Discovery of 4-methyl-N-(4-((4-methylpiperazin- 1-yl)methyl)-3-(trifluoromethyl)phenyl)-3-((6-(pyridin-3-yl)-1H-pyrazolo[3,4-d]pyrimidin-4-yl)-oxy)benzamide as a potent inhibitor of RET and its gatekeeper mutant

Selective RET kinase inhibition for patients with RET-altered cancers

(2018) V Subbiah et al.   ANNALS OF ONCOLOGY

Osimertinib in Untreated EGFR-Mutated Advanced Non–Small-Cell Lung Cancer

(2018) Jean-Charles Soria et al.   NEW ENGLAND JOURNAL OF MEDICINE

Precision Targeted Therapy with BLU-667 for RET -Driven Cancers

(2018) Vivek Subbiah et al.   Cancer Discovery

Targeting RET-driven cancers: lessons from evolving preclinical and clinical landscapes

(2017) Alexander Drilon et al.   Nature Reviews Clinical Oncology

Drugging the catalytically inactive state of RET kinase in RET-rearranged tumors

(2017) Dennis Plenker et al.   Science Translational Medicine

Enriching screening libraries with bioactive fragment space

(2016) Na Zhang et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

RET Aberrations in Diverse Cancers: Next-Generation Sequencing of 4,871 Patients

(2016) Shumei Kato et al.   CLINICAL CANCER RESEARCH

RET kinase inhibitors: a review of recent patents (2012–2015)

(2016) Luca Mologni et al.   EXPERT OPINION ON THERAPEUTIC PATENTS

A comprehensive overview of the role of the RET proto-oncogene in thyroid carcinoma

(2016) Cristina Romei et al.   Nature Reviews Endocrinology

PF-06463922, an ALK/ROS1 Inhibitor, Overcomes Resistance to First and Second Generation ALK Inhibitors in Preclinical Models

(2015) Helen Y. Zou et al.   CANCER CELL

A Pyrazolo[3,4-d]pyrimidin-4-amine Derivative Containing an Isoxazole Moiety Is a Selective and Potent Inhibitor of RET Gatekeeper Mutants

(2015) Hojong Yoon et al.   JOURNAL OF MEDICINAL CHEMISTRY

Clinical and prognostic implications of RET rearrangements in metastatic lung adenocarcinoma patients with malignant pleural effusion

(2015) Tzu-Hsiu Tsai et al.   LUNG CANCER

Exploration of Type II Binding Mode: A Privileged Approach for Kinase Inhibitor Focused Drug Discovery?

(2014) Zheng Zhao et al.   ACS Chemical Biology

RET-rearranged non-small-cell lung carcinoma: a clinicopathological and molecular analysis

(2014) K Tsuta et al.   BRITISH JOURNAL OF CANCER

Conformational Analysis of the DFG-Out Kinase Motif and Biochemical Profiling of Structurally Validated Type II Inhibitors

(2014) R. S. K. Vijayan et al.   JOURNAL OF MEDICINAL CHEMISTRY

Sorafenib in radioactive iodine-refractory, locally advanced or metastatic differentiated thyroid cancer: a randomised, double-blind, phase 3 trial

(2014) Marcia S Brose et al.   LANCET

Alectinib Shows Potent Antitumor Activity against RET-Rearranged Non-Small Cell Lung Cancer

(2014) T. Kodama et al.   MOLECULAR CANCER THERAPEUTICS

Ceritinib in ALK-Rearranged Non–Small-Cell Lung Cancer

(2014) Alice T. Shaw et al.   NEW ENGLAND JOURNAL OF MEDICINE

First-Line Crizotinib versus Chemotherapy in ALK-Positive Lung Cancer

(2014) Benjamin J. Solomon et al.   NEW ENGLAND JOURNAL OF MEDICINE

Type II Kinase Inhibitors: An Opportunity in Cancer for Rational Design

(2013) Javier Blanc et al.   Anti-Cancer Agents in Medicinal Chemistry

Antitumor activities of the targeted multi-tyrosine kinase inhibitor lenvatinib (E7080) against RET gene fusion-driven tumor models

(2013) Kiyoshi Okamoto et al.   CANCER LETTERS

Cabozantinib in Progressive Medullary Thyroid Cancer

(2013) Rossella Elisei et al.   JOURNAL OF CLINICAL ONCOLOGY

Phase III Study of Afatinib or Cisplatin Plus Pemetrexed in Patients With Metastatic Lung Adenocarcinoma WithEGFRMutations

(2013) Lecia V. Sequist et al.   JOURNAL OF CLINICAL ONCOLOGY

Ponatinib is a potent inhibitor of wild-type and drug-resistant gatekeeper mutant RET kinase

(2013) Luca Mologni et al.   MOLECULAR AND CELLULAR ENDOCRINOLOGY

Novel Targets in Non-Small Cell Lung Cancer: ROS1 and RET Fusions

(2013) J. F. Gainor et al.   ONCOLOGIST

KIF5B-RET fusions in lung adenocarcinoma

(2012) Takashi Kohno et al.   NATURE MEDICINE

Vandetanib in Patients With Locally Advanced or Metastatic Medullary Thyroid Cancer: A Randomized, Double-Blind Phase III Trial

(2011) Samuel A. Wells et al.   JOURNAL OF CLINICAL ONCOLOGY

Comprehensive assay of kinase catalytic activity reveals features of kinase inhibitor selectivity

(2011) Theonie Anastassiadis et al.   NATURE BIOTECHNOLOGY

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

Small-molecule inhibitors binding to protein kinase. Part II: the novel pharmacophore approach of type II and type III inhibition

(2008) AC Backes et al.   Expert Opinion on Drug Discovery

Small-molecule inhibitors binding to protein kinases. Part I: exceptions from the traditional pharmacophore approach of type I inhibition

(2008) AC Backes et al.   Expert Opinion on Drug Discovery

A quantitative analysis of kinase inhibitor selectivity

(2008) Mazen W Karaman et al.   NATURE BIOTECHNOLOGY

The T790M mutation in EGFR kinase causes drug resistance by increasing the affinity for ATP

(2008) C.-H. Yun et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA