Resistance to imatinib (Glivec): update on clinical mechanisms

Efficacy and Safety of Imatinib Mesylate in Advanced Gastrointestinal Stromal Tumors

2002 • 4,254 citations

Effects of a selective inhibitor of the Abl tyrosine kinase on the growth of Bcr–Abl positive cells

1996 • 3,649 citations

PDGFRA Activating Mutations in Gastrointestinal Stromal Tumors

2003 • 2,224 citations

Hematologic and Cytogenetic Responses to Imatinib Mesylate in Chronic Myelogenous Leukemia

2002 • 2,056 citations

Structural Mechanism for STI-571 Inhibition of Abelson Tyrosine Kinase

2000 • 1,770 citations

Abl protein-tyrosine kinase inhibitor STI571 inhibits in vitro signal transduction mediated by c-kit and platelet-derived growth factor receptors.

2000 • 1,264 citations

Imatinib induces hematologic and cytogenetic responses in patients with chronic myelogenous leukemia in myeloid blast crisis: results of a phase II study

2002 • 1,195 citations

Inhibition of the Abl protein-tyrosine kinase in vitro and in vivo by a 2-phenylaminopyrimidine derivative.

1996 • 1,080 citations

Inhibition of c-kit receptor tyrosine kinase activity by STI 571, a selective tyrosine kinase inhibitor

2000 • 1,038 citations

Molecular and chromosomal mechanisms of resistance to imatinib (STI571) therapy

2002 • 923 citations

Selection and characterization of BCR-ABL positive cell lines with differential sensitivity to the tyrosine kinase inhibitor STI571: diverse mechanisms of resistance

2000 • 789 citations

Detection of BCR-ABL mutations in patients with CML treated with imatinib is virtually always accompanied by clinical resistance, and mutations in the ATP phosphate-binding loop (P-loop) are associated with a poor prognosis

2003 • 783 citations

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

2002 • 675 citations

High frequency of point mutations clustered within the adenosine triphosphate–binding region of BCR/ABL in patients with chronic myeloid leukemia or Ph-positive acute lymphoblastic leukemia who develop imatinib (STI571) resistance

2002 • 675 citations

Mechanisms of Autoinhibition and STI-571/Imatinib Resistance Revealed by Mutagenesis of BCR-ABL

2003 • 624 citations

A phase 2 study of imatinib in patients with relapsed or refractory Philadelphia chromosome-positive acute lymphoid leukemias

2002 • 566 citations

Persistence of malignant hematopoietic progenitors in chronic myelogenous leukemia patients in complete cytogenetic remission following imatinib mesylate treatment

2003 • 554 citations

MDR1 gene overexpression confers resistance to imatinib mesylate in leukemia cell line models

2003 • 554 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

CGP 57148, a Tyrosine Kinase Inhibitor, Inhibits the Growth of Cells Expressing BCR-ABL, TEL-ABL, and TEL-PDGFR Fusion Proteins

1997 • 527 citations

Induction of resistance to the Abelson inhibitor STI571 in human leukemic cells through gene amplification

2000 • 511 citations

The c-KIT mutation causing human mastocytosis is resistant to STI571 and other KIT kinase inhibitors; kinases with enzymatic site mutations show different inhibitor sensitivity profiles than wild-type kinases and those with regulatory-type mutations

2002 • 443 citations

CGP 57148, a Tyrosine Kinase Inhibitor, Inhibits the Growth of Cells Expressing BCR-ABL, TEL-ABL, and TEL-PDGFR Fusion Proteins

1997 • 438 citations

Mechanism of resistance to the ABL tyrosine kinase inhibitor STI571 in BCR/ABL–transformed hematopoietic cell lines

2000 • 420 citations

Role of alpha1 Acid Glycoprotein in the In Vivo Resistance of Human BCR-ABL+ Leukemic Cells to the Abl Inhibitor STI571

2000 • 332 citations

Dose escalation of imatinib mesylate can overcome resistance to standard-dose therapy in patients with chronic myelogenous leukemia

2002 • 321 citations

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

2003 • 321 citations

Roots of Clinical Resistance to STI-571 Cancer Therapy

2001 • 291 citations

Efficacy of STI571, an Abl tyrosine kinase inhibitor, in conjunction with other antileukemic agents against Bcr-Abl–positive cells

2000 • 291 citations

BCR-ABL point mutants isolated from patients with imatinib mesylate–resistant chronic myeloid leukemia remain sensitive to inhibitors of the BCR-ABL chaperone heat shock protein 90

2002 • 289 citations

Effects of Blocking Platelet-Derived Growth Factor-Receptor Signaling in a Mouse Model of Experimental Prostate Cancer Bone Metastases

2003 • 275 citations

Clinical resistance to the kinase inhibitor STI-571 in chronic myeloid leukemia by mutation of Tyr-253 in the Abl kinase domain P-loop

2002 • 262 citations

Ph+ acute lymphoblastic leukemia resistant to the tyrosine kinase inhibitor STI571 has a unique BCR-ABL gene mutation

2002 • 259 citations

Juxtamembrane mutant V560GKit is more sensitive to Imatinib (STI571) compared with wild-type c-kit whereas the kinase domain mutant D816VKit is resistant.

2002 • 259 citations

Overcoming STI571 resistance with the farnesyl transferase inhibitor SCH66336

2002 • 255 citations

Monitoring chronic myeloid leukaemia therapy by real-time quantitative PCR in blood is a reliable alternative to bone marrow cytogenetics

1999 • 245 citations

Efficacy of STI571, an Abl tyrosine kinase inhibitor, in conjunction with other antileukemic agents against Bcr-Abl–positive cells

2000 • 244 citations

Alpha1 acid glycoprotein binds to imatinib (STI571) and substantially alters its pharmacokinetics in chronic myeloid leukemia patients.

2003 • 226 citations

Cotreatment with the histone deacetylase inhibitor suberoylanilide hydroxamic acid (SAHA) enhances imatinib-induced apoptosis of Bcr-Abl–positive human acute leukemia cells

2003 • 224 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

The impact of clonal evolution on response to imatinib mesylate (STI571) in accelerated phase CML

2002 • 156 citations

Phosphatidylinositol-3 kinase inhibitors enhance the anti-leukemia effect of STI571

2002 • 154 citations

Inhibition of bcr-abl gene expression by small interfering RNA sensitizes for imatinib mesylate (STI571)

2003 • 144 citations

Dual-specific Src and Abl kinase inhibitors, PP1 and CGP76030, inhibit growth and survival of cells expressing imatinib mesylate–resistant Bcr-Abl kinases

2002 • 129 citations

Presence of the BCR-ABL mutation Glu255Lys prior to STI571 (imatinib) treatment in patients with Ph+ acute lymphoblastic leukemia

2003 • 129 citations

Imatinib mesylate for Philadelphia chromosome-positive, chronic-phase myeloid leukemia after failure of interferon-alpha: follow-up results.

2002 • 126 citations

Effects of the Bcr/abl kinase inhibitors STI571 and adaphostin (NSC 680410) on chronic myelogenous leukemia cells in vitro

2002 • 120 citations

Molecular characterization and sensitivity of STI-571 (imatinib mesylate, Gleevec)-resistant, Bcr-Abl-positive, human acute leukemia cells to SRC kinase inhibitor PD180970 and 17-allylamino-17-demethoxygeldanamycin.

2002 • 112 citations

Restoration of sensitivity to STI571 in STI571-resistant chronic myeloid leukemia cells

2001 • 101 citations

In vitro studies of the combination of imatinib mesylate (Gleevec) and arsenic trioxide (Trisenox) in chronic myelogenous leukemia

2002 • 98 citations

Preexistence and evolution of imatinib mesylate-resistant clones in chronic myelogenous leukemia detected by a PNA-based PCR clamping technique

2003 • 94 citations

Serial monitoring of BCR–ABL by peripheral blood real‐time polymerase chain reaction predicts the marrow cytogenetic response to imatinib mesylate in chronic myeloid leukaemia

2002 • 92 citations

Drug responses of imatinib mesylate-resistant cells: synergism of imatinib with other chemotherapeutic drugs

2002 • 91 citations

α1-Acid glycoprotein expressed in the plasma of chronic myeloid leukemia patients does not mediate significant in vitro resistance to STI571

2002 • 83 citations

Comparison of effects of the tyrosine kinase inhibitors AG957, AG490, and STI571 on BCR-ABL–expressing cells, demonstrating synergy between AG490 and STI571

2001 • 79 citations

Elevated Bcr-Abl expression levels are sufficient for a haematopoietic cell line to acquire a drug-resistant phenotype

2001 • 79 citations

Mutation in the ATP-binding pocket of the ABL kinase domain in an STI571-resistant BCR/ABL-positive cell line.

2002 • 78 citations

BCR/ABL amplification in chronic myelocytic leukemia blast crisis following imatinib mesylate administration

2002 • 76 citations

Determination of α-1 Acid Glycoprotein in Patients with Ph+ Chronic Myeloid Leukemia during the First 13 Weeks of Therapy with STI571

2002 • 64 citations

Kinetics of BCR‐ABL fusion transcript levels in chronic myeloid leukemia patients treated with STI571 measured by quantitative real‐time polymerase chain reaction

2001 • 62 citations

Mechanisms of resistance imatinib (STI571) in preclinical models and in leukemia patients

2001 • 55 citations

Double minutes containing amplified bcr‐abl fusion gene in a case of chronic myeloid leukemia treated by imatinib

2003 • 55 citations

Treatment of inoperable gastrointestinal stromal tumor (GIST) with Imatinib (Glivec, Gleevec).

2002 • 54 citations

Mechanisms of resistance to imatinib (STI571) and prospects for combination with conventional chemotherapeutic agents

2001 • 49 citations

Preexistence and evolution of imatinib mesylate-resistant clones in chronic myelogenous leukemia detected by a PNA-based PCR clamping technique

2003 • 48 citations

Targeted therapies in the treatment of Philadelphia chromosome–positive acute lymphoblastic leukemia

2002 • 47 citations

Mutation in the ATP-binding site of BCR-ABL in a patient with chronic myeloid leukaemia with increasing resistance to STI571

2002 • 42 citations

Analysis of Gene Expression Profiles in an Imatinib‐Resistant Cell Line, KCL22/SR

2003 • 39 citations

Resistenz auf tumorspezifische Therapie mit Imatinib durch klonale Selektion mutierter Zellen

2002 • 28 citations

Spontaneous Reversion from Blast to Chronic Phase after Withdrawal of Imatinib Mesylate in a Patient with Chronic Myelogenous Leukemia

2002 • 10 citations