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 (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.
authors.affiliation: Chemogenomics Laboratory, Research Program on Biomedical Informatics, IMIM Hospital del Mar Research Institute and Universitat Pompeu Fabra, Doctor Aiguader 88, 08003 Barcelona, Catalonia, Spain.
authors.forename: Albert A
authors.initials: AA
authors.lastname: Antolín
authors.forename: Xavier
authors.initials: X
authors.lastname: Jalencas
authors.forename: José
authors.initials: J
authors.lastname: Yélamos
authors.forename: Jordi
authors.initials: J
authors.lastname: Mestres
mesh_terms: D004791:Enzyme Inhibitors / Q000494:pharmacology*; D006801:Humans; D020128:Inhibitory Concentration 50; D008958:Models, Molecular; D010616:Phenanthrenes / Q000494:pharmacology*; D000067856:Poly(ADP-ribose) Polymerase Inhibitors; D051573:Proto-Oncogene Proteins c-pim-1 / Q000037:antagonists & inhibitors*
chemical_list: D004791:Enzyme Inhibitors; C434926:N-(oxo-5,6-dihydrophenanthridin-2-yl)-N,N-dimethylacetamide hydrochloride; D010616:Phenanthrenes; D000067856:Poly(ADP-ribose) Polymerase Inhibitors; D051573:Proto-Oncogene Proteins c-pim-1; C406031:proto-oncogene proteins pim