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In vitro Activity of Bcr-Abl Inhibitors AMN107 and BMS-354825 against Clinically Relevant Imatinib-Resistant Abl Kinase Domain Mutants

Data up to Jan 2025

Published2005
Citations1,039
References22
Clinical Trials (1)

Total Citations Per Year

Abstract

References (22)

Efficacy and Safety of a Specific Inhibitor of the BCR-ABL Tyrosine Kinase in Chronic Myeloid Leukemia

2001 • 5,189 citations

Imatinib Compared with Interferon and Low-Dose Cytarabine for Newly Diagnosed Chronic-Phase Chronic Myeloid Leukemia

2003 • 3,532 citations

Activity of a Specific Inhibitor of the BCR-ABL Tyrosine Kinase in the Blast Crisis of Chronic Myeloid Leukemia and Acute Lymphoblastic Leukemia with the Philadelphia Chromosome

2001 • 2,749 citations

Overriding Imatinib Resistance with a Novel ABL Kinase Inhibitor

2004 • 1,785 citations

Structural Mechanism for STI-571 Inhibition of Abelson Tyrosine Kinase

2000 • 1,770 citations

Characterization of AMN107, a selective inhibitor of native and mutant Bcr-Abl

2005 • 1,435 citations

The development of imatinib as a therapeutic agent for chronic myeloid leukemia

2004 • 1,231 citations

Imatinib induces durable hematologic and cytogenetic responses in patients with accelerated phase chronic myeloid leukemia: results of a phase 2 study

2002 • 1,069 citations

Crystal structures of the kinase domain of c-Abl in complex with the small molecule inhibitors PD173955 and imatinib (STI-571).

2002 • 925 citations

BCR-ABL independence and LYN kinase overexpression in chronic myelogenous leukemia cells selected for resistance to STI571

2002 • 675 citations

Several types of mutations of the Abl gene can be found in chronic myeloid leukemia patients resistant to STI571, and they can pre-exist to the onset of treatment

2002 • 534 citations

Pharmacokinetics and Pharmacodynamics of Imatinib in a Phase I Trial With Chronic Myeloid Leukemia Patients

2004 • 467 citations

Imatinib as a Paradigm of Targeted Therapies

2004 • 366 citations

Several Bcr-Abl kinase domain mutants associated with imatinib mesylate resistance remain sensitive to imatinib

2003 • 321 citations

c-Abl Has High Intrinsic Tyrosine Kinase Activity That Is Stimulated by Mutation of the Src Homology 3 Domain and by Autophosphorylation at Two Distinct Regulatory Tyrosines

2000 • 270 citations

Short interfering RNA (siRNA) targeting the Lyn kinase induces apoptosis in primary, and drug-resistant, BCR-ABL1(+) leukemia cells

2004 • 233 citations

Activity of the Bcr-Abl kinase inhibitor PD180970 against clinically relevant Bcr-Abl isoforms that cause resistance to imatinib mesylate (Gleevec, STI571).

2002 • 211 citations

Inhibition of wild-type and mutant Bcr-Abl by AP23464, a potent ATP-based oncogenic protein kinase inhibitor: implications for CML

2004 • 196 citations

Analysis of the Structural Basis of Specificity of Inhibition of the Abl Kinase by STI571

2002 • 171 citations

Imatinib (STI571) Resistance in Chronic Myelogenous Leukemia: Molecular Basis of the Underlying Mechanisms and Potential Strategies for Treatment

2004 • 167 citations

A cell-based screen for resistance of Bcr-Abl-positive leukemia identifies the mutation pattern for PD166326, an alternative Abl kinase inhibitor

2005 • 93 citations

A Phase I/II Study of AMN107, a Novel Aminopyrimidine Inhibitor of Bcr-Abl, on a Continuous Daily Dosing Schedule in Adult Patients (pts) with Imatinib-Resistant Advanced Phase Chronic Myeloid Leukemia (CML) or Relapsed/Refractory Philadelphia Chromosome (Ph+) Acute Llymphocytic Leukemia (ALL).

2004 • 33 citations

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In vitro Activity of Bcr-Abl Inhibitors AMN107 and BMS-354825 against Clinically Relevant… (2005) – Cancer Research | Metascience Observatory Explorer