Optimisation of a triazolopyridine based histone demethylase inhibitor yields a potent and selective KDM2A (FBXL11) inhibitor.
Optimisation of a triazolopyridine based histone demethylase inhibitor yields a potent and selective KDM2A (FBXL11) inhibitor.
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DOI：
10.1039/c4md00291a
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发表时间：
2014-12-01
期刊：
影响因子：
--
通讯作者：
Brennan PE
中科院分区：
文献类型：
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作者：
England KS;Tumber A;Krojer T;Scozzafava G;Ng SS;Daniel M;Szykowska A;Che K;von Delft F;Burgess-Brown NA;Kawamura A;Schofield CJ;Brennan PE
已经开发了一种JmjC组蛋白赖氨酸脱甲基酶KDM 2A（化合物35，pIC 50 7.2）的有效抑制剂，其对来自其他KDM亚家族的代表具有优异的选择性;发现三唑并吡啶化合物与JmjC KDM的活性位点结合之后，对KDM 2A抑制和选择性的三唑取代基进行了优化。
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.