Literature DB >> 18942826

Inhibitor scaffolds for 2-oxoglutarate-dependent histone lysine demethylases.

Nathan R Rose1, Stanley S Ng, Jasmin Mecinović, Benoît M R Liénard, Simon H Bello, Zhe Sun, Michael A McDonough, Udo Oppermann, Christopher J Schofield.   

Abstract

The dynamic methylation of histone lysyl residues plays an important role in biology by regulating transcription, maintaining genomic integrity, and by contributing to epigenetic effects. Here we describe a variety of inhibitor scaffolds that inhibit the human 2-oxoglutarate-dependent JMJD2 subfamily of histone demethylases. Combined with structural data, these chemical starting points will be useful to generate small-molecule probes to analyze the physiological roles of these enzymes in epigenetic signaling.

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Year:  2008        PMID： 18942826     DOI： 10.1021/jm800936s

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


  83 in total

Review 1.  Epigenetic protein families: a new frontier for drug discovery.

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Journal:  Nat Rev Drug Discov       Date:  2012-04-13       Impact factor: 84.694

Review 2.  Chemical and biochemical approaches in the study of histone methylation and demethylation.

Authors:  Keqin Kathy Li; Cheng Luo; Dongxia Wang; Hualiang Jiang; Y George Zheng
Journal:  Med Res Rev       Date:  2012-07       Impact factor: 12.944

3.  Plant growth regulator daminozide is a selective inhibitor of human KDM2/7 histone demethylases.

Authors:  Nathan R Rose; Esther C Y Woon; Anthony Tumber; Louise J Walport; Rasheduzzaman Chowdhury; Xuan Shirley Li; Oliver N F King; Clarisse Lejeune; Stanley S Ng; Tobias Krojer; Mun Chiang Chan; Anna M Rydzik; Richard J Hopkinson; Ka Hing Che; Michelle Daniel; Claire Strain-Damerell; Carina Gileadi; Grazyna Kochan; Ivanhoe K H Leung; James Dunford; Kar Kheng Yeoh; Peter J Ratcliffe; Nicola Burgess-Brown; Frank von Delft; Susanne Muller; Brian Marsden; Paul E Brennan; Michael A McDonough; Udo Oppermann; Robert J Klose; Christopher J Schofield; Akane Kawamura
Journal:  J Med Chem       Date:  2012-07-11       Impact factor: 7.446

Review 4.  Small molecule epigenetic inhibitors targeted to histone lysine methyltransferases and demethylases.

Authors:  Zhanxin Wang; Dinshaw J Patel
Journal:  Q Rev Biophys       Date:  2013-09-02       Impact factor: 5.318

5.  The small molecule JIB-04 disrupts O2 binding in the Fe-dependent histone demethylase KDM4A/JMJD2A.

Authors:  Barbara Cascella; Soon Goo Lee; Sukrit Singh; Joseph M Jez; Liviu M Mirica
Journal:  Chem Commun (Camb)       Date:  2017-02-09       Impact factor: 6.222

6.  Histone lysine demethylase (KDM) subfamily 4: structures, functions and therapeutic potential.

Authors:  Roselyne M Labbé; Andreana Holowatyj; Zeng-Quan Yang
Journal:  Am J Transl Res       Date:  2013-12-01       Impact factor: 4.060

Review 7.  The promise and failures of epigenetic therapies for cancer treatment.

Authors:  Pasano Bojang; Kenneth S Ramos
Journal:  Cancer Treat Rev       Date:  2013-07-05       Impact factor: 12.111

Review 8.  The TET enzymes.

Authors:  Peppi Koivunen; Tuomas Laukka
Journal:  Cell Mol Life Sci       Date:  2017-11-28       Impact factor: 9.261

9.  Inhibition of histone demethylases by 4-carboxy-2,2'-bipyridyl compounds.

Authors:  Kai-Hsuan Chang; Oliver N F King; Anthony Tumber; Esther C Y Woon; Tom D Heightman; Michael A McDonough; Christopher J Schofield; Nathan R Rose
Journal:  ChemMedChem       Date:  2011-03-15       Impact factor: 3.466

10.  Investigations on the oxygen dependence of a 2-oxoglutarate histone demethylase.

Authors:  Elena M Sánchez-Fernández; Hanna Tarhonskaya; Khalid Al-Qahtani; Richard J Hopkinson; James S O McCullagh; Christopher J Schofield; Emily Flashman
Journal:  Biochem J       Date:  2013-01-15       Impact factor: 3.857
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