title: Optimization of novel combi-molecules: identification of balanced and mixed bcr-abl/DNA targeting properties.
abstract: Steps toward the identification of combi-molecules with strong abl tyrosine kinase (TK) inhibitory property and significant DNA damaging potential are described. The optimized combi-molecule 13a was shown to induce approximately twofold stronger abl TK inhibitory activity than Gleevec and high levels of DNA damage in chronic myelogenous leukemic cells.
authors.affiliation: Cancer Drug Research Laboratory, Division of Medical Oncology, Department of Medicine, McGill University/Royal Victoria Hospital, 687 Pine Avenue West Rm. M-719, Montreal, Que., Canada H3A 1A1.
authors.forename: Zakaria
authors.initials: Z
authors.lastname: Rachid
authors.forename: Athanasia
authors.initials: A
authors.lastname: Katsoulas
authors.forename: Christopher
authors.initials: C
authors.lastname: Williams
authors.forename: Anne-Laure
authors.initials: AL
authors.lastname: Larroque
authors.forename: James
authors.initials: J
authors.lastname: McNamee
authors.forename: Bertrand J
authors.initials: BJ
authors.lastname: Jean-Claude
mesh_terms: D045744:Cell Line, Tumor; D004247:DNA / Q000187:drug effects* / Q000378:metabolism; D004249:DNA Damage; D016044:Fusion Proteins, bcr-abl / Q000378:metabolism*; D006801:Humans; D008958:Models, Molecular
chemical_list: D004247:DNA; D016044:Fusion Proteins, bcr-abl