Discovery of a miniaturized PROTAC with potent activity and high selectivity

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)

J. Jean Cui, Michelle Tran‐Dubé, Hong Shen et al. · Journal of Medicinal Chemistry · 2011 · 922 citations · Full text

Pharmacy, Medicinal Chemistry, Pharmacology +17

Oncogenic mutations of ALK kinase in neuroblastoma

Yuyan Chen, Junko Takita, Young Lim Choi et al. · Nature · 2008 · 914 citations

Medicine, Molecular Genetics, Oncology +14

PROTAC-induced BET protein degradation as a therapy for castration-resistant prostate cancer

Kanak Raina, Jing Lü, Yimin Qian et al. · Proceedings of the National Academy of Sciences · 2016 · 827 citations · Full text

Medicine, Molecular Biology, Oncology +17

Discovery of (10 <i>R</i> )-7-Amino-12-fluoro-2,10,16-trimethyl-15-oxo-10,15,16,17-tetrahydro- <i>2H</i> -8,4-(metheno)pyrazolo[4,3- <i>h</i> ][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

Ted W. Johnson, Paul Richardson, Simon Bailey et al. · Journal of Medicinal Chemistry · 2014 · 585 citations · Full text

Medicine, Medicinal Chemistry, Pharmacology +16

Landscape of Acquired Resistance to Osimertinib in <i>EGFR</i> -Mutant NSCLC and Clinical Validation of Combined EGFR and RET Inhibition with Osimertinib and BLU-667 for Acquired <i>RET</i> Fusion

Zofia Piotrowska, Hideko Isozaki, Jochen K. Lennerz et al. · Cancer Discovery · 2018 · 445 citations

Medicine, Oncology, Pharmacology +17