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Volume 15, Issue 5
1 May 2016
Molecular Cancer Therapeutics Cover Image for Volume 15, Issue 5
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  • Cover Image

    Cover Image

    Issue 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.
  • PDF Icon PDF LinkTable of Contents
ISSN 1535-7163
EISSN 1538-8514

Highlights

Highlights of This Issue
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Reviews

Featured Image
Strategic Combinations: The Future of Oncolytic Virotherapy with Reovirus
Xing Zhao; Cariad Chester; Narendiran Rajasekaran; ZhiXu He; Holbrook E. Kohrt
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The Role of PGC1α in Cancer Metabolism and its Therapeutic Implications
Zheqiong Tan; Xiangjian Luo; Lanbo Xiao; Min Tang; Ann M. Bode; Zigang Dong; Ya Cao
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Small Molecule Therapeutics

Author Choice
Preclinical Characterization of G1T28: A Novel CDK4/6 Inhibitor for Reduction of Chemotherapy-Induced Myelosuppression
John E. Bisi; Jessica A. Sorrentino; Patrick J. Roberts; Francis X. Tavares; Jay C. Strum
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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
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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
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ABCG2 and ABCB1 Limit the Efficacy of Dasatinib in a PDGF-B–Driven Brainstem Glioma Model
Rajendar K. Mittapalli; Alexander H. Chung; Karen E. Parrish; Donna Crabtree; Kyle G. Halvorson; Guo Hu; William F. Elmquist; Oren J. Becher
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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
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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
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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
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Posaconazole, a Second-Generation Triazole Antifungal Drug, Inhibits the Hedgehog Signaling Pathway and Progression of Basal Cell Carcinoma
Baozhi Chen; Vinh Trang; Alex Lee; Noelle S. Williams; Alexandra N. Wilson; Ervin H. Epstein, Jr; Jean Y. Tang; James Kim
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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
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Addition of DHA Synergistically Enhances the Efficacy of Regorafenib for Kidney Cancer Therapy
Jeffrey Kim; Arzu Ulu; Debin Wan; Jun Yang; Bruce D Hammock; Robert H. Weiss
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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
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Preclinical Evaluation of UAB30 in Pediatric Renal and Hepatic Malignancies
Alicia M. Waters; Jerry E. Stewart; Venkatram R. Atigadda; Elizabeth Mroczek-Musulman; Donald D. Muccio; Clinton J. Grubbs; Elizabeth A. Beierle
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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
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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
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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
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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
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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
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Novel Anti-CRR9/CLPTM1L Antibodies with Antitumorigenic Activity Inhibit Cell Surface Accumulation, PI3K Interaction, and Survival Signaling
László G. Puskás; Imola Mán; Gabor Szebeni; László Tiszlavicz; Susan Tsai; Michael A. James
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Improved Tumor-Specific Drug Accumulation by Polymer Therapeutics with pH-Sensitive Drug Release Overcomes Chemotherapy Resistance
Anne-Kathrin Heinrich; Henrike Lucas; Lucie Schindler; Petr Chytil; Tomáš Etrych; Karsten Mäder; Thomas Mueller
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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
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Cancer Biology and Signal Transduction

The Bromodomain BET Inhibitor JQ1 Suppresses Tumor Angiogenesis in Models of Childhood Sarcoma
Hemant K. Bid; Doris A. Phelps; Linlin Xaio; Denis C. Guttridge; Jiayuh Lin; Cheryl London; Laurence H. Baker; Xiaokui Mo; Peter J. Houghton
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BRD4 Regulates EZH2 Transcription through Upregulation of C-MYC and Represents a Novel Therapeutic Target in Bladder Cancer
Xinchao Wu; Dong Liu; Dan Tao; Wei Xiang; Xingyuan Xiao; Miao Wang; Liang Wang; Gang Luo; Yawei Li; Fuqing Zeng; Guosong Jiang
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Expression of GRP78, Master Regulator of the Unfolded Protein Response, Increases Chemoresistance in Pancreatic Ductal Adenocarcinoma
Jenifer B. Gifford; Wei Huang; Ann E. Zeleniak; Antreas Hindoyan; Hong Wu; Timothy R. Donahue; Reginald Hill
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Protein Kinase Inhibitor H89 Enhances the Activity of Pseudomonas Exotoxin A–Based Immunotoxins
Xiufen Liu; Fabian Müller; Alan S. Wayne; Ira Pastan
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Recombinant Arabidopsis HSP70 Sustains Cell Survival and Metastatic Potential of Breast Cancer Cells
Alessandra Nigro; Loredana Mauro; Francesca Giordano; Salvatore Panza; Rina Iannacone; Grazia Maria Liuzzi; Saveria Aquila; Francesca De Amicis; Francesco Cellini; Cesare Indiveri; Maria Luisa Panno
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CD20-Targeting Immunotherapy Promotes Cellular Senescence in B-Cell Lymphoma
J. Henry M. Däbritz; Yong Yu; Maja Milanovic; Martin Schönlein; Mathias T. Rosenfeldt; Jan R. Dörr; Andreas M. Kaufmann; Bernd Dörken; Clemens A. Schmitt
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Long Noncoding RNA PVT1 Promotes Non–Small Cell Lung Cancer Cell Proliferation through Epigenetically Regulating LATS2 Expression
Li Wan; Ming Sun; Guo-Jian Liu; Chen-Chen Wei; Er-Bao Zhang; Rong Kong; Tong-Peng Xu; Ming-De Huang; Zhao-Xia Wang
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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
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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
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MR Studies of Glioblastoma Models Treated with Dual PI3K/mTOR Inhibitor and Temozolomide:Metabolic Changes Are Associated with Enhanced Survival
Marina Radoul; Myriam M. Chaumeil; Pia Eriksson; Alan S. Wang; Joanna J. Phillips; Sabrina M. Ronen
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High Expression of miR-532-5p, a Tumor Suppressor, Leads to Better Prognosis in Ovarian Cancer Both In Vivo and In Vitro
Fan Wang; Jeremy T.-H. Chang; Chester Jingshiu Kao; R. Stephanie Huang
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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
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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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