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EPITOOLS SIGNED

Chemical biology approaches to unraveling the histone code

Total Cost €

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EC-Contrib. €

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Partnership

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Project "EPITOOLS" data sheet

The following table provides information about the project.

Coordinator
THE CHANCELLOR, MASTERS AND SCHOLARS OF THE UNIVERSITY OF OXFORD 

Organization address
address: WELLINGTON SQUARE UNIVERSITY OFFICES
city: OXFORD
postcode: OX1 2JD
website: www.ox.ac.uk

contact info
title: n.a.
name: n.a.
surname: n.a.
function: n.a.
email: n.a.
telephone: n.a.
fax: n.a.

 Coordinator Country United Kingdom [UK]
 Total cost 1˙758˙846 €
 EC max contribution 1˙758˙846 € (100%)
 Programme 1. H2020-EU.1.1. (EXCELLENT SCIENCE - European Research Council (ERC))
 Code Call ERC-2015-STG
 Funding Scheme ERC-STG
 Starting year 2016
 Duration (year-month-day) from 2016-04-01   to  2021-03-31

 Partnership

Take a look of project's partnership.

# participants  country  role  EC contrib. [€] 
1    THE CHANCELLOR, MASTERS AND SCHOLARS OF THE UNIVERSITY OF OXFORD UK (OXFORD) coordinator 1˙758˙846.00

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 Project objective

Posttranslational modifications on histones play crucial roles in the epigenetic regulation of eukaryotic gene expression. Chemical modifications that occur on histone tails include acetylation, methylation, phosphorylation, ubiquitination, and SUMOylation. This chemical diversity together with the positions and combinations of these modifications give rise to complex networks of highly controlled gene expression programs. The identification and characterisation of chromatin-associated proteins (or epigenetic regulators) in recent years has advanced our understanding of the significance of these histone modifications and the regulatory outcomes in development and in disease. The project aims to generate new classes of highly selective and potent chemical probes for epigenetic regulators, focusing on enzymes and proteins associated with methyl-lysine marks. A novel modified peptide-based discovery platform, which combines molecular, chemical, biophysical and cellular techniques, will be developed and applied. These chemical probes will be useful for biological and biomedical research, and will serve as potential starting points for therapeutic epigenetic intervention.

 Publications

year authors and title journal last update
List of publications.
2017 Akane Kawamura, Martin Münzel, Tatsuya Kojima, Clarence Yapp, Bhaskar Bhushan, Yuki Goto, Anthony Tumber, Takayuki Katoh, Oliver N. F. King, Toby Passioura, Louise J. Walport, Stephanie B. Hatch, Sarah Madden, Susanne Müller, Paul E. Brennan, Rasheduzzaman Chowdhury, Richard J. Hopkinson, Hiroaki Suga, Christopher J. Schofield
Highly selective inhibition of histone demethylases by de novo macrocyclic peptides
published pages: 14773, ISSN: 2041-1723, DOI: 10.1038/ncomms14773
Nature Communications 8 2019-06-19
2018 Toby Passioura, Bhaskar Bhushan, Anthony Tumber, Akane Kawamura, Hiroaki Suga
Structure-activity studies of a macrocyclic peptide inhibitor of histone lysine demethylase 4A
published pages: 1225-1231, ISSN: 0968-0896, DOI: 10.1016/j.bmc.2018.01.013
Bioorganic & Medicinal Chemistry 26/6 2019-04-18
2018 Kosuke Nishio, Roman Belle, Takayuki Katoh, Akane Kawamura, Toru Sengoku, Kazuharu Hanada, Noboru Ohsawa, Mikako Shirouzu, Shigeyuki Yokoyama, Hiroaki Suga
Thioether Macrocyclic Peptides Selected against TET1 Compact Catalytic Domain Inhibit TET1 Catalytic Activity
published pages: 979-985, ISSN: 1439-4227, DOI: 10.1002/cbic.201800047
ChemBioChem 19/9 2019-04-18
2018 Bhaskar Bhushan, Alexandre Erdmann, Yijia Zhang, Roman Belle, Catrine Johannson, Udo Oppermann, Richard J. Hopkinson, Christopher J. Schofield, Akane Kawamura
Investigations on small molecule inhibitors targeting the histone H3K4 tri-methyllysine binding PHD-finger of JmjC histone demethylases
published pages: 2984-2991, ISSN: 0968-0896, DOI: 10.1016/j.bmc.2018.03.030
Bioorganic & Medicinal Chemistry 26/11 2019-04-18
2018 T. E. McAllister, T.-L. Yeh, M. I. Abboud, I. K. H. Leung, E. S. Hookway, O. N. F. King, B. Bhushan, S. T. Williams, R. J. Hopkinson, M. Münzel, N. D. Loik, R. Chowdhury, U. Oppermann, T. D. W. Claridge, Y. Goto, H. Suga, C. J. Schofield, A. Kawamura
Non-competitive cyclic peptides for targeting enzyme–substrate complexes
published pages: 4569-4578, ISSN: 2041-6520, DOI: 10.1039/c8sc00286j
Chemical Science 9/20 2019-04-18
2018 Louise J. Walport, Richard J. Hopkinson, Rasheduzzaman Chowdhury, Yijia Zhang, Joanna Bonnici, Rachel Schiller, Akane Kawamura, Christopher J. Schofield
Mechanistic and structural studies of KDM-catalysed demethylation of histone 1 isotype 4 at lysine 26
published pages: 3264-3273, ISSN: 0014-5793, DOI: 10.1002/1873-3468.13231
FEBS Letters 592/19 2019-04-18
2017 Roman Belle, Abbas H. K. Al Temimi, Kiran Kumar, Bas J. G. E. Pieters, Anthony Tumber, James E. Dunford, Catrine Johansson, Udo Oppermann, Tom Brown, Christopher J. Schofield, Richard J. Hopkinson, Robert S. Paton, Akane Kawamura, Jasmin Mecinović
Investigating d -lysine stereochemistry for epigenetic methylation, demethylation and recognition
published pages: 13264-13267, ISSN: 1359-7345, DOI: 10.1039/c7cc08028j
Chemical Communications 53/99 2019-04-18

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