Explore the words cloud of the EPITOOLS project. It provides you a very rough idea of what is the project "EPITOOLS" about.
The following table provides information about the project.
THE CHANCELLOR, MASTERS AND SCHOLARS OF THE UNIVERSITY OF OXFORD
|Coordinator Country||United Kingdom [UK]|
|Total cost||1˙758˙846 €|
|EC max contribution||1˙758˙846 € (100%)|
1. H2020-EU.1.1. (EXCELLENT SCIENCE - European Research Council (ERC))
|Duration (year-month-day)||from 2016-04-01 to 2021-03-31|
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|1||THE CHANCELLOR, MASTERS AND SCHOLARS OF THE UNIVERSITY OF OXFORD||UK (OXFORD)||coordinator||1˙758˙846.00|
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.
|year||authors and title||journal||last update|
Akane Kawamura, Martin MÃ¼nzel, 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 MÃ¼ller, 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|
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|
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
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|
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. MÃ¼nzel, 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 enzymeâ€“substrate complexes
published pages: 4569-4578, ISSN: 2041-6520, DOI: 10.1039/c8sc00286j
|Chemical Science 9/20||2019-04-18|
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|
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 MecinoviÄ‡
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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