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1 January 2016
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Activation of the receptor tyrosine kinase Met and its ligand, hepatocyte growth factor/scatter factor, leads to dissociation of cells from the primary tumor, causing metastasis. Therefore, both proteins and their interaction are major metastasis targets. Using a fragment-based approach, small lead compounds were identified that target this protein–protein interface leading to a reduction in phosphorylation of downstream effectors such as Akt, inhibition of cell migration, and prevention of tumor formation in cell-based assays. For details, see the article by Winter and colleagues on page 3. - PDF Icon PDF LinkTable of Contents
ISSN 1535-7163
EISSN 1538-8514
Highlights
Small Molecule Therapeutics
Identification of Selective Lead Compounds for Treatment of High-Ploidy Breast Cancer
Alka Choudhary; Brittany Zachek; Robert F. Lera; Lauren M. Zasadil; Amber Lasek; Ryan A. Denu; Hyunjung Kim; Craig Kanugh; Jennifer J. Laffin; Josephine M. Harter; Kari B. Wisinski; Sandeep Saha; Beth A. Weaver; Mark E. Burkard
Synergistic Myeloma Cell Death via Novel Intracellular Activation of Caspase-10–Dependent Apoptosis by Carfilzomib and Selinexor
Shaun Rosebeck; Mattina M. Alonge; Malathi Kandarpa; Anoop Mayampurath; Samuel L. Volchenboum; Jagoda Jasielec; Dominik Dytfeld; Sean P. Maxwell; Stephanie J. Kraftson; Dilara McCauley; Sharon Shacham; Michael Kauffman; Andrzej J. Jakubowiak
Specific Antileukemic Activity of PD0332991, a CDK4/6 Inhibitor, against Philadelphia Chromosome–Positive Lymphoid Leukemia
Atsushi Nemoto; Satoshi Saida; Itaru Kato; Jiro Kikuchi; Yusuke Furukawa; Yasuhiro Maeda; Koshi Akahane; Hiroko Honna-Oshiro; Kumiko Goi; Keiko Kagami; Shinya Kimura; Yuko Sato; Seiichi Okabe; Akira Niwa; Kenichiro Watanabe; Tatsutoshi Nakahata; Toshio Heike; Kanji Sugita; Takeshi Inukai
Large Molecule Therapeutics
Nanoconjugation of PSMA-Targeting Ligands Enhances Perinuclear Localization and Improves Efficacy of Delivered Alpha-Particle Emitters against Tumor Endothelial Analogues
Charles Zhu; Amey Bandekar; Michelle Sempkowski; Sangeeta Ray Banerjee; Martin G. Pomper; Frank Bruchertseifer; Alfred Morgenstern; Stavroula Sofou
Dual Agonist Surrobody Simultaneously Activates Death Receptors DR4 and DR5 to Induce Cancer Cell Death
Snezana Milutinovic; Arun K. Kashyap; Teruki Yanagi; Carina Wimer; Sihong Zhou; Ryann O'Neil; Aaron L. Kurtzman; Alexsandr Faynboym; Li Xu; Charles H. Hannum; Paul W. Diaz; Shu-ichi Matsuzawa; Michael Horowitz; Lawrence Horowitz; Ramesh R. Bhatt; John C. Reed
Cancer Biology and Signal Transduction
Bevacizumab-Induced Inhibition of Angiogenesis Promotes a More Homogeneous Intratumoral Distribution of Paclitaxel, Improving the Antitumor Response
Marta Cesca; Lavinia Morosi; Alexander Berndt; Ilaria Fuso Nerini; Roberta Frapolli; Petra Richter; Alessandra Decio; Olaf Dirsch; Edoardo Micotti; Silvia Giordano; Maurizio D'Incalci; Enrico Davoli; Massimo Zucchetti; Raffaella Giavazzi
Activation of EGFR Bypass Signaling by TGFα Overexpression Induces Acquired Resistance to Alectinib in ALK-Translocated Lung Cancer Cells
Tetsuo Tani; Hiroyuki Yasuda; Junko Hamamoto; Aoi Kuroda; Daisuke Arai; Kota Ishioka; Keiko Ohgino; Masayoshi Miyawaki; Ichiro Kawada; Katsuhiko Naoki; Yuichiro Hayashi; Tomoko Betsuyaku; Kenzo Soejima
Author Choice
Preclinical Evidence That Trametinib Enhances the Response to Antiangiogenic Tyrosine Kinase Inhibitors in Renal Cell Carcinoma
Victoria L. Bridgeman; Elaine Wan; Shane Foo; Mark R. Nathan; Jonathan C. Welti; Sophia Frentzas; Peter B. Vermeulen; Natasha Preece; Caroline J. Springer; Thomas Powles; Paul D. Nathan; James Larkin; Martin Gore; Naveen S. Vasudev; Andrew R. Reynolds
Companion Diagnostics and Cancer Biomarkers
Models and Technologies
Targeted Photodynamic Virotherapy Armed with a Genetically Encoded Photosensitizer
Kiyoto Takehara; Hiroshi Tazawa; Naohiro Okada; Yuuri Hashimoto; Satoru Kikuchi; Shinji Kuroda; Hiroyuki Kishimoto; Yasuhiro Shirakawa; Nobuhiro Narii; Hiroyuki Mizuguchi; Yasuo Urata; Shunsuke Kagawa; Toshiyoshi Fujiwara
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