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1 March 2016
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Cover Image
Cover Image
The cover image shows the chemical structure of the novel RAF inhibitor BI 882370 and a schematic representation of its binding mode in the ATP pocket derived from the co-crystal structure with wild-type BRAF kinase. Arrows indicate key polar interactions between the inhibitor and the protein. Solvent-exposed parts of both the ligand and the protein residues are indicated as blue spheres. Green circles indicate amino acids with lipophilic side chains and pink circles show amino acids with polar residues. For details, see the article by Waizenegger and colleagues beginning on page 354. - PDF Icon PDF LinkTable of Contents
ISSN 1535-7163
EISSN 1538-8514
Highlights
Review
Small Molecule Therapeutics
Author Choice
A Novel RAF Kinase Inhibitor with DFG-Out–Binding Mode: High Efficacy in BRAF-Mutant Tumor Xenograft Models in the Absence of Normal Tissue Hyperproliferation
Irene C. Waizenegger; Anke Baum; Steffen Steurer; Heinz Stadtmüller; Gerd Bader; Otmar Schaaf; Pilar Garin-Chesa; Andreas Schlattl; Norbert Schweifer; Christian Haslinger; Florian Colbatzky; Sien Mousa; Arno Kalkuhl; Norbert Kraut; Günther R. Adolf
Preclinical Evaluation of a Novel Orally Available SRC/Raf/VEGFR2 Inhibitor, SKLB646, in the Treatment of Triple-Negative Breast Cancer
Ming-Wu Zheng; Chun-Hui Zhang; Kai Chen; Mei Huang; Ya-Ping Li; Wan-Ting Lin; Rong-Jie Zhang; Lei Zhong; Rong Xiang; Lin-Li Li; Xin-Yu Liu; Yu-Quan Wei; Sheng-Yong Yang
Trastuzumab-Based Photoimmunotherapy Integrated with Viral HER2 Transduction Inhibits Peritoneally Disseminated HER2-Negative Cancer
Michihiro Ishida; Shunsuke Kagawa; Kyoko Shimoyama; Kiyoto Takehara; Kazuhiro Noma; Shunsuke Tanabe; Yasuhiro Shirakawa; Hiroshi Tazawa; Hisataka Kobayashi; Toshiyoshi Fujiwara
Structure-Based Screen Identification of a Mammalian Ste20-like Kinase 4 (MST4) Inhibitor with Therapeutic Potential for Pituitary Tumors
Weipeng Xiong; Christopher J. Matheson; Mei Xu; Donald S. Backos; Taylor S. Mills; Smita Salian-Mehta; Katja Kiseljak-Vassiliades; Philip Reigan; Margaret E. Wierman
High Sensitivity of an Ha-RAS Transgenic Model of Superficial Bladder Cancer to Metformin Is Associated with ∼240-Fold Higher Drug Concentration in Urine than Serum
Zhongbo Liu; Noriko N. Yokoyama; Christopher A. Blair; Xuesen Li; Daina Avizonis; Xue-Ru Wu; Edward Uchio; Ramy Youssef; Michael McClelland; Michael Pollak; Xiaolin Zi
Large Molecule Therapeutics
Phase I Study of DMOT4039A, an Antibody–Drug Conjugate Targeting Mesothelin, in Patients with Unresectable Pancreatic or Platinum-Resistant Ovarian Cancer
Colin D. Weekes; Laetitia E. Lamberts; Mitesh J. Borad; Johannes Voortman; Robert R. McWilliams; Jennifer R. Diamond; Elisabeth G.E. de Vries; Henk M. Verheul; Christopher H. Lieu; George P. Kim; Yulei Wang; Suzie J. Scales; Divya Samineni; Flavia Brunstein; YounJeong Choi; Daniel J. Maslyar; Gerardo Colon-Otero
Cancer Biology and Signal Transduction
GSK-3β Governs Inflammation-Induced NFATc2 Signaling Hubs to Promote Pancreatic Cancer Progression
Sandra Baumgart; Nai-Ming Chen; Jin-San Zhang; Daniel D. Billadeau; Irina N. Gaisina; Alan P. Kozikowski; Shiv K. Singh; Daniel Fink; Philipp Ströbel; Caroline Klindt; Lizhi Zhang; William R. Bamlet; Alexander Koenig; Elisabeth Hessmann; Thomas M. Gress; Volker Ellenrieder; Albrecht Neesse
Models and Technologies
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