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Optimisation of a triazolopyridine based histone demethylase inhibitor yields a potent and selective KDM2A (FBXL11) inhibitor
A potent inhibitor of the JmjC histone lysine demethylase KDM2A (compound 35, pIC(50) 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...
| Autores principales: | , , , , , , , , , , , , |
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| Formato: | Online Artículo Texto |
| Lenguaje: | English |
| Publicado: |
2014
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| Materias: | |
| Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4678576/ https://www.ncbi.nlm.nih.gov/pubmed/26682034 http://dx.doi.org/10.1039/C4MD00291A |
| _version_ | 1782405468913664000 |
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| author | England, Katherine S. Tumber, Anthony Krojer, Tobias Scozzafava, Giuseppe Ng, Stanley S. Daniel, Michelle Szykowska, Aleksandra Che, KaHing von Delft, Frank Burgess-Brown, Nicola A. Kawamura, Akane Schofield, Christopher J. Brennan, Paul E. |
| author_facet | England, Katherine S. Tumber, Anthony Krojer, Tobias Scozzafava, Giuseppe Ng, Stanley S. Daniel, Michelle Szykowska, Aleksandra Che, KaHing von Delft, Frank Burgess-Brown, Nicola A. Kawamura, Akane Schofield, Christopher J. Brennan, Paul E. |
| author_sort | England, Katherine S. |
| collection | PubMed |
| description | A potent inhibitor of the JmjC histone lysine demethylase KDM2A (compound 35, pIC(50) 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. |
| format | Online Article Text |
| id | pubmed-4678576 |
| institution | National Center for Biotechnology Information |
| language | English |
| publishDate | 2014 |
| record_format | MEDLINE/PubMed |
| spelling | pubmed-46785762015-12-15 Optimisation of a triazolopyridine based histone demethylase inhibitor yields a potent and selective KDM2A (FBXL11) inhibitor England, Katherine S. Tumber, Anthony Krojer, Tobias Scozzafava, Giuseppe Ng, Stanley S. Daniel, Michelle Szykowska, Aleksandra Che, KaHing von Delft, Frank Burgess-Brown, Nicola A. Kawamura, Akane Schofield, Christopher J. Brennan, Paul E. Medchemcomm Article A potent inhibitor of the JmjC histone lysine demethylase KDM2A (compound 35, pIC(50) 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. 2014-12-01 /pmc/articles/PMC4678576/ /pubmed/26682034 http://dx.doi.org/10.1039/C4MD00291A Text en http://creativecommons.org/licenses/by/3.0/ This article is licensed under a Creative Commons Attribution 3.0 Unported Licence. |
| spellingShingle | Article England, Katherine S. Tumber, Anthony Krojer, Tobias Scozzafava, Giuseppe Ng, Stanley S. Daniel, Michelle Szykowska, Aleksandra Che, KaHing von Delft, Frank Burgess-Brown, Nicola A. Kawamura, Akane Schofield, Christopher J. Brennan, Paul E. Optimisation of a triazolopyridine based histone demethylase inhibitor yields a potent and selective KDM2A (FBXL11) inhibitor |
| title | Optimisation of a triazolopyridine based histone demethylase inhibitor yields a potent and selective KDM2A (FBXL11) inhibitor |
| title_full | Optimisation of a triazolopyridine based histone demethylase inhibitor yields a potent and selective KDM2A (FBXL11) inhibitor |
| title_fullStr | Optimisation of a triazolopyridine based histone demethylase inhibitor yields a potent and selective KDM2A (FBXL11) inhibitor |
| title_full_unstemmed | Optimisation of a triazolopyridine based histone demethylase inhibitor yields a potent and selective KDM2A (FBXL11) inhibitor |
| title_short | Optimisation of a triazolopyridine based histone demethylase inhibitor yields a potent and selective KDM2A (FBXL11) inhibitor |
| title_sort | optimisation of a triazolopyridine based histone demethylase inhibitor yields a potent and selective kdm2a (fbxl11) inhibitor |
| topic | Article |
| url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4678576/ https://www.ncbi.nlm.nih.gov/pubmed/26682034 http://dx.doi.org/10.1039/C4MD00291A |
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