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Volume 13, Issue 5
1 May 2014
Molecular Cancer Therapeutics Cover Image for Volume 13, Issue 5
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    Cover Image

    Issue cover image
    Angiogenesis is important for tumor progression. In squamous cell carcinoma of the head and neck (SCCHN), angiogenesis is activated by cytokines including IL-6 and VEGF. Galanin receptor 2 (GALR2) is a G protein–coupled receptor that induces aggressive growth in SCCHN. GALR2 stimulates tumor angiogenesis in SCCHN via p38-mediated inhibition of tristetraprolin (TTP) with resultant enhanced cytokine secretion. Given that p38 inhibitors are in clinical use for inflammatory disorders, GALR2/p38-mediated cytokine secretion may be an excellent target for new adjuvant therapy in SCCHN. For details, see article by Banerjee, Van Tubergen, and colleagues on page 1323.
  • PDF Icon PDF LinkTable of Contents
ISSN 1535-7163
EISSN 1538-8514

Highlights

Highlights of This Issue
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Review

Picking the Point of Inhibition: A Comparative Review of PI3K/AKT/mTOR Pathway Inhibitors
Rodrigo Dienstmann; Jordi Rodon; Violeta Serra; Josep Tabernero
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Small Molecule Therapeutics

Enhancement of Nab-Paclitaxel Antitumor Activity through Addition of Multitargeting Antiangiogenic Agents in Experimental Pancreatic Cancer
Niranjan Awasthi; Changhua Zhang; Anna M. Schwarz; Stefan Hinz; Margaret A. Schwarz; Roderich E. Schwarz
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Author Choice
The Phosphoinositide 3-Kinase α Selective Inhibitor BYL719 Enhances the Effect of the Protein Kinase C Inhibitor AEB071 in GNAQ/GNA11-Mutant Uveal Melanoma Cells
Elgilda Musi; Grazia Ambrosini; Elisa de Stanchina; Gary K. Schwartz
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Centmitor-1, a Novel Acridinyl-Acetohydrazide, Possesses Similar Molecular Interaction Field and Antimitotic Cellular Phenotype as Rigosertib, ON 01910.Na
Jenni H.E. Mäki-Jouppila; Leena J. Laine; Jonathan Rehnberg; Elli Narvi; Pekka Tiikkainen; Elvira Hukasova; Pasi Halonen; Arne Lindqvist; Lila Kallio; Antti Poso; Marko J. Kallio
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Preclinical Evaluation of the Supercritical Extract of Azadirachta Indica (Neem) Leaves In Vitro and In Vivo on Inhibition of Prostate Cancer Tumor Growth
Qiang Wu; Manish Kohli; H. Robert. Bergen, III; John C. Cheville; R. Jeffrey Karnes; Hong Cao; Charles Y.F. Young; Donald J. Tindall; Mark A. McNiven; Krishna Vanaja Donkena
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Characterization of the Activity of the PI3K/mTOR Inhibitor XL765 (SAR245409) in Tumor Models with Diverse Genetic Alterations Affecting the PI3K Pathway
Peiwen Yu; A. Douglas Laird; Xiangnan Du; Jianming Wu; Kwang-Ai Won; Kyoko Yamaguchi; Pin Pin Hsu; Fawn Qian; Christopher T. Jaeger; Wentao Zhang; Chris A. Buhr; Paula Shen; Wendy Abulafia; Jason Chen; Jenny Young; Arthur Plonowski; F. Michael Yakes; Felix Chu; Michelle Lee; Frauke Bentzien; Sanh Tan Lam; Stephanie Dale; David J. Matthews; Peter Lamb; Paul Foster
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UPARANT: A Urokinase Receptor–Derived Peptide Inhibitor of VEGF-Driven Angiogenesis with Enhanced Stability and In Vitro and In Vivo Potency
Maria Vincenza Carriero; Katia Bifulco; Michele Minopoli; Liliana Lista; Ornella Maglio; Luigi Mele; Gioconda Di Carluccio; Mario De Rosa; Vincenzo Pavone
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Preclinical Pharmacological Evaluation of a Novel Multiple Kinase Inhibitor, ON123300, in Brain Tumor Models
Xiaoping Zhang; Hua Lv; Qingyu Zhou; Rana Elkholi; Jerry E. Chipuk; M.V. Ramana Reddy; E. Premkumar Reddy; James M. Gallo
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Author Choice
Characterization of the Novel and Specific PI3Kα Inhibitor NVP-BYL719 and Development of the Patient Stratification Strategy for Clinical Trials
Christine Fritsch; Alan Huang; Christian Chatenay-Rivauday; Christian Schnell; Anupama Reddy; Manway Liu; Audrey Kauffmann; Daniel Guthy; Dirk Erdmann; Alain De Pover; Pascal Furet; Hui Gao; Stephane Ferretti; Youzhen Wang; Joerg Trappe; Saskia M. Brachmann; Sauveur-Michel Maira; Christopher Wilson; Markus Boehm; Carlos Garcia-Echeverria; Patrick Chene; Marion Wiesmann; Robert Cozens; Joseph Lehar; Robert Schlegel; Giorgio Caravatti; Francesco Hofmann; William R. Sellers
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Protein Kinase D as a Potential Chemotherapeutic Target for Colorectal Cancer
Ning Wei; Edward Chu; Peter Wipf; John C. Schmitz
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Highly Active Combination of BRD4 Antagonist and Histone Deacetylase Inhibitor against Human Acute Myelogenous Leukemia Cells
Warren Fiskus; Sunil Sharma; Jun Qi; John A. Valenta; Leasha J. Schaub; Bhavin Shah; Karissa Peth; Bryce P. Portier; Melissa Rodriguez; Santhana G.T. Devaraj; Ming Zhan; Jianting Sheng; Swaminathan P. Iyer; James E. Bradner; Kapil N. Bhalla
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Combination of Imatinib with CXCR4 Antagonist BKT140 Overcomes the Protective Effect of Stroma and Targets CML In Vitro and In Vivo
Katia Beider; Merav Darash-Yahana; Orly Blaier; Maya Koren-Michowitz; Michal Abraham; Hanna Wald; Ori Wald; Eithan Galun; Orly Eizenberg; Amnon Peled; Arnon Nagler
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The Use of Olaparib (AZD2281) Potentiates SN-38 Cytotoxicity in Colon Cancer Cells by Indirect Inhibition of Rad51-Mediated Repair of DNA Double-Strand Breaks
Makiko Tahara; Takeshi Inoue; Futoshi Sato; Yasuyuki Miyakura; Hisanaga Horie; Yoshikazu Yasuda; Hirofumi Fujii; Kenjiro Kotake; Kokichi Sugano
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A Novel Temozolomide–Perillyl Alcohol Conjugate Exhibits Superior Activity against Breast Cancer Cells In Vitro and Intracranial Triple-Negative Tumor Growth In Vivo
Thomas C. Chen; Hee-Yeon Cho; Weijun Wang; Manasi Barath; Natasha Sharma; Florence M. Hofman; Axel H. Schönthal
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Cancer Biology and Signal Transduction

Targeting STAT5 in Hematologic Malignancies through Inhibition of the Bromodomain and Extra-Terminal (BET) Bromodomain Protein BRD2
Suhu Liu; Sarah R. Walker; Erik A. Nelson; Robert Cerulli; Michael Xiang; Patricia A. Toniolo; Jun Qi; Richard M. Stone; Martha Wadleigh; James E. Bradner; David A. Frank
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Embelin Reduces Colitis-Associated Tumorigenesis through Limiting IL-6/STAT3 Signaling
Yun Dai; Hongmei Jiao; Guigen Teng; Weihong Wang; Rongxin Zhang; Yunhong Wang; Lionel Hebbard; Jacob George; Liang Qiao
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Ponatinib Induces Apoptosis in Imatinib-Resistant Human Mast Cells by Dephosphorylating Mutant D816V KIT and Silencing β-Catenin Signaling
Bei Jin; Ke Ding; Jingxuan Pan
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PIM Kinases Are Essential for Chronic Lymphocytic Leukemia Cell Survival (PIM2/3) and CXCR4-Mediated Microenvironmental Interactions (PIM1)
Sarah Decker; Johannes Finter; Aaron James Forde; Sandra Kissel; Juerg Schwaller; Thomas Sebastian Mack; Anabel Kuhn; Nathanael Gray; Marie Follo; Hassan Jumaa; Meike Burger; Katja Zirlik; Dietmar Pfeifer; Chandrasekhar V. Miduturu; Hermann Eibel; Hendrik Veelken; Christine Dierks
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Pharmacologic Suppression of JAK1/2 by JAK1/2 Inhibitor AZD1480 Potently Inhibits IL-6–Induced Experimental Prostate Cancer Metastases Formation
Lei Gu; Pooja Talati; Paraskevi Vogiatzi; Ana L. Romero-Weaver; Junaid Abdulghani; Zhiyong Liao; Benjamin Leiby; David T. Hoang; Tuomas Mirtti; Kalle Alanen; Michael Zinda; Dennis Huszar; Marja T. Nevalainen
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Hedgehog Pathway Inhibition in Chondrosarcoma Using the Smoothened Inhibitor IPI-926 Directly Inhibits Sarcoma Cell Growth
Veronica T. Campbell; Puviindran Nadesan; S. Amanda Ali; Chang Ye Yale Wang; Heather Whetstone; Raymond Poon; Qingxia Wei; John Keilty; Jennifer Proctor; Lauren W. Wang; Suneel S. Apte; Karen McGovern; Benjamin A. Alman; Jay S. Wunder
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Epithelial-to-Mesenchymal Transition Mediates Docetaxel Resistance and High Risk of Relapse in Prostate Cancer
Mercedes Marín-Aguilera; Jordi Codony-Servat; Òscar Reig; Juan José Lozano; Pedro Luis Fernández; María Verónica Pereira; Natalia Jiménez; Michael Donovan; Pere Puig; Lourdes Mengual; Raquel Bermudo; Albert Font; Enrique Gallardo; María José Ribal; Antonio Alcaraz; Pere Gascón; Begoña Mellado
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Identification of Transmembrane Protein 98 as a Novel Chemoresistance-Conferring Gene in Hepatocellular Carcinoma
Kevin Tak-Pan Ng; Chung Mau Lo; Dong Yong Guo; Xiang Qi; Chang Xian Li; Wei Geng; Xiao Bing Liu; Chang Chun Ling; Yuen Yuen Ma; Wai Ho Yeung; Yan Shao; Ronnie Tung-Ping Poon; Sheung Tat Fan; Kwan Man
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Aurora Kinase Inhibition Induces PUMA via NF-κB to Kill Colon Cancer Cells
Jing Sun; Kyle Knickelbein; Kan He; Dongshi Chen; Crissy Dudgeon; Yongqian Shu; Jian Yu; Lin Zhang
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Nuclear Translocation of Hand-1 Acts as a Molecular Switch to Regulate Vascular Radiosensitivity in Medulloblastoma Tumors: The Protein uPAR Is a Cytoplasmic Sequestration Factor for Hand-1
Swapna Asuthkar; Venkateswara Rao Gogineni; Jasti S. Rao; Kiran Kumar Velpula
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The G Protein–Coupled Receptor GALR2 Promotes Angiogenesis in Head and Neck Cancer
Rajat Banerjee; Elizabeth A. Van Tubergen; Christina S. Scanlon; Robert Vander Broek; Joel P. Lints; Min Liu; Nickole Russo; Ronald C. Inglehart; Yugang Wang; Peter J. Polverini; Keith L. Kirkwood; Nisha J. D'Silva
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The Role of Gene Body Cytosine Modifications in MGMT Expression and Sensitivity to Temozolomide
Erika L. Moen; Amy L. Stark; Wei Zhang; M. Eileen Dolan; Lucy A. Godley
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ERBB3/HER2 Signaling Promotes Resistance to EGFR Blockade in Head and Neck and Colorectal Cancer Models
Li Zhang; Carla Castanaro; Bo Luan; Katie Yang; Liangfen Fan; Jeanette L. Fairhurst; Ashique Rafique; Terra B. Potocky; Jing Shan; Frank J. Delfino; Ergang Shi; Tammy Huang; Joel H. Martin; Gang Chen; Douglas MacDonald; John S. Rudge; Gavin Thurston; Christopher Daly
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Nuclear Epidermal Growth Factor Receptor Is a Functional Molecular Target in Triple-Negative Breast Cancer
Toni M. Brand; Mari Iida; Emily F. Dunn; Neha Luthar; Kellie T. Kostopoulos; Kelsey L. Corrigan; Matthew J. Wleklinski; David Yang; Kari B. Wisinski; Ravi Salgia; Deric L. Wheeler
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Metallothionein 1G and Zinc Sensitize Human Colorectal Cancer Cells to Chemotherapy
Juan M. Arriaga; Angela Greco; José Mordoh; Michele Bianchini
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Companion Diagnostics and Cancer Biomarkers

Concordance of Genomic Alterations between Primary and Recurrent Breast Cancer
Funda Meric-Bernstam; Garrett M. Frampton; Jaime Ferrer-Lozano; Roman Yelensky; Jose A. Pérez-Fidalgo; Ying Wang; Gary A. Palmer; Jeffrey S. Ross; Vincent A. Miller; Xiaoping Su; Pilar Eroles; Juan Antonio Barrera; Octavio Burgues; Ana M. Lluch; Xiaofeng Zheng; Aysegul Sahin; Philip J. Stephens; Gordon B. Mills; Maureen T. Cronin; Ana M. Gonzalez-Angulo
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