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

Albert A. Antolín; Xavier Jalencas; José Yélamos; Jordi Mestres

doi:10.1021/cb300317y

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

Albert A. Antolín
, Xavier Jalencas
, José Yélamos
, Jordi Mestres

Pompeu Fabra University

Research output: Contribution to journal › Scientific article › peer-review

63 Citations (Scopus)

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 (IC₅₀ = 3.7 μM) and Pim2 (IC₅₀ = 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.

Original language	English
Pages (from-to)	1962-1967
Number of pages	6
Journal	ACS Chemical Biology
Volume	7
Issue number	12
DOIs	https://doi.org/10.1021/cb300317y
Publication status	Published - 21 Dec 2012
Externally published	Yes

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10.1021/cb300317y

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title = "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 (IC50 = 3.7 μM) and Pim2 (IC50 = 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.",

author = "Antol{\'i}n, \{Albert A.\} and Xavier Jalencas and Jos{\'e} Y{\'e}lamos and Jordi Mestres",

year = "2012",

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doi = "10.1021/cb300317y",

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T1 - Identification of pim kinases as novel targets for PJ34 with confounding effects in PARP biology

AU - Antolín, Albert A.

AU - Jalencas, Xavier

AU - Yélamos, José

AU - Mestres, Jordi

PY - 2012/12/21

Y1 - 2012/12/21

N2 - 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 μM) and Pim2 (IC50 = 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.

AB - 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 μM) and Pim2 (IC50 = 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.

UR - https://www.scopus.com/pages/publications/84871588981

U2 - 10.1021/cb300317y

DO - 10.1021/cb300317y

M3 - Scientific article

C2 - 23025350

AN - SCOPUS:84871588981

SN - 1554-8929

VL - 7

SP - 1962

EP - 1967

JO - ACS Chemical Biology

JF - ACS Chemical Biology

IS - 12

ER -

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

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