Mutation in the FGFR1 tyrosine kinase domain or inactivation of PTEN is associated with acquired resistance to FGFR inhibitors in FGFR1-driven leukemia/lymphomas

Development of ZMYM2-FGFR1 driven AML in human CD34+ cells in immunocompromised mice

(2016) Mingqiang Ren et al.   INTERNATIONAL JOURNAL OF CANCER

High-Level Clonal FGFR Amplification and Response to FGFR Inhibition in a Translational Clinical Trial

(2016) A. Pearson et al.   Cancer Discovery

Illuminating the Molecular Mechanisms of Tyrosine Kinase Inhibitor Resistance for the FGFR1 Gatekeeper Mutation: The Achilles’ Heel of Targeted Therapy

(2015) Christal D. Sohl et al.   ACS Chemical Biology

A model of BCR-FGFR1 driven human AML in immunocompromised mice

(2015) John K. Cowell et al.   BRITISH JOURNAL OF HAEMATOLOGY

FGFR1OP2-FGFR1 induced myeloid leukemia and T-cell lymphoma in a mouse model

(2015) H. Qin et al.   HAEMATOLOGICA

Clinical activity of ponatinib in a patient with FGFR1-rearranged mixed-phenotype acute leukemia

(2015) M S Khodadoust et al.   LEUKEMIA

FGFR1OP2-FGFR1 induced myeloid leukemia and T-cell lymphoma in a mouse model

(2015) H. Qin et al.   HAEMATOLOGICA

Dual PI3K/mTOR inhibition shows antileukemic activity in MLL-rearranged acute myeloid leukemia

(2014) N Sandhöfer et al.   LEUKEMIA

Convergent loss of PTEN leads to clinical resistance to a PI(3)Kα inhibitor

(2014) Dejan Juric et al.   NATURE

Development of covalent inhibitors that can overcome resistance to first-generation FGFR kinase inhibitors

(2014) Li Tan et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Dysregulated signaling pathways in the development of CNTRL-FGFR1-induced myeloid and lymphoid malignancies associated with FGFR1 in human and mouse models

(2013) M. Ren et al.   BLOOD

Systems Analysis of the NCI-60 Cancer Cell Lines by Alignment of Protein Pathway Activation Modules with “-OMIC” Data Fields and Therapeutic Response Signatures

(2013) Giulia Federici et al.   MOLECULAR CANCER RESEARCH

AZD4547: An Orally Bioavailable, Potent, and Selective Inhibitor of the Fibroblast Growth Factor Receptor Tyrosine Kinase Family

(2012) P. R. Gavine et al.   CANCER RESEARCH

Ponatinib suppresses the development of myeloid and lymphoid malignancies associated with FGFR1 abnormalities

(2012) M Ren 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

Acute Progression of BCR-FGFR1 Induced Murine B-Lympho/Myeloproliferative Disorder Suggests Involvement of Lineages at the Pro-B Cell Stage

(2012) MingQiang Ren et al.   PLoS One

Fibroblast growth factors and their receptors in cancer

(2011) Jørgen Wesche et al.   BIOCHEMICAL JOURNAL

Constitutive Notch pathway activation in murine ZMYM2-FGFR1-induced T-cell lymphomas associated with atypical myeloproliferative disease

(2011) M. Ren et al.   BLOOD

Src Activation Plays an Important Key Role in Lymphomagenesis Induced by FGFR1 Fusion Kinases

(2011) M. Ren et al.   CANCER RESEARCH

E-3810 Is a Potent Dual Inhibitor of VEGFR and FGFR that Exerts Antitumor Activity in Multiple Preclinical Models

(2011) Ezia Bello et al.   CANCER RESEARCH

The kinase inhibitor TKI258 is active against the novel CUX1-FGFR1 fusion detected in a patient with T-lymphoblastic leukemia/lymphoma and t(7;8)(q22;p11)

(2011) B. Wasag et al.   HAEMATOLOGICA

Discovery of 3-(2,6-Dichloro-3,5-dimethoxy-phenyl)-1-{6-[4-(4-ethyl-piperazin-1-yl)-phenylamino]-pyrimidin-4-yl}-1-methyl-urea (NVP-BGJ398), A Potent and Selective Inhibitor of the Fibroblast Growth Factor Receptor Family of Receptor Tyrosine Kinase

(2011) Vito Guagnano et al.   JOURNAL OF MEDICINAL CHEMISTRY

A Structure-Guided Approach to Creating Covalent FGFR Inhibitors

(2010) Wenjun Zhou et al.   CHEMISTRY & BIOLOGY

FGF signalling: diverse roles during early vertebrate embryogenesis

(2010) K. Dorey et al.   DEVELOPMENT

8p11 myeloproliferative syndrome: a review

(2010) Courtney C. Jackson et al.   HUMAN PATHOLOGY

Frequent and Focal FGFR1 Amplification Associates with Therapeutically Tractable FGFR1 Dependency in Squamous Cell Lung Cancer

(2010) J. Weiss et al.   Science Translational Medicine

Genetic fingerprinting of the development and progression of T-cell lymphoma in a murine model of atypical myeloproliferative disorder initiated by the ZNF198-fibroblast growth factor receptor-1 chimeric tyrosine kinase

(2009) M. Ren et al.   BLOOD

High frequency of PTEN, PI3K, and AKT abnormalities in T-cell acute lymphoblastic leukemia

(2009) A. Gutierrez et al.   BLOOD

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

PTEN Loss Contributes to Erlotinib Resistance in EGFR-Mutant Lung Cancer by Activation of Akt and EGFR

(2009) M. L. Sos et al.   CANCER RESEARCH

Identification and characterization of NVP-BEZ235, a new orally available dual phosphatidylinositol 3-kinase/mammalian target of rapamycin inhibitor with potent in vivo antitumor activity

(2008) S.-M. Maira et al.   MOLECULAR CANCER THERAPEUTICS

Effective use of PI3K and MEK inhibitors to treat mutant Kras G12D and PIK3CA H1047R murine lung cancers

(2008) Jeffrey A Engelman et al.   NATURE MEDICINE