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, cilt.1834, sa.7, ss.1449-1459, 2013 (SCI İndekslerine Giren Dergi) identifier identifier identifier

  • Yayın Türü: Makale / Derleme
  • Cilt numarası: 1834 Konu: 7
  • Basım Tarihi: 2013
  • Doi Numarası: 10.1016/j.bbapap.2012.12.009
  • Dergi Adı: BIOCHIMICA ET BIOPHYSICA ACTA-PROTEINS AND PROTEOMICS
  • Sayfa Sayıları: ss.1449-1459

Özet

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.