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1 November 2016
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Cover Image
Cover Image
ABOUT THE COVER
The cover features a molecular modeling diagram depicting molecular interaction between LY294002, the active moiety of SF1126, and the BRD4 bromodomain binding domain 1 (BD1). SF1126 is the first known dual inhibitor of PI3K and BRD4 in a single chemotype. The figure shows LY294002 and JQ1 docked at the key acetyl-lysine recognition pocket of BRD4-BD1. LY294002 is displayed with brown carbons and JQ1 with magenta carbons. SF1126 will enter clinical trials in liver cancer this year. For details, see the article by Singh, Joshi, and Burgoyne et al on page 2553. - PDF Icon PDF LinkTable of Contents
- PDF Icon PDF LinkEditorial Board
ISSN 1535-7163
EISSN 1538-8514
Highlights
Small Molecule Therapeutics
Author Choice
Single Agent and Synergistic Activity of the “First-in-Class” Dual PI3K/BRD4 Inhibitor SF1126 with Sorafenib in Hepatocellular Carcinoma
Alok R. Singh; Shweta Joshi; Adam M. Burgoyne; Jason K. Sicklick; Sadakatsu Ikeda; Yuko Kono; Joseph R. Garlich; Guillermo A. Morales; Donald L. Durden
AZD5153: A Novel Bivalent BET Bromodomain Inhibitor Highly Active against Hematologic Malignancies
Garrett W. Rhyasen; Maureen M. Hattersley; Yi Yao; Austin Dulak; Wenxian Wang; Philip Petteruti; Ian L. Dale; Scott Boiko; Tony Cheung; Jingwen Zhang; Shenghua Wen; Lillian Castriotta; Deborah Lawson; Michael Collins; Larry Bao; Miika J. Ahdesmaki; Graeme Walker; Greg O'Connor; Tammie C. Yeh; Alfred A. Rabow; Jonathan R. Dry; Corinne Reimer; Paul Lyne; Gordon B. Mills; Stephen E. Fawell; Michael J. Waring; Michael Zinda; Edwin Clark; Huawei Chen
Proteoglycans as Target for an Innovative Therapeutic Approach in Chondrosarcoma: Preclinical Proof of Concept
Caroline Peyrode; Valérie Weber; Aurélien Voissière; Aurélie Maisonial-Besset; Aurélien Vidal; Philippe Auzeloux; Vincent Gaumet; Michèle Borel; Marie-Mélanie Dauplat; Mercedes Quintana; Françoise Degoul; Françoise Rédini; Jean-Michel Chezal; Elisabeth Miot-Noirault
AC0010, an Irreversible EGFR Inhibitor Selectively Targeting Mutated EGFR and Overcoming T790M-Induced Resistance in Animal Models and Lung Cancer Patients
Xiao Xu; Long Mao; Wanhong Xu; Wei Tang; Xiaoying Zhang; Biao Xi; Rongda Xu; Xin Fang; Jia Liu; Ce Fang; Li Zhao; Xiaobo Wang; Ji Jiang; Pei Hu; Hongyun Zhao; Li Zhang
Author Choice
E7090, a Novel Selective Inhibitor of Fibroblast Growth Factor Receptors, Displays Potent Antitumor Activity and Prolongs Survival in Preclinical Models
Saori Watanabe Miyano; Yuji Yamamoto; Kotaro Kodama; Yukiko Miyajima; Masaki Mikamoto; Takayuki Nakagawa; Hiroko Kuramochi; Setsuo Funasaka; Satoshi Nagao; Naoko Hata Sugi; Kiyoshi Okamoto; Yukinori Minoshima; Yusuke Nakatani; Yuki Karoji; Isao Ohashi; Yoshinobu Yamane; Toshimi Okada; Tomohiro Matsushima; Junji Matsui; Masao Iwata; Toshimitsu Uenaka; Akihiko Tsuruoka
Mitochondria-Targeted Doxorubicin: A New Therapeutic Strategy against Doxorubicin-Resistant Osteosarcoma
Ilaria Buondonno; Elena Gazzano; Sae Rin Jean; Valentina Audrito; Joanna Kopecka; Marilù Fanelli; Iris C. Salaroglio; Costanzo Costamagna; Ilaria Roato; Eleonora Mungo; Claudia M. Hattinger; Silvia Deaglio; Shana O. Kelley; Massimo Serra; Chiara Riganti
Reactive Oxygen Species Mediates the Synergistic Activity of Fenretinide Combined with the Microtubule Inhibitor ABT-751 against Multidrug-Resistant Recurrent Neuroblastoma Xenografts
Nancy E. Chen; N. Vanessa Maldonado; Vazgen Khankaldyyan; Hiroyuki Shimada; Michael M. Song; Barry J. Maurer; C. Patrick Reynolds
Large Molecule Therapeutics
Author Choice
The Discovery and Preclinical Development of ASG-5ME, an Antibody–Drug Conjugate Targeting SLC44A4-Positive Epithelial Tumors Including Pancreatic and Prostate Cancer
Michael Mattie; Arthur Raitano; Kendall Morrison; Karen Morrison; Zili An; Linnette Capo; Alla Verlinsky; Monica Leavitt; Jimmy Ou; Rossana Nadell; Hector Aviña; Claudia Guevara; Faisal Malik; Ruth Moser; Steven Duniho; Jeffrey Coleman; Ying Li; Daniel S. Pereira; Fernando Doñate; Ingrid B.J. Joseph; Pia Challita-Eid; Dennis Benjamin; David R. Stover
Author Choice
RN927C, a Site-Specific Trop-2 Antibody–Drug Conjugate (ADC) with Enhanced Stability, Is Highly Efficacious in Preclinical Solid Tumor Models
Pavel Strop; Thomas-Toan Tran; Magdalena Dorywalska; Kathy Delaria; Russell Dushin; Oi Kwan Wong; Wei-Hsien Ho; Dahui Zhou; Aidong Wu; Eugenia Kraynov; Laura Aschenbrenner; Bora Han; Christopher J. O'Donnell; Jaume Pons; Arvind Rajpal; Dave L. Shelton; Shu-Hui Liu
ADCT-301, a Pyrrolobenzodiazepine (PBD) Dimer–Containing Antibody–Drug Conjugate (ADC) Targeting CD25-Expressing Hematological Malignancies
Michael J. Flynn; Francesca Zammarchi; Peter C. Tyrer; Ayse U. Akarca; Narinder Janghra; Charles E. Britten; Carin E.G. Havenith; Jean-Noel Levy; Arnaud Tiberghien; Luke A. Masterson; Conor Barry; Francois D'Hooge; Teresa Marafioti; Paul W.H.I. Parren; David G. Williams; Philip W. Howard; Patrick H. van Berkel; John A. Hartley
Cancer Biology and Signal Transduction
Regulation of HIF1α under Hypoxia by APE1/Ref-1 Impacts CA9 Expression: Dual Targeting in Patient-Derived 3D Pancreatic Cancer Models
Derek P. Logsdon; Michelle Grimard; Meihua Luo; Safi Shahda; Yanlin Jiang; Yan Tong; Zhangsheng Yu; Nicholas Zyromski; Ernestina Schipani; Fabrizio Carta; Claudiu T. Supuran; Murray Korc; Mircea Ivan; Mark R. Kelley; Melissa L. Fishel
The Novel Tubulin-Binding Checkpoint Activator BAL101553 Inhibits EB1-Dependent Migration and Invasion and Promotes Differentiation of Glioblastoma Stem-like Cells
Raphaël Bergès; Aurélie Tchoghandjian; Stéphane Honoré; Marie-Anne Estève; Dominique Figarella-Branger; Felix Bachmann; Heidi A. Lane; Diane Braguer
Dinaciclib Induces Anaphase Catastrophe in Lung Cancer Cells via Inhibition of Cyclin-Dependent Kinases 1 and 2
Alexey V. Danilov; Shanhu Hu; Bernardo Orr; Kristina Godek; Lisa Maria Mustachio; David Sekula; Xi Liu; Masanori Kawakami; Faye M. Johnson; Duane A. Compton; Sarah J. Freemantle; Ethan Dmitrovsky
c-Jun N-Terminal Kinase Inactivation by Mitogen-Activated Protein Kinase Phosphatase 1 Determines Resistance to Taxanes and Anthracyclines in Breast Cancer
Raúl Rincón; Sandra Zazo; Cristina Chamizo; Rebeca Manso; Paula González-Alonso; Ester Martín-Aparicio; Ion Cristóbal; Carmen Cañadas; Rosario Perona; Ana Lluch; Pilar Eroles; Jesús García-Foncillas; Joan Albanell; Ana Rovira; Juan Madoz-Gúrpide; Federico Rojo
Companion Diagnostics and Cancer Biomarkers
Author Choice
Identification of Pharmacodynamic Transcript Biomarkers in Response to FGFR Inhibition by AZD4547
Oona Delpuech; Claire Rooney; Lorraine Mooney; Dawn Baker; Robert Shaw; Michael Dymond; Dennis Wang; Pei Zhang; Sarah Cross; Margaret Veldman-Jones; Joanne Wilson; Barry R. Davies; Jonathan R. Dry; Elaine Kilgour; Paul D. Smith
Expression of Genes Involved in Vascular Morphogenesis and Maturation Predicts Efficacy of Bevacizumab-Based Chemotherapy in Patients Undergoing Liver Resection
Stefan Stremitzer; Wu Zhang; Dongyun Yang; Yan Ning; Yu Sunakawa; Satoshi Matsusaka; Anish Parekh; Satoshi Okazaki; Diana Hanna; Stephanie H. Astrow; Miriana Moran; Jose Hernandez; Craig Stephens; Stefan J. Scherer; Judith Stift; Friedrich Wrba; Thomas Gruenberger; Heinz-Josef Lenz
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