The use of cellular thermal shift assay (CETSA) to study Crizotinib resistance in ALK-expressing human cancers

A Small-Molecule Protein-Protein Interaction Inhibitor of PARP1 That Targets Its BRCT Domain

(2015) Zhenkun Na et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

CETSA: a target engagement assay with potential to transform drug discovery

(2015) Annika Jenmalm Jensen et al.   Future Medicinal Chemistry

Inhibition of β-Catenin Enhances the Anticancer Effect of Irreversible EGFR-TKI in EGFR-Mutated Non–small-cell Lung Cancer with a T790M Mutation

(2015) Yosuke Togashi et al.   Journal of Thoracic Oncology

A selective inhibitor of PRMT5 with in vivo and in vitro potency in MCL models

(2015) Elayne Chan-Penebre et al.   Nature Chemical Biology

Understanding the Interplay between Expression, Mutation and Activity of ALK Receptor in Rhabdomyosarcoma Cells for Clinical Application of Small-Molecule Inhibitors

(2015) Marica Peron et al.   PLoS One

Assessing the Efficacy of Mdm2/Mdm4-Inhibiting Stapled Peptides Using Cellular Thermal Shift Assays

(2015) Ban Xiong Tan et al.   Scientific Reports

Discovery and characterization of novel small-molecule inhibitors targeting nicotinamide phosphoribosyltransferase

(2015) Tian-Ying Xu et al.   Scientific Reports

Molecular rationale for the use of PI3K/AKT/mTOR pathway inhibitors in combination with crizotinib in ALK-mutated neuroblastoma

(2015) Nathan F. Moore et al.   Oncotarget

ALK Mutations Confer Differential Oncogenic Activation and Sensitivity to ALK Inhibition Therapy in Neuroblastoma

(2014) Scott C. Bresler et al.   CANCER CELL

Selective ALK inhibitor alectinib with potent antitumor activity in models of crizotinib resistance

(2014) Tatsushi Kodama et al.   CANCER LETTERS

Two Novel ALK Mutations Mediate Acquired Resistance to the Next-Generation ALK Inhibitor Alectinib

(2014) R. Katayama et al.   CLINICAL CANCER RESEARCH

Activating mutations in ALK kinase domain confer resistance to structurally unrelated ALK inhibitors in NPM-ALK-positive anaplastic large-cell lymphoma

(2014) Daria Zdzalik et al.   JOURNAL OF CANCER RESEARCH AND CLINICAL ONCOLOGY

Overcoming the resistance to Crizotinib in patients with Non-Small Cell Lung Cancer harboring EML4/ALK translocation

(2014) Cesar A. Perez et al.   LUNG CANCER

Stereospecific targeting of MTH1 by (S)-crizotinib as an anticancer strategy

(2014) Kilian V. M. Huber et al.   NATURE

The cellular thermal shift assay for evaluating drug target interactions in cells

(2014) Rozbeh Jafari et al.   Nature Protocols

BM-1197: A Novel and Specific Bcl-2/Bcl-xL Inhibitor Inducing Complete and Long-Lasting Tumor Regression In Vivo

(2014) Longchuan Bai et al.   PLoS One

Control of ALK (wild type and mutated forms) phosphorylation: Specific role of the phosphatase PTP1B

(2013) M.C. Boutterin et al.   CELLULAR SIGNALLING

Safety and activity of crizotinib for paediatric patients with refractory solid tumours or anaplastic large-cell lymphoma: a Children's Oncology Group phase 1 consortium study

(2013) Yael P Mossé et al.   LANCET ONCOLOGY

Discovery and Preclinical Characterization of Novel Small Molecule TRK and ROS1 Tyrosine Kinase Inhibitors for the Treatment of Cancer and Inflammation

(2013) Ramesh Narayanan et al.   PLoS One

Monitoring Drug Target Engagement in Cells and Tissues Using the Cellular Thermal Shift Assay

(2013) D. M. Molina et al.   SCIENCE

Targeted Inhibition of the Molecular Chaperone Hsp90 Overcomes ALK Inhibitor Resistance in Non–Small Cell Lung Cancer

(2013) Jim Sang et al.   Cancer Discovery

Presence of anaplastic lymphoma kinase in inflammatory breast cancer

(2013) Fredika M Robertson et al.   SpringerPlus

Genetic and Pharmacologic Inhibition of β-Catenin Targets Imatinib-Resistant Leukemia Stem Cells in CML

(2012) Florian H. Heidel et al.   Cell Stem Cell

Disheveled proteins promote cell growth and tumorigenicity in ALK-positive anaplastic large cell lymphoma

(2012) Samar A. Hegazy et al.   CELLULAR SIGNALLING

Mechanisms of Resistance to Crizotinib in Patients withALKGene Rearranged Non–Small Cell Lung Cancer

(2012) Robert C. Doebele et al.   CLINICAL CANCER RESEARCH

Differential Protein Stability and ALK Inhibitor Sensitivity of EML4-ALK Fusion Variants

(2012) J. M. Heuckmann et al.   CLINICAL CANCER RESEARCH

The battle against ALK resistance: successes and setbacks

(2012) Claudia Voena et al.   EXPERT OPINION ON INVESTIGATIONAL DRUGS

Crizotinib-Resistant NPM-ALK Mutants Confer Differential Sensitivity to Unrelated Alk Inhibitors

(2012) M. Ceccon et al.   MOLECULAR CANCER RESEARCH

The Cancer Cell Line Encyclopedia enables predictive modelling of anticancer drug sensitivity

(2012) Jordi Barretina et al.   NATURE

Mechanisms of Acquired Crizotinib Resistance in ALK-Rearranged Lung Cancers

(2012) R. Katayama et al.   Science Translational Medicine

CH5424802, a Selective ALK Inhibitor Capable of Blocking the Resistant Gatekeeper Mutant

(2011) Hiroshi Sakamoto et al.   CANCER CELL

Structure Based Drug Design of Crizotinib (PF-02341066), a Potent and Selective Dual Inhibitor of Mesenchymal–Epithelial Transition Factor (c-MET) Kinase and Anaplastic Lymphoma Kinase (ALK)

(2011) J. Jean Cui et al.   JOURNAL OF MEDICINAL CHEMISTRY

Anaplastic lymphoma kinase in human cancer

(2011) Antonella Barreca et al.   JOURNAL OF MOLECULAR ENDOCRINOLOGY

Targeting Oncogenic ALK: A Promising Strategy for Cancer Treatment

(2011) E. Grande et al.   MOLECULAR CANCER THERAPEUTICS

Crizotinib in Anaplastic Large-Cell Lymphoma

(2011) Carlo Gambacorti-Passerini et al.   NEW ENGLAND JOURNAL OF MEDICINE

Therapeutic strategies to overcome crizotinib resistance in non-small cell lung cancers harboring the fusion oncogene EML4-ALK

(2011) R. Katayama et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Differential Inhibitor Sensitivity of Anaplastic Lymphoma Kinase Variants Found in Neuroblastoma

(2011) S. C. Bresler et al.   Science Translational Medicine

Appearance of the Novel Activating F1174S ALK Mutation in Neuroblastoma Correlates with Aggressive Tumor Progression and Unresponsiveness to Therapy

(2010) T. Martinsson et al.   CANCER RESEARCH

 -catenin is constitutively active and increases STAT3 expression/activation in anaplastic lymphoma kinase-positive anaplastic large cell lymphoma

(2010) M. Anand et al.   HAEMATOLOGICA

EML4-ALK Mutations in Lung Cancer That Confer Resistance to ALK Inhibitors

(2010) Young Lim Choi et al.   NEW ENGLAND JOURNAL OF MEDICINE

EML4-ALK Rearrangement in Non-Small Cell Lung Cancer and Non-Tumor Lung Tissues

(2009) Maria Paola Martelli et al.   AMERICAN JOURNAL OF PATHOLOGY

Proteome-Wide Identification of Novel Binding Partners to the Oncogenic Fusion Gene Protein, NPM-ALK, using Tandem Affinity Purification and Mass Spectrometry

(2009) Fang Wu et al.   AMERICAN JOURNAL OF PATHOLOGY

High incidence of DNA mutations and gene amplifications of theALKgene in advanced sporadic neuroblastoma tumours

(2008) Helena Carén et al.   BIOCHEMICAL JOURNAL

Identification of ALK as a major familial neuroblastoma predisposition gene

(2008) Yaël P. Mossé et al.   NATURE

Activating mutations in ALK provide a therapeutic target in neuroblastoma

(2008) Rani E. George et al.   NATURE

Oncogenic mutations of ALK kinase in neuroblastoma

(2008) Yuyan Chen et al.   NATURE

Somatic and germline activating mutations of the ALK kinase receptor in neuroblastoma

(2008) Isabelle Janoueix-Lerosey et al.   NATURE