Identification of potential cellular targets of aloisine A by affinity chromatography.

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Corbel C, Haddoub R, Guiffant D, Lozach O, Gueyrard D, Lemoine J, Ratin M, Meijer L, Bach S, Goekjian P

Identification of potential cellular targets of aloisine A by affinity chromatography.

Bioorg Med Chem. 2009 Aug 1;17(15):5572-82. doi: 10.1016/j.bmc.2009.06.024. Epub 2009 Jun 18.

PubMed ID

19596197 [ View in PubMed

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Abstract

Affinity chromatography was used to identify potential cellular targets of aloisine A (7-n-butyl-6-(4'-hydroxyphenyl)-5H-pyrrolo[2,3b]pyrazine), a potent inhibitor of cyclin-dependent kinases. This technique is based on the immobilization of the drug on a solid matrix, followed by identification of specifically bound proteins. To this end, both aloisine A and the protein-kinase inactive control N-methyl aloisine, bearing extended linker chains have been synthesized. We present the preparation of such analogues having the triethylene glycol chain at different positions of the molecule, as well as their immobilization on an agarose-based matrix. Affinity chromatography of various biological extracts on the aloisine matrices allowed the identification of both protein kinases and non-kinase proteins as potential cellular targets of aloisine.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
6-PHENYL[5H]PYRROLO[2,3-B]PYRAZINE	Cyclin-dependent kinase 5	IC 50 (nM)	200	N/A	N/A	Details