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Identification of Pim Kinases as Novel Targets for PJ34 with Confounding Effects in PARP Biology

  作者 ANTOLIN ALBERT A; JALENCAS XAVIER; YELAMOS JOSE; MESTRES JORDI  
  选自 期刊  ACS CHEMICAL BIOLOGY;  卷期  2012年7-12;  页码  1962-1967  
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[摘要]Small molecules are widely used in chemical biology without complete knowledge of their target profile, at risk of deriving conclusions that ignore potential confounding effects from unknown off-target interactions. The prediction and further experimental confirmation of novel affinities for PJ34 on Pim1 (IC50 = 3.7 mu M) and Pim2 (IC50 = 16 mu M) serine/threonine kinases, together with their involvement in many of the processes relevant to PARP biology, questions the appropriateness of using PJ34 as a chemical tool to probe the biological role of PARP1 and PARP2 at the high micromolar concentrations applied in most studies.

 
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