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Article Dans Une Revue Bioorganic and Medicinal Chemistry Année : 2009

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

Rose Haddoub
  • Fonction : Auteur
Damien Guiffant
  • Fonction : Auteur
Olivier Lozach
David Gueyrard
  • Fonction : Auteur
Morgane Ratin
Stéphane Bach
Peter Goekjian
  • Fonction : Auteur

Résumé

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.

Dates et versions

hal-00416033 , version 1 (11-09-2009)

Identifiants

Citer

Caroline Corbel, Rose Haddoub, Damien Guiffant, Olivier Lozach, David Gueyrard, et al.. Identification of potential cellular targets of aloisine A by affinity chromatography.. Bioorganic and Medicinal Chemistry, 2009, 17 (15), pp.5572-82. ⟨10.1016/j.bmc.2009.06.024⟩. ⟨hal-00416033⟩
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