Ponatinib efficiently kills imatinib-resistant chronic eosinophilic leukemia cells harboring gatekeeper mutant T674I FIP1L1-PDGFRα: roles of Mcl-1 and β-catenin

Long-term follow-up of treatment with imatinib in eosinophilia-associated myeloid/lymphoid neoplasms with PDGFR rearrangements in blast phase

(2013) G Metzgeroth et al.   LEUKEMIA

Ponatinib is active against imatinib-resistant mutants of FIP1L1-PDGFRA and KIT and against FGFR1-derived fusion kinases

(2012) E Lierman et al.   LEUKEMIA

Ponatinib in Refractory Philadelphia Chromosome–Positive Leukemias

(2012) Jorge E. Cortes et al.   NEW ENGLAND JOURNAL OF MEDICINE

Conformational Control Inhibition of the BCR-ABL1 Tyrosine Kinase, Including the Gatekeeper T315I Mutant, by the Switch-Control Inhibitor DCC-2036

(2011) Wayne W. Chan et al.   CANCER CELL

The ABL Switch Control Inhibitor DCC-2036 Is Active against the Chronic Myeloid Leukemia Mutant BCR-ABLT315I and Exhibits a Narrow Resistance Profile

(2011) C. A. Eide et al.   CANCER RESEARCH

Sorafenib induces cell death in chronic lymphocytic leukemia by translational downregulation of Mcl-1

(2011) S Huber et al.   LEUKEMIA

Limited clinical activity of nilotinib and sorafenib in FIP1L1-PDGFRA positive chronic eosinophilic leukemia with imatinib-resistant T674I mutation

(2011) G Metzgeroth et al.   LEUKEMIA

Potent Activity of Ponatinib (AP24534) in Models of FLT3-Driven Acute Myeloid Leukemia and Other Hematologic Malignancies

(2011) J. M. Gozgit et al.   MOLECULAR CANCER THERAPEUTICS

Discovery of a small-molecule type II inhibitor of wild-type and gatekeeper mutants of BCR-ABL, PDGFR , Kit, and Src kinases: novel type II inhibitor of gatekeeper mutants

(2010) E. Weisberg et al.   BLOOD

GDP366, a novel small molecule dual inhibitor of survivin and Op18, induces cell growth inhibition, cellular senescence and mitotic catastrophe in human cancer cells

(2010) Xianping Shi et al.   CANCER BIOLOGY & THERAPY

Antineoplastic Mechanisms of Niclosamide in Acute Myelogenous Leukemia Stem Cells: Inactivation of the NF- B Pathway and Generation of Reactive Oxygen Species

(2010) Y. Jin et al.   CANCER RESEARCH

Structural Mechanism of the Pan-BCR-ABL Inhibitor Ponatinib (AP24534): Lessons for Overcoming Kinase Inhibitor Resistance

(2010) Tianjun Zhou et al.   Chemical Biology & Drug Design

Clinical implications of KIT and PDGFRA genotyping in GIST

(2010) Javier Martín-Broto et al.   Clinical & Translational Oncology

Discovery of 3-[2-(Imidazo[1,2-b]pyridazin-3-yl)ethynyl]-4-methyl-N-{4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl}benzamide (AP24534), a Potent, Orally Active Pan-Inhibitor of Breakpoint Cluster Region-Abelson (BCR-ABL) Kinase Including the T315I Gatekeeper Mutant

(2010) Wei-Sheng Huang et al.   JOURNAL OF MEDICINAL CHEMISTRY

Pristimerin induces apoptosis in imatinib-resistant chronic myelogenous leukemia cells harboring T315I mutation by blocking NF-κB signaling and depleting Bcr-Abl

(2010) Zhongzheng Lu et al.   Molecular Cancer

AP24534, a Pan-BCR-ABL Inhibitor for Chronic Myeloid Leukemia, Potently Inhibits the T315I Mutant and Overcomes Mutation-Based Resistance

(2009) Thomas O'Hare et al.   CANCER CELL

The  -Catenin Axis Integrates Multiple Signals Downstream from RET/Papillary Thyroid Carcinoma Leading to Cell Proliferation

(2009) M. D. Castellone et al.   CANCER RESEARCH

Triptolide abrogates oncogene FIP1L1-PDGFRα addiction and induces apoptosis in hypereosinophilic syndrome

(2009) Yanli Jin et al.   CANCER SCIENCE

Triptolide Inhibits Bcr-Abl Transcription and Induces Apoptosis in STI571-resistant Chronic Myelogenous Leukemia Cells Harboring T315I Mutation

(2009) X. Shi et al.   CLINICAL CANCER RESEARCH

FIP1L1-PDGFRα D842V, a novel panresistant mutant, emerging after treatment of FIP1L1-PDGFRα T674I eosinophilic leukemia with single agent sorafenib

(2009) E Lierman et al.   LEUKEMIA

Transient Potent BCR-ABL Inhibition Is Sufficient to Commit Chronic Myeloid Leukemia Cells Irreversibly to Apoptosis

(2008) Neil P. Shah et al.   CANCER CELL

KIT regulates tyrosine phosphorylation and nuclear localization of β-catenin in mast cell leukemia

(2008) Tomohiro Kajiguchi et al.   LEUKEMIA RESEARCH

Activation of tyrosine kinases by mutation of the gatekeeper threonine

(2008) Mohammad Azam et al.   NATURE STRUCTURAL & MOLECULAR BIOLOGY