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Updated: Aug 20, 2026

A Method for Screening and Validation of Resistant Mutations Against Kinase Inhibitors
Published on: December 7, 2014
[Origin of resistance to Imatinib mesylate: lessons learned from this experience]
Catherine Roche-Lestienne1, François-Xavier Mahon, Claude Preudhomme
1Institut de recherche contre le Cancer, Inserm U.524 et CHRU de Lille, 1, place de Verdun, 59045 Lille, France. croche@lille.inserm.fr
Abstract:
For drug development and pharmaceutical research, targeting the molecular abnormalities is considered as a new challenge. A number of diseases including cancer are linked to perturbation of tyrosine kinase (TK). Imatinib (Glivec or Gleevec, Novartis), the most potent inhibitor of c-abl TK, was recently developed. This molecule has been approved in the treatment of chronic myeloid leukemia (CML). However, emergence of clinical resistance regarding a low rate of CML patients leads to intensive research. In the current article, we discuss the data and the mechanism of the resistance phenomenon. This review illustrates the important requirement to transfer back the information from patient to laboratory in order to improve future drug design.
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