Mechanisms of resistance to BCR–ABL kinase inhibitors

The poor response to imatinib observed in CML patients with low OCT-1 activity is not attributable to lower uptake of imatinib into their CD34+ cells

(2010) J. R. Engler et al.   BLOOD

Bone marrow mesenchymal stromal cells non-selectively protect chronic myeloid leukemia cells from imatinib-induced apoptosis via the CXCR4/CXCL12 axis

(2010) F. Vianello et al.   HAEMATOLOGICA

Functional Activity of the OCT-1 Protein Is Predictive of Long-Term Outcome in Patients With Chronic-Phase Chronic Myeloid Leukemia Treated With Imatinib

(2010) Deborah L. White et al.   JOURNAL OF CLINICAL ONCOLOGY

Adherence Is the Critical Factor for Achieving Molecular Responses in Patients With Chronic Myeloid Leukemia Who Achieve Complete Cytogenetic Responses on Imatinib

(2010) David Marin et al.   JOURNAL OF CLINICAL ONCOLOGY

Blocking cytokine signaling along with intense Bcr-Abl kinase inhibition induces apoptosis in primary CML progenitors

(2010) D K Hiwase et al.   LEUKEMIA

Nilotinib does not significantly reduce imatinib OCT-1 activity in either cell lines or primary CML cells

(2010) L Eadie et al.   LEUKEMIA

Chronic Myeloid Leukemia CD34+ cells have reduced uptake of imatinib due to low OCT-1 Activity

(2010) J R Engler et al.   LEUKEMIA

hOCT1 transcript levels and single nucleotide polymorphisms as predictive factors for response to imatinib in chronic myeloid leukemia

(2010) A Bazeos et al.   LEUKEMIA

Activation of the p38 Map kinase pathway is essential for the antileukemic effects of dasatinib

(2010) Disha Dumka et al.   LEUKEMIA & LYMPHOMA

Dasatinib treatment of chronic-phase chronic myeloid leukemia: analysis of responses according to preexisting BCR-ABL mutations

(2009) M. C. Muller et al.   BLOOD

Philadelphia-positive patients who already harbor imatinib-resistant Bcr-Abl kinase domain mutations have a higher likelihood of developing additional mutations associated with resistance to second- or third-line tyrosine kinase inhibitors

(2009) S. Soverini et al.   BLOOD

Selecting optimal second-line tyrosine kinase inhibitor therapy for chronic myeloid leukemia patients after imatinib failure: does the BCR-ABL mutation status really matter?

(2009) S. Branford et al.   BLOOD

A gene expression signature of CD34+ cells to predict major cytogenetic response in chronic-phase chronic myeloid leukemia patients treated with imatinib

(2009) S. K. McWeeney et al.   BLOOD

Brain Accumulation of Dasatinib Is Restricted by P-Glycoprotein (ABCB1) and Breast Cancer Resistance Protein (ABCG2) and Can Be Enhanced by Elacridar Treatment

(2009) J. S. Lagas et al.   CLINICAL CANCER RESEARCH

Inhibition of MDR1 does not sensitize primitive chronic myeloid leukemia CD34+ cells to imatinib

(2009) Sophia Hatziieremia et al.   EXPERIMENTAL HEMATOLOGY

BCR-ABLGene Expression Is Required for Its Mutations in a Novel KCL-22 Cell Culture Model for Acquired Resistance of Chronic Myelogenous Leukemia

(2009) Hongfeng Yuan et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Chronic Myeloid Leukemia: An Update of Concepts and Management Recommendations of European LeukemiaNet

(2009) Michele Baccarani et al.   JOURNAL OF CLINICAL ONCOLOGY

Impact of BaselineBCR-ABLMutations on Response to Nilotinib in Patients With Chronic Myeloid Leukemia in Chronic Phase

(2009) Timothy Hughes et al.   JOURNAL OF CLINICAL ONCOLOGY

A pilot study of continuous imatinib vs pulsed imatinib with or without G-CSF in CML patients who have achieved a complete cytogenetic response

(2009) M W Drummond et al.   LEUKEMIA

Nilotinib-mediated inhibition of ABCB1 increases intracellular concentration of dasatinib in CML cells: implications for combination TKI therapy

(2009) D K Hiwase et al.   LEUKEMIA

Nilotinib concentration in cell lines and primary CD34+ chronic myeloid leukemia cells is not mediated by active uptake or efflux by major drug transporters

(2009) A Davies et al.   LEUKEMIA

Plerixafor inhibits chemotaxis toward SDF-1 and CXCR4-mediated stroma contact in a dose-dependent manner resulting in increased susceptibility of BCR-ABL+cell to Imatinib and Nilotinib

(2009) Falk Dillmann et al.   LEUKEMIA & LYMPHOMA

A gene expression signature of primary resistance to imatinib in chronic myeloid leukemia

(2009) Hugues de Lavallade et al.   LEUKEMIA RESEARCH

Gene expression profiling of imatinib and PD166326-resistant CML cell lines identifies Fyn as a gene associated with resistance to BCR-ABL inhibitors

(2009) S. Grosso et al.   MOLECULAR CANCER THERAPEUTICS

Understanding the Role of Mutations in Therapeutic Decision Making for Chronic Myeloid Leukemia

(2009) Elias Jabbour et al.   SEMINARS IN HEMATOLOGY

Monitoring disease response to tyrosine kinase inhibitor therapy in CML

(2009) T. P. Hughes et al.   Hematology-American Society of Hematology Education Program

Characteristics and outcome of chronic myeloid leukemia patients with F317L BCR-ABL kinase domain mutation after therapy with tyrosine kinase inhibitors

(2008) E. Jabbour et al.   BLOOD

Effective dasatinib uptake may occur without human organic cation transporter 1 (hOCT1): implications for the treatment of imatinib-resistant chronic myeloid leukemia

(2008) A. Giannoudis et al.   BLOOD

Characteristics and outcomes of patients with chronic myeloid leukemia and T315I mutation following failure of imatinib mesylate therapy

(2008) E. Jabbour et al.   BLOOD

BCR/ABL and Other Kinases from Chronic Myeloproliferative Disorders Stimulate Single-Strand Annealing, an Unfaithful DNA Double-Strand Break Repair

(2008) K. Cramer et al.   CANCER RESEARCH

Evidence that Resistance to Nilotinib May Be Due to BCR-ABL, Pgp, or Src Kinase Overexpression

(2008) F.-X. Mahon et al.   CANCER RESEARCH

Interaction of Imatinib with Human Organic Ion Carriers

(2008) S. Hu et al.   CLINICAL CANCER RESEARCH

Dasatinib Cellular Uptake and Efflux in Chronic Myeloid Leukemia Cells: Therapeutic Implications

(2008) D. K. Hiwase et al.   CLINICAL CANCER RESEARCH

Overcoming imatinib resistance using Src inhibitor CGP76030, Abl inhibitor nilotinib and Abl/Lyn inhibitor INNO-406 in newly established K562 variants withBCR-ABLgene amplification

(2008) Koji Morinaga et al.   INTERNATIONAL JOURNAL OF CANCER

Activity of Bosutinib, Dasatinib, and Nilotinib Against 18 Imatinib-Resistant BCR/ABL Mutants

(2008) Sara Redaelli et al.   JOURNAL OF CLINICAL ONCOLOGY

Association Between Imatinib-Resistant BCR-ABL Mutation-Negative Leukemia and Persistent Activation of LYN Kinase

(2008) Ji Wu et al.   JNCI-Journal of the National Cancer Institute

Enhanced BCR-ABL kinase inhibition does not result in increased inhibition of downstream signaling pathways or increased growth suppression in CML progenitors

(2008) H Konig et al.   LEUKEMIA

BCR/ABL promotes accumulation of chromosomal aberrations induced by oxidative and genotoxic stress

(2008) M Koptyra et al.   LEUKEMIA

Imatinib resistance in multidrug-resistant K562 human leukemic cells

(2008) Yanina Assef et al.   LEUKEMIA RESEARCH

CXCR4 up-regulation by imatinib induces chronic myelogenous leukemia (CML) cell migration to bone marrow stroma and promotes survival of quiescent CML cells

(2008) L. Jin et al.   MOLECULAR CANCER THERAPEUTICS