Journal article

Optimisation of a triazolopyridine based histone demethylase inhibitor yields a potent and selective KDM2A (FBXL11) inhibitor

Abstract:: A potent inhibitor of the JmjC histone lysine demethylase KDM2A (compound 35, pIC50 7.2) with excellent selectivity over representatives from other KDM subfamilies has been developed; the discovery that a triazolopyridine compound binds to the active site of JmjC KDMs was followed by optimisation of the triazole substituent for KDM2A inhibition and selectivity. This journal is

Publication status:: Published

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APA Style

England, K., Tumber, A., Krojer, T., Scozzafava, G., Ng, S., Daniel, M., Szykowska, A., Che, K., von Delft, F., Burgess-Brown, N., Kawamura, A., Schofield, C., & Brennan, P. (2014). Optimisation of a triazolopyridine based histone demethylase inhibitor yields a potent and selective KDM2A (FBXL11) inhibitor. MEDCHEMCOMM, 5(12), 1879–1886.

MLA Style

England, K, et al. “Optimisation of a Triazolopyridine Based Histone Demethylase Inhibitor Yields a Potent and Selective KDM2A (FBXL11) Inhibitor.” MEDCHEMCOMM, vol. 5, no. 12, 2014, pp. 1879–86.

Chicago Style

England, K, A Tumber, T Krojer, et al. 2014. “Optimisation of a Triazolopyridine Based Histone Demethylase Inhibitor Yields a Potent and Selective KDM2A (FBXL11) Inhibitor.” MEDCHEMCOMM 5 (12): 1879–86.
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Publisher copy:: 10.1039/c4md00291a

Authors

+ England, K More by this author

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+ Tumber, A More by this author

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+ Krojer, T More by this author

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+ Scozzafava, G More by this author

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+ Ng, S More by this author

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Publisher:: Royal Society of Chemistry
Journal:: MEDCHEMCOMM More from this journal
Volume:: 5
Issue:: 12
Pages:: 1879-1886
Publication date:: 2014-01-01
DOI:: 10.1039/c4md00291a
EISSN:: 2040-2511
ISSN:: 2040-2503

Language:: English
Pubs id:: pubs:492501
UUID:: uuid:c8e6bc5c-c1a6-4979-89ab-3e329b8a4b44
Local pid:: pubs:492501
Source identifiers:: 492501
Deposit date:: 2014-12-19
ARK identifier:: ark:/29072/ora_c8e6bc5cc1a6497989ab3e329b8a4b44

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Copyright date:: 2014

Licence:: Terms and Conditions of Use for Oxford University Research Archive

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