Type ◽  
Cytopathic Effects ◽  
Transmission Electron

ABSTRACT Treatment of Acanthamoeba keratitis (AK) is difficult because Acanthamoeba cysts are resistant to drugs, and as such, successful treatment requires an effective approach that inhibits cyst formation. Histone deacetylase inhibitors (HDACis) are involved in cell proliferation, differentiation, and apoptotic cell death. In this study, the effects of HDACis such as MPK472 and KSK64 on Acanthamoeba castellanii trophozoites and cysts were observed. MPK472 and KSK64 showed at least 60% amoebicidal activity against Acanthamoeba trophozoites at a concentration of 10 μM upon 8 h of treatment. Neither of the two HDACis affected mature cysts, but significant amoebicidal activities (36.4 and 33.9%) were observed against encysting Acanthamoeba following treatment with 5 and 10 μM HDACis for 24 h. Light microscopy and transmission electron microscopy results confirmed that the encystation of Acanthamoeba was inhibited by the two HDACis. In addition to this, low cytopathic effects on human corneal epithelial (HCE) cells were observed following treatment with MPK472 and KSK64 for 24 h. Our results indicate that the HDACis MPK472 and KSK64 could be used as new candidates for the development of an optimal therapeutic option for AK.

Determination of the class and isoform selectivity of small-molecule histone deacetylase inhibitors

2007 ◽  
Vol 409 (2) ◽  
pp. 581-589 ◽  
Author(s):  
Nagma Khan ◽  
Michael Jeffers ◽  
Sampath Kumar ◽  
Craig Hackett ◽  
Ferenc Boldog ◽  
...  
Keyword(s):  
Histone Deacetylase ◽  
Histone Deacetylase Inhibitors ◽  
Trichostatin A ◽  
Hdac Inhibitors ◽  
Specific Inhibitor ◽  
Class Ii ◽  
Class I ◽  
Regulation Of Transcription ◽  
Control Of Gene Expression ◽  
Inhibitor Treatment

The human HDAC (histone deacetylase) family, a well-validated anticancer target, plays a key role in the control of gene expression through regulation of transcription. While HDACs can be subdivided into three main classes, the class I, class II and class III HDACs (sirtuins), it is presently unclear whether inhibiting multiple HDACs using pan-HDAC inhibitors, or targeting specific isoforms that show aberrant levels in tumours, will prove more effective as an anticancer strategy in the clinic. To address the above issues, we have tested a number of clinically relevant HDACis (HDAC inhibitors) against a panel of rhHDAC (recombinant human HDAC) isoforms. Eight rhHDACs were expressed using a baculoviral system, and a Fluor de Lys™ (Biomol International) HDAC assay was optimized for each purified isoform. The potency and selectivity of ten HDACs on class I isoforms (rhHDAC1, rhHDAC2, rhHDAC3 and rhHDAC8) and class II HDAC isoforms (rhHDAC4, rhHDAC6, rhHDAC7 and rhHDAC9) was determined. MS-275 was HDAC1-selective, MGCD0103 was HDAC1- and HDAC2-selective, apicidin was HDAC2- and HDAC3-selective and valproic acid was a specific inhibitor of class I HDACs. The hydroxamic acid-derived compounds (trichostatin A, NVP-LAQ824, panobinostat, ITF2357, vorinostat and belinostat) were potent pan-HDAC inhibitors. The growth-inhibitory effect of the HDACis on HeLa cells showed that both pan-HDAC and class-I-specific inhibitors inhibited cell growth. The results also showed that both pan-HDAC and class-I-specific inhibitor treatment resulted in increased acetylation of histones, but only pan-HDAC inhibitor treatment resulted in increased tubulin acetylation, which is in agreement with their activity towards the HDAC6 isoform.

Structural Origin of Selectivity in Class II-Selective Histone Deacetylase Inhibitors

2008 ◽  
Vol 51 (10) ◽  
pp. 2898-2906 ◽  
Author(s):  
Guillermina Estiu ◽  
Edward Greenberg ◽  
Christopher B. Harrison ◽  
Nicholas P. Kwiatkowski ◽  
Ralph Mazitschek ◽  
...  
Keyword(s):  
Histone Deacetylase ◽  
Histone Deacetylase Inhibitors ◽  
Class Ii

2-Trifluoroacetylthiophenes, a novel series of potent and selective class II histone deacetylase inhibitors

2008 ◽  
Vol 18 (11) ◽  
pp. 3456-3461 ◽  
Author(s):  
Philip Jones ◽  
Matthew J. Bottomley ◽  
Andrea Carfí ◽  
Ottavia Cecchetti ◽  
Federica Ferrigno ◽  
...  
Keyword(s):  
Histone Deacetylase ◽  
Histone Deacetylase Inhibitors ◽  
Class Ii
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