Literature DB >> 23672185

Discovery of the first histone deacetylase 6/8 dual inhibitors.

David E Olson1, Florence F Wagner, Taner Kaya, Jennifer P Gale, Nadia Aidoud, Emeline L Davoine, Fanny Lazzaro, Michel Weïwer, Yan-Ling Zhang, Edward B Holson.   

Abstract

We disclose the first small molecule histone deacetylase (HDAC) inhibitor (3, BRD73954) capable of potently and selectively inhibiting both HDAC6 and HDAC8 despite the fact that these isoforms belong to distinct phylogenetic classes within the HDAC family of enzymes. Our data demonstrate that meta substituents of phenyl hydroxamic acids are readily accommodated upon binding to HDAC6 and, furthermore, are necessary for the potent inhibition of HDAC8.

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Year:  2013        PMID： 23672185     DOI： 10.1021/jm400390r

Source DB:  PubMed          Journal:  J Med Chem        ISSN： 0022-2623            Impact factor:   7.446


  20 in total

1.  Discovery of the First-in-Class Dual Histone Deacetylase-Proteasome Inhibitor.

Authors:  Sanil Bhatia; Viktoria Krieger; Michael Groll; Jeremy D Osko; Nina Reßing; Heinz Ahlert; Arndt Borkhardt; Thomas Kurz; David W Christianson; Julia Hauer; Finn K Hansen
Journal:  J Med Chem       Date:  2018-11-08       Impact factor: 7.446

2.  Human ATP-binding cassette transporters ABCB1 and ABCG2 confer resistance to histone deacetylase 6 inhibitor ricolinostat (ACY-1215) in cancer cell lines.

Authors:  Chung-Pu Wu; Ya-Ju Hsieh; Megumi Murakami; Shahrooz Vahedi; Sung-Han Hsiao; Ni Yeh; An-Wei Chou; Yan-Qing Li; Yu-Shan Wu; Jau-Song Yu; Suresh V Ambudkar
Journal:  Biochem Pharmacol       Date:  2018-07-17       Impact factor: 5.858

Review 3.  Histone deacetylases and their inhibitors in cancer, neurological diseases and immune disorders.

Authors:  Katrina J Falkenberg; Ricky W Johnstone
Journal:  Nat Rev Drug Discov       Date:  2014-08-18       Impact factor: 84.694

4.  Hydroxamate-based histone deacetylase inhibitors can protect neurons from oxidative stress via a histone deacetylase-independent catalase-like mechanism.

Authors:  David E Olson; Sama F Sleiman; Megan W Bourassa; Florence F Wagner; Jennifer P Gale; Yan-Ling Zhang; Rajiv R Ratan; Edward B Holson
Journal:  Chem Biol       Date:  2015-04-16

5.  Design, Synthesis, and Biological Evaluation of Tetrahydroisoquinoline-Based Histone Deacetylase 8 Selective Inhibitors.

Authors:  Taha Y Taha; Shaimaa M Aboukhatwa; Rachel C Knopp; Naohiko Ikegaki; Hazem Abdelkarim; Jayaprakash Neerasa; Yunlong Lu; Raghupathi Neelarapu; Thomas W Hanigan; Gregory R J Thatcher; Pavel A Petukhov
Journal:  ACS Med Chem Lett       Date:  2017-08-01       Impact factor: 4.345

6.  Structural Requirements of HDAC Inhibitors: SAHA Analogues Modified at the C2 Position Display HDAC6/8 Selectivity.

Authors:  Ahmed T Negmeldin; Geetha Padige; Anton V Bieliauskas; Mary Kay H Pflum
Journal:  ACS Med Chem Lett       Date:  2017-02-07       Impact factor: 4.345

7.  Development of a Potent and Selective HDAC8 Inhibitor.

Authors:  Oscar J Ingham; Ronald M Paranal; William B Smith; Randolph A Escobar; Han Yueh; Tracy Snyder; John A Porco; James E Bradner; Aaron B Beeler
Journal:  ACS Med Chem Lett       Date:  2016-09-01       Impact factor: 4.345

8.  The structural requirements of histone deacetylase inhibitors: SAHA analogs modified at the C5 position display dual HDAC6/8 selectivity.

Authors:  Ahmed T Negmeldin; Mary Kay H Pflum
Journal:  Bioorg Med Chem Lett       Date:  2017-06-13       Impact factor: 2.823

Review 9.  Small molecule inhibitors of zinc-dependent histone deacetylases.

Authors:  Florence F Wagner; Michel Weїwer; Michael C Lewis; Edward B Holson
Journal:  Neurotherapeutics       Date:  2013-10       Impact factor: 7.620

10.  The structural requirements of histone deacetylase inhibitors: C4-modified SAHA analogs display dual HDAC6/HDAC8 selectivity.

Authors:  Ahmed T Negmeldin; Joseph R Knoff; Mary Kay H Pflum
Journal:  Eur J Med Chem       Date:  2017-10-31       Impact factor: 6.514
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