Literature DB >> 22575654

Identification of catechols as histone-lysine demethylase inhibitors.

Anders L Nielsen1, Line H Kristensen, Karen B Stephansen, Jan B L Kristensen, Charlotte Helgstrand, Michael Lees, Paul Cloos, Kristian Helin, Michael Gajhede, Lars Olsen.   

Abstract

Identification of inhibitors of histone-lysine demethylase (HDM) enzymes is important because of their involvement in the development of cancer. An ELISA-based assay was developed for identification of inhibitors of the HDM KDM4C in a natural products library. Based on one of the hits with affinity in the low μM range (1, a catechol), a subset of structurally related compounds was selected and tested against a panel of HDMs. In this subset, two inhibitors (2 and 10) had comparable affinities towards KDM4C and KDM6A but no effect on PHF8. One inhibitor restored H3K9me3 levels in KDM4C transfected U2-OS cells.
Copyright © 2012 Federation of European Biochemical Societies. Published by Elsevier B.V. All rights reserved.

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Year:  2012        PMID： 22575654     DOI： 10.1016/j.febslet.2012.03.001

Source DB:  PubMed          Journal:  FEBS Lett        ISSN： 0014-5793            Impact factor:   4.124


  14 in total

Review 1.  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

Review 2.  The role of histone demethylases in cancer therapy.

Authors:  Inga Hoffmann; Martin Roatsch; Martin L Schmitt; Luca Carlino; Martin Pippel; Wolfgang Sippl; Manfred Jung
Journal:  Mol Oncol       Date:  2012-08-07       Impact factor: 6.603

Review 3.  Histone demethylases in physiology and cancer: a tale of two enzymes, JMJD3 and UTX.

Authors:  Kelly Marie Arcipowski; Carlos Alberto Martinez; Panagiotis Ntziachristos
Journal:  Curr Opin Genet Dev       Date:  2016-05-03       Impact factor: 5.578

4.  Pro-growth role of the JMJD2C histone demethylase in HCT-116 colon cancer cells and identification of curcuminoids as JMJD2 inhibitors.

Authors:  Tae-Dong Kim; James R Fuchs; Eric Schwartz; Dalia Abdelhamid; Jonathan Etter; William L Berry; Chenglong Li; Michael A Ihnat; Pui-Kai Li; Ralf Janknecht
Journal:  Am J Transl Res       Date:  2014-05-15       Impact factor: 4.060

5.  Identification of small molecule inhibitors of Jumonji AT-rich interactive domain 1B (JARID1B) histone demethylase by a sensitive high throughput screen.

Authors:  Joyce Sayegh; Jian Cao; Mike Ran Zou; Alfonso Morales; Lauren P Blair; Michael Norcia; Denton Hoyer; Alan J Tackett; Jane S Merkel; Qin Yan
Journal:  J Biol Chem       Date:  2013-02-13       Impact factor: 5.157

6.  Aspartate/asparagine-β-hydroxylase: a high-throughput mass spectrometric assay for discovery of small molecule inhibitors.

Authors:  Lennart Brewitz; Anthony Tumber; Inga Pfeffer; Michael A McDonough; Christopher J Schofield
Journal:  Sci Rep       Date:  2020-05-26       Impact factor: 4.379

7.  An high-throughput in vivo screening system to select H3K4-specific histone demethylase inhibitors.

Authors:  Cecilia Mannironi; Marco Proietto; Francesca Bufalieri; Enrico Cundari; Angela Alagia; Svetlana Danovska; Teresa Rinaldi; Valeria Famiglini; Antonio Coluccia; Giuseppe La Regina; Romano Silvestri; Rodolfo Negri
Journal:  PLoS One       Date:  2014-01-29       Impact factor: 3.240

Review 8.  The H3K27me3 demethylase UTX in normal development and disease.

Authors:  Joni Van der Meulen; Frank Speleman; Pieter Van Vlierberghe
Journal:  Epigenetics       Date:  2014-02-21       Impact factor: 4.528

Review 9.  Discovery and resupply of pharmacologically active plant-derived natural products: A review.

Authors:  Atanas G Atanasov; Birgit Waltenberger; Eva-Maria Pferschy-Wenzig; Thomas Linder; Christoph Wawrosch; Pavel Uhrin; Veronika Temml; Limei Wang; Stefan Schwaiger; Elke H Heiss; Judith M Rollinger; Daniela Schuster; Johannes M Breuss; Valery Bochkov; Marko D Mihovilovic; Brigitte Kopp; Rudolf Bauer; Verena M Dirsch; Hermann Stuppner
Journal:  Biotechnol Adv       Date:  2015-08-15       Impact factor: 14.227

Review 10.  Lysine Demethylases: Promising Drug Targets in Melanoma and Other Cancers.

Authors:  Gaya Punnia-Moorthy; Peter Hersey; Abdullah Al Emran; Jessamy Tiffen
Journal:  Front Genet       Date:  2021-06-16       Impact factor: 4.599
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