PF-06463922 is a potent and selective next-generation ROS1/ALK inhibitor capable of blocking crizotinib-resistant ROS1 mutations

Molecular Changes Associated with Acquired Resistance to Crizotinib in ROS1-Rearranged Non-Small Cell Lung Cancer

(2015) A. Song et al.   CLINICAL CANCER RESEARCH

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

(2014) Tatsushi Kodama et al.   CANCER LETTERS

Cabozantinib Overcomes Crizotinib Resistance in ROS1 Fusion-Positive Cancer

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

Design of Potent and Selective Inhibitors to Overcome Clinical Anaplastic Lymphoma Kinase Mutations Resistant to Crizotinib

(2014) Qinhua Huang et al.   JOURNAL OF MEDICINAL CHEMISTRY

Discovery of (10R)-7-Amino-12-fluoro-2,10,16-trimethyl-15-oxo-10,15,16,17-tetrahydro-2H-8,4-(metheno)pyrazolo[4,3-h][2,5,11]-benzoxadiazacyclotetradecine-3-carbonitrile (PF-06463922), a Macrocyclic Inhibitor of Anaplastic Lymphoma Kinase (ALK) and c-ros Oncogene 1 (ROS1) with Preclinical Brain Exposure and Broad-Spectrum Potency against ALK-Resistant Mutations

(2014) Ted W. Johnson et al.   JOURNAL OF MEDICINAL CHEMISTRY

Next-Generation Sequencing Reveals a Novel NSCLC ALK F1174V Mutation and Confirms ALK G1202R Mutation Confers High-Level Resistance to Alectinib (CH5424802/RO5424802) in ALK-Rearranged NSCLC Patients Who Progressed on Crizotinib

(2014) Sai-Hong Ignatius Ou et al.   Journal of Thoracic Oncology

The landscape of kinase fusions in cancer

(2014) Nicolas Stransky et al.   Nature Communications

Kinase fusions are frequent in Spitz tumours and spitzoid melanomas

(2014) Thomas Wiesner et al.   Nature Communications

The ALK Inhibitor Ceritinib Overcomes Crizotinib Resistance in Non-Small Cell Lung Cancer

(2014) L. Friboulet et al.   Cancer Discovery

ROS1 Immunohistochemistry for Detection of ROS1-Rearranged Lung Adenocarcinomas

(2013) Lynette M. Sholl et al.   AMERICAN JOURNAL OF SURGICAL PATHOLOGY

Insight into Crizotinib Resistance Mechanisms Caused by Three Mutations in ALK Tyrosine Kinase using Free Energy Calculation Approaches

(2013) Huiyong Sun et al.   Journal of Chemical Information and Modeling

Emerging Paradigms in the Development of Resistance to Tyrosine Kinase Inhibitors in Lung Cancer

(2013) Justin F. Gainor et al.   JOURNAL OF CLINICAL ONCOLOGY

ALKin Lung Cancer: Past, Present, and Future

(2013) Alice T. Shaw et al.   JOURNAL OF CLINICAL ONCOLOGY

Chaperones as thermodynamic sensors of drug-target interactions reveal kinase inhibitor specificities in living cells

(2013) Mikko Taipale et al.   NATURE BIOTECHNOLOGY

Acquired Resistance to Crizotinib from a Mutation in CD74–ROS1

(2013) Mark M. Awad et al.   NEW ENGLAND JOURNAL OF MEDICINE

Foretinib is a potent inhibitor of oncogenic ROS1 fusion proteins

(2013) M. A. Davare et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Breakpoint Analysis of Transcriptional and Genomic Profiles Uncovers Novel Gene Fusions Spanning Multiple Human Cancer Types

(2013) Craig P. Giacomini et al.   PLoS Genetics

Abstract 3764: SC-1, a sorafenib derivative, induces apoptosis in epidermal growth factor receptor wild type non-small cell lung cancer through the inhibition of signal transducers and activators of transcription 3

(2012) Cheng-Yi Wang et al.   CANCER RESEARCH

Analysis of Receptor Tyrosine Kinase ROS1-Positive Tumors in Non-Small Cell Lung Cancer: Identification of a FIG-ROS1 Fusion

(2012) V. M. Rimkunas 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

ROS1 as a ‘druggable’ receptor tyrosine kinase: lessons learned from inhibiting the ALK pathway

(2012) Sai-Hong Ignatius Ou et al.   Expert Review of Anticancer Therapy

The transcriptional landscape and mutational profile of lung adenocarcinoma

(2012) J.-S. Seo et al.   GENOME RESEARCH

ROS1 Rearrangements Define a Unique Molecular Class of Lung Cancers

(2012) Kristin Bergethon et al.   JOURNAL OF CLINICAL ONCOLOGY

RET, ROS1 and ALK fusions in lung cancer

(2012) Kengo Takeuchi et al.   NATURE MEDICINE

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

Survey of Tyrosine Kinase Signaling Reveals ROS Kinase Fusions in Human Cholangiocarcinoma

(2011) Ting-Lei Gu et al.   PLoS One

Chromosome 3 Anomalies Investigated by Genome Wide SNP Analysis of Benign, Low Malignant Potential and Low Grade Ovarian Serous Tumours

(2011) Ashley H. Birch et al.   PLoS One

A Cre/LoxP conditional luciferase reporter transgenic mouse for bioluminescence monitoring of tumorigenesis

(2009) Steve Woolfenden et al.   GENESIS

Acquired resistance to tyrosine kinase inhibitors during cancer therapy

(2008) Jeffrey A Engelman et al.   CURRENT OPINION IN GENETICS & DEVELOPMENT