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

被引：56

作者：

Antolin, Albert A. ^{[1
]}

Jalencas, Xavier ^{[1
]}

Yelamos, Jose ^{[2
]}

Mestres, Jordi ^{[1
]}

机构：

[1] IMIM Hosp del Mar Res Inst, Chemogen Lab, Res Program Biomed Informat, Barcelona 08003, Catalonia, Spain

[2] IMIM Hosp del Mar Res Inst, Dept Immunol, Res Program Canc, Barcelona 08003, Catalonia, Spain

来源：

ACS CHEMICAL BIOLOGY | 2012年 / 7卷 / 12期

关键词：

POLY(ADP-RIBOSE); INHIBITION; EXPRESSION;

D O I：

10.1021/cb300317y

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

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.

引用

收藏

页码：1962 / 1967

页数：6

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