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1 May 2016
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Cover Image
Cover Image
The tetravalent FAP-DR5 bispecific antibody (RG7386) is rationally designed to exhibit bivalent binding to FAP and DR5. By simultaneous binding to both targets, the death receptor on tumor cells is being hyper–cross-linked, resulting in strictly target-dependent apoptosis induction of cancer cells. For details, see the article by Brünker, Wartha, and colleagues beginning on page 946.Close Modal - PDF Icon PDF LinkTable of Contents
ISSN 1535-7163
EISSN 1538-8514
Highlights
Reviews
Small Molecule Therapeutics
Applying Small Molecule Signal Transducer and Activator of Transcription-3 (STAT3) Protein Inhibitors as Pancreatic Cancer Therapeutics
Carolyn C. Arpin; Stephen Mac; Yanlin Jiang; Huiwen Cheng; Michelle Grimard; Brent D.G. Page; Malgorzata M. Kamocka; Sina Haftchenary; Han Su; Daniel P. Ball; David A. Rosa; Ping-Shan Lai; Rodolfo F. Gómez-Biagi; Ahmed M. Ali; Rahul Rana; Helmut Hanenberg; Kagan Kerman; Kyle C. McElyea; George E. Sandusky; Patrick T. Gunning; Melissa L. Fishel
EC-70124, a Novel Glycosylated Indolocarbazole Multikinase Inhibitor, Reverts Tumorigenic and Stem Cell Properties in Prostate Cancer by Inhibiting STAT3 and NF-κB
Gianluca Civenni; Nicole Longoni; Paula Costales; Cecilia Dallavalle; Cristina García Inclán; Domenico Albino; Luz Elena Nuñez; Francisco Morís; Giuseppina M. Carbone; Carlo V. Catapano
Histone Deacetylase Inhibitors Enhance the Therapeutic Potential of Reovirus in Multiple Myeloma
Andrew Stiff; Enrico Caserta; Douglas W. Sborov; Gerard J. Nuovo; Xiaokui Mo; Sarah Y. Schlotter; Alessandro Canella; Emily Smith; Joseph Badway; Matthew Old; Alena Cristina Jaime-Ramirez; Pearlly Yan; Don M. Benson; John C. Byrd; Robert Baiocchi; Balveen Kaur; Craig C. Hofmeister; Flavia Pichiorri
Combined Effects of Suberoylanilide Hydroxamic Acid and Cisplatin on Radiation Sensitivity and Cancer Cell Invasion in Non–Small Cell Lung Cancer
Jianguo Feng; Shirong Zhang; Kan Wu; Bing Wang; Jeffrey Y.C. Wong; Hong Jiang; Rujun Xu; Lisha Ying; Haixiu Huang; Xiaoliang Zheng; Xufeng Chen; Shenglin Ma
Bortezomib Inhibits Giant Cell Tumor of Bone through Induction of Cell Apoptosis and Inhibition of Osteoclast Recruitment, Giant Cell Formation, and Bone Resorption
Leqin Xu; Jian Luo; Rongrong Jin; Zhiying Yue; Peng Sun; Zhengfeng Yang; Xinghai Yang; Wei Wan; Jishen Zhang; Shichang Li; Mingyao Liu; Jianru Xiao
Author Choice
Intermittent High-Dose Scheduling of AZD8835, a Novel Selective Inhibitor of PI3Kα and PI3Kδ, Demonstrates Treatment Strategies for PIK3CA-Dependent Breast Cancers
Kevin Hudson; Urs J. Hancox; Cath Trigwell; Robert McEwen; Urszula M. Polanska; Myria Nikolaou; Pablo Morentin Gutierrez; Alvaro Avivar-Valderas; Oona Delpuech; Phillippa Dudley; Lyndsey Hanson; Rebecca Ellston; Alys Jones; Marie Cumberbatch; Sabina C. Cosulich; Lara Ward; Francisco Cruzalegui; Stephen Green
Effective Concentration of a Multikinase Inhibitor within Bone Marrow Correlates with In Vitro Cell Killing in Therapy-Resistant Chronic Myeloid Leukemia
Chaofeng Mu; Xiaoyan Wu; Helen Ma; Wenjing Tao; Guodong Zhang; Xiaojun Xia; Jianliang Shen; Junhua Mai; Tong Sun; Xiaoping Sun; Ralph B. Arlinghaus; Haifa Shen
Author Choice
7-(2-Thienyl)-7-Deazaadenosine (AB61), a New Potent Nucleoside Cytostatic with a Complex Mode of Action
Pavla Perlíková; Gabriela Rylová; Petr Nauš; Tomáš Elbert; Eva Tloušťová; Aurelie Bourderioux; Lenka Poštová Slavětínská; Kamil Motyka; Dalibor Doležal; Pawel Znojek; Alice Nová; Monika Harvanová; Petr Džubák; Michal Šiller; Jan Hlaváč; Marián Hajdúch; Michal Hocek
Large Molecule Therapeutics
Author Choice
Development of Novel Quaternary Ammonium Linkers for Antibody–Drug Conjugates
Patrick J. Burke; Joseph Z. Hamilton; Thomas A. Pires; Jocelyn R. Setter; Joshua H. Hunter; Julia H. Cochran; Andrew B. Waight; Kristine A. Gordon; Brian E. Toki; Kim K. Emmerton; Weiping Zeng; Ivan J. Stone; Peter D. Senter; Robert P. Lyon; Scott C. Jeffrey
Author Choice
RG7386, a Novel Tetravalent FAP-DR5 Antibody, Effectively Triggers FAP-Dependent, Avidity-Driven DR5 Hyperclustering and Tumor Cell Apoptosis
Peter Brünker; Katharina Wartha; Thomas Friess; Sandra Grau-Richards; Inja Waldhauer; Claudia Ferrara Koller; Barbara Weiser; Meher Majety; Valeria Runza; Huifeng Niu; Kathryn Packman; Ningping Feng; Sherif Daouti; Ralf J. Hosse; Ekkehard Mössner; Thomas G. Weber; Frank Herting; Werner Scheuer; Hadassah Sade; Cuiying Shao; Bin Liu; Peng Wang; Gary Xu; Suzana Vega-Harring; Christian Klein; Klaus Bosslet; Pablo Umaña
Molecular Basis of Valine-Citrulline-PABC Linker Instability in Site-Specific ADCs and Its Mitigation by Linker Design
Magdalena Dorywalska; Russell Dushin; Ludivine Moine; Santiago E. Farias; Dahui Zhou; Thayalan Navaratnam; Victor Lui; Adela Hasa-Moreno; Meritxell Galindo Casas; Thomas-Toan Tran; Kathy Delaria; Shu-Hui Liu; Davide Foletti; Christopher J. O'Donnell; Jaume Pons; David L. Shelton; Arvind Rajpal; Pavel Strop
A Novel Recombinant Anti-CD22 Immunokinase Delivers Proapoptotic Activity of Death-Associated Protein Kinase (DAPK) and Mediates Cytotoxicity in Neoplastic B Cells
Nils Lilienthal; Gregor Lohmann; Giuliano Crispatzu; Elena Vasyutina; Stefan Zittrich; Petra Mayer; Carmen Diana Herling; Mehmet Kemal Tur; Michael Hallek; Gabriele Pfitzer; Stefan Barth; Marco Herling
Gastric Adenocarcinomas Express the Glycosphingolipid Gb3/CD77: Targeting of Gastric Cancer Cells with Shiga Toxin B-Subunit
Philipp Emanuel Geyer; Matthias Maak; Ulrich Nitsche; Markus Perl; Alexander Novotny; Julia Slotta-Huspenina; Estelle Dransart; Anne Holtorf; Ludger Johannes; Klaus-Peter Janssen
Cancer Biology and Signal Transduction
Antagonizing the Hedgehog Pathway with Vismodegib Impairs Malignant Pleural Mesothelioma Growth In Vivo by Affecting Stroma
Mayura Meerang; Karima Bérard; Emanuela Felley-Bosco; Olivia Lauk; Bart Vrugt; Andreas Boss; David Kenkel; Angela Broggini-Tenzer; Rolf A. Stahel; Stephan Arni; Walter Weder; Isabelle Opitz
Companion Diagnostics and Cancer Biomarkers
Nanofluidic Digital PCR and Extended Genotyping of RAS and BRAF for Improved Selection of Metastatic Colorectal Cancer Patients for Anti-EGFR Therapies
Daniel Azuara; Cristina Santos; Adriana Lopez-Doriga; Julieta Grasselli; Marga Nadal; Xavier Sanjuan; Fátima Marin; Joana Vidal; Robert Montal; Victor Moreno; Beatriz Bellosillo; Guillem Argiles; Elena Elez; Rodrigo Dienstmann; Clara Montagut; Josep Tabernero; Gabriel Capellá; Ramon Salazar
Author Choice
Expression Profile of BCL-2, BCL-XL, and MCL-1 Predicts Pharmacological Response to the BCL-2 Selective Antagonist Venetoclax in Multiple Myeloma Models
Elizabeth A. Punnoose; Joel D. Leverson; Franklin Peale; Erwin R. Boghaert; Lisa D. Belmont; Nguyen Tan; Amy Young; Michael Mitten; Ellen Ingalla; Walter C. Darbonne; Anatol Oleksijew; Paul Tapang; Peng Yue; Jason Oeh; Leslie Lee; Sophie Maiga; Wayne J. Fairbrother; Martine Amiot; Andrew J. Souers; Deepak Sampath
Models and Technologies
Modeling Therapy Response and Spatial Tissue Distribution of Erlotinib in Pancreatic Cancer
Barbara M. Grüner; Isabel Winkelmann; Annette Feuchtinger; Na Sun; Benjamin Balluff; Nicole Teichmann; Alexander Herner; Evdokia Kalideris; Katja Steiger; Rickmer Braren; Michaela Aichler; Irene Esposito; Roland M. Schmid; Axel Walch; Jens T. Siveke
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