Identification of pim kinases as novel targets for PJ34 with confounding effects in PARP biology.

Abstract:

: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 (IC(50) = 3.7 μM) and Pim2 (IC(50) = 16 μM) 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.

journal_name

ACS Chem Biol

journal_title

ACS chemical biology

authors

Antolín AA,Jalencas X,Yélamos J,Mestres J

doi

10.1021/cb300317y

subject

Has Abstract

pub_date

2012-12-21 00:00:00

pages

1962-7

issue

12

eissn

1554-8929

issn

1554-8937

journal_volume

7

pub_type

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