The (un)targeted cancer kinome
The (un)targeted cancer kinome
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DOI：
10.1038/nchembio.297
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发表时间：
2010-03-01
影响因子：
14.8
通讯作者：
Knapp, Stefan
中科院分区：
文献类型：
--
作者：
Fedorov, Oleg;Mueller, Susanne;Knapp, Stefan
癌症信号传导的复杂性以及由此导致的靶标选择困难，使激酶药物的发现强烈偏向于临床验证的靶标。最近，基因组测序和 RNAi 研究中出现了尚未表征的新激酶靶点。迫切需要化学探针来对这些激酶进行功能注释并刺激新药物的发现工作。
The complexity of cancer signaling and the resulting difficulties in target selection have strongly biased kinase drug discovery towards clinically validated targets. Recently, novel kinase targets that are uncharacterized have emerged from genome sequencing and RNAi studies. Chemical probes are urgently needed to functionally annotate these kinases and to stimulate new drug discovery efforts.