Fragment-Based Discovery of a Dual pan-RET/VEGFR2 Kinase Inhibitor Optimized for Single-Agent Polypharmacology

Exploiting polypharmacology for drug target deconvolution

(2014) Taranjit Singh Gujral et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Cabozantinib in Progressive Medullary Thyroid Cancer

(2013) Rossella Elisei 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

Tumor adaptation and resistance to RAF inhibitors

(2013) Piro Lito et al.   NATURE MEDICINE

Overcoming mutation-based resistance to antiandrogens with rational drug design

(2013) Minna D Balbas et al.   eLife

RET fusion genes are associated with chronic myelomonocytic leukemia and enhance monocytic differentiation

(2012) P Ballerini et al.   LEUKEMIA

Validation of ITD mutations in FLT3 as a therapeutic target in human acute myeloid leukaemia

(2012) Catherine C. Smith et al.   NATURE

Chemical genetic discovery of targets and anti-targets for cancer polypharmacology

(2012) Arvin C. Dar et al.   NATURE

Chipping away at the lung cancer genome

(2012) William Pao 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

Cabozantinib (XL184), a Novel MET and VEGFR2 Inhibitor, Simultaneously Suppresses Metastasis, Angiogenesis, and Tumor Growth

(2011) F. M. Yakes et al.   MOLECULAR CANCER THERAPEUTICS

A roadmap for targeted therapies

(2011) Francesca Carlomagno et al.   Nature Reviews Endocrinology

Mammal-restricted elements predispose human RET to folding impairment by HSCR mutations

(2010) Svend Kjær et al.   NATURE STRUCTURAL & MOLECULAR BIOLOGY

Transforming fragments into candidates: small becomes big in medicinal chemistry

(2009) Gerdien E. de Kloe et al.   DRUG DISCOVERY TODAY

Challenges of fragment screening

(2009) Diane Joseph-McCarthy   JOURNAL OF COMPUTER-AIDED MOLECULAR DESIGN

Novel mutant-selective EGFR kinase inhibitors against EGFR T790M

(2009) Wenjun Zhou et al.   NATURE

Identification of tyrosine 806 as a molecular determinant of RET kinase sensitivity to ZD6474

(2008) Francesca Carlomagno et al.   ENDOCRINE-RELATED CANCER

Type-II Kinase Inhibitor Docking, Screening, and Profiling Using Modified Structures of Active Kinase States

(2008) Irina Kufareva et al.   JOURNAL OF MEDICINAL CHEMISTRY

Synthesis, Modeling, and RET Protein Kinase Inhibitory Activity of 3- and 4-Substituted β-Carbolin-1-ones

(2008) Raffaella Cincinelli et al.   JOURNAL OF MEDICINAL CHEMISTRY