Mechanisms of resistance to BCR-ABL and other kinase inhibitors


Lamontanara A. J. , Gencer E. B. , Kuzyk O., Hantschel O.

BIOCHIMICA ET BIOPHYSICA ACTA-PROTEINS AND PROTEOMICS, vol.1834, no.7, pp.1449-1459, 2013 (Journal Indexed in SCI) identifier identifier identifier

  • Publication Type: Article / Review
  • Volume: 1834 Issue: 7
  • Publication Date: 2013
  • Doi Number: 10.1016/j.bbapap.2012.12.009
  • Title of Journal : BIOCHIMICA ET BIOPHYSICA ACTA-PROTEINS AND PROTEOMICS
  • Page Numbers: pp.1449-1459

Abstract

In this article, we are reviewing the molecular mechanisms that lead to kinase inhibitor resistance. As the oncogenic BCR-ABL kinase is the target of the first approved small-molecule kinase inhibitor imatinib, we will first focus on the structural and mechanistic basis for imatinib resistance. We will then show ways how next generations of BCR-ABL inhibitors and alternative targeting strategies have helped to offer effective treatment options for imatinib-resistant patients. Based on these insights, we discuss commonalities and further mechanisms that lead to resistance to other kinase inhibitors in solid tumors. This article is part of a Special Issue entitled: Inhibitors of Protein Kinases (2012). (C) 2012 Elsevier B.V. All rights reserved.