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1 October 2017
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ABOUT THE COVER
Quantitative liquid chromatography/mass spectrometry (LC/MS) metabolomics in two BRAF mutant human melanoma xenograft models (WM266.4 and A375), were used to select the metabolites increased or decreased in tumor versus non-tumor bearing animals, whose changes were reversed by the MEK inhibitor RO4987655. Of these 21 metabolites identified preclinically in these models that were sensitive to MEK inhibition, 15 on-treatment changes were significantly correlated with objective responses in patients with advanced melanoma treated with RO4987655 and seven metabolite levels had pre-treatment predictive value. For more details see the article by Ang and colleagues (beginning on page 2315). - PDF Icon PDF LinkTable of Contents
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ISSN 1535-7163
EISSN 1538-8514
Highlights
Small Molecule Therapeutics
Antitumor Effect of the Atypical Retinoid ST1926 in Acute Myeloid Leukemia and Nanoparticle Formulation Prolongs Lifespan and Reduces Tumor Burden of Xenograft Mice
Leeanna El-Houjeiri; Walid Saad; Berthe Hayar; Patrick Aouad; Nadim Tawil; Rana Abdel-Samad; Rita Hleihel; Maguy Hamie; Angelo Mancinelli; Claudio Pisano; Hiba El Hajj; Nadine Darwiche
A Small-Molecule Inhibitor of WEE1, AZD1775, Synergizes with Olaparib by Impairing Homologous Recombination and Enhancing DNA Damage and Apoptosis in Acute Leukemia
Tamara B. Garcia; Jonathan C. Snedeker; Dmitry Baturin; Lori Gardner; Susan P. Fosmire; Chengjing Zhou; Craig T. Jordan; Sujatha Venkataraman; Rajeev Vibhakar; Christopher C. Porter
PI3Kγ/δ and NOTCH1 Cross-Regulate Pathways That Define the T-cell Acute Lymphoblastic Leukemia Disease Signature
Evgeni Efimenko; Utpal P. Davé; Irina V. Lebedeva; Yao Shen; Maria J. Sanchez-Quintero; Daniel Diolaiti; Andrew Kung; Brian J. Lannutti; Jianchung Chen; Ronald Realubit; Zoya Niatsetskaya; Vadim Ten; Charles Karan; Xi Chen; Andrea Califano; Thomas G. Diacovo
Inhibition of Androgen Receptor Nuclear Localization and Castration-Resistant Prostate Tumor Growth by Pyrroloimidazole-based Small Molecules
Khalid Z. Masoodi; Yadong Xu; Javid A. Dar; Kurtis Eisermann; Laura E. Pascal; Erica Parrinello; Junkui Ai; Paul A. Johnston; Joel B. Nelson; Peter Wipf; Zhou Wang
Dual Inhibition of NOX2 and Receptor Tyrosine Kinase by BJ-1301 Enhances Anticancer Therapy Efficacy via Suppression of Autocrine-Stimulatory Factors in Lung Cancer
Jaya Gautam; Jin-Mo Ku; Sushil Chandra Regmi; Hyunyoung Jeong; Ying Wang; Suhrid Banskota; Myo-Hyeon Park; Tae-gyu Nam; Byeong-Seon Jeong; Jung-Ae Kim
Efficacy of AKT Inhibitor ARQ 092 Compared with Sorafenib in a Cirrhotic Rat Model with Hepatocellular Carcinoma
Gaël S. Roth; Zuzana Macek Jilkova; Ayca Zeybek Kuyucu; Keerthi Kurma; Séyédéh Tayébéh Ahmad Pour; Giovanni Abbadessa; Yi Yu; Benoit Busser; Patrice N. Marche; Vincent Leroy; Thomas Decaens
Large Molecule Therapeutics
Alpha Particle Enhanced Blood Brain/Tumor Barrier Permeabilization in Glioblastomas Using Integrin Alpha-v Beta-3–Targeted Liposomes
Anirudh Sattiraju; Xiaobing Xiong; Darpan N. Pandya; Thaddeus J. Wadas; Ang Xuan; Yao Sun; Youngkyoo Jung; Kiran Kumar Solingapuram Sai; Jay F. Dorsey; King C. Li; Akiva Mintz
Author Choice
Epidermal Growth Factor Receptor (EGFR)-targeted Photoimmunotherapy (PIT) for the Treatment of EGFR-expressing Bladder Cancer
Reema Railkar; L. Spencer Krane; Q. Quentin Li; Thomas Sanford; Mohammad Rashid Siddiqui; Diana Haines; Srinivas Vourganti; Sam J. Brancato; Peter L. Choyke; Hisataka Kobayashi; Piyush K. Agarwal
Exposure-Response Analyses of Ramucirumab from Two Randomized, Phase III Trials of Second-line Treatment for Advanced Gastric or Gastroesophageal Junction Cancer
Josep Tabernero; Atsushi Ohtsu; Kei Muro; Eric Van Cutsem; Sang Cheul Oh; György Bodoky; Yasuhiro Shimada; Shuichi Hironaka; Jaffer A. Ajani; Jiri Tomasek; Howard Safran; Kumari Chandrawansa; Yanzhi Hsu; Michael Heathman; Azhar Khan; Lan Ni; Allen S. Melemed; Ling Gao; David Ferry; Charles S. Fuchs
Cancer Biology and Signal Transduction
The IGF1R/INSR Inhibitor BI 885578 Selectively Inhibits Growth of IGF2-Overexpressing Colorectal Cancer Tumors and Potentiates the Efficacy of Anti-VEGF Therapy
Michael P. Sanderson; Marco H. Hofmann; Pilar Garin-Chesa; Norbert Schweifer; Andreas Wernitznig; Stefan Fischer; Astrid Jeschko; Reiner Meyer; Jürgen Moll; Thomas Pecina; Heribert Arnhof; Ulrike Weyer-Czernilofsky; Stephan K. Zahn; Günther R. Adolf; Norbert Kraut
Author Choice
JAK1/STAT3 Activation through a Proinflammatory Cytokine Pathway Leads to Resistance to Molecularly Targeted Therapy in Non–Small Cell Lung Cancer
Kazuhiko Shien; Vassiliki A. Papadimitrakopoulou; Dennis Ruder; Carmen Behrens; Li Shen; Neda Kalhor; Juhee Song; J. Jack Lee; Jing Wang; Ximing Tang; Roy S. Herbst; Shinichi Toyooka; Luc Girard; John D. Minna; Jonathan M. Kurie; Ignacio I. Wistuba; Julie G. Izzo
The Tumor-Suppressor Protein OPCML Potentiates Anti–EGFR- and Anti–HER2-Targeted Therapy in HER2-Positive Ovarian and Breast Cancer
Elisa Zanini; Louay S. Louis; Jane Antony; Evdoxia Karali; Imoh S. Okon; Arthur B. McKie; Sebastian Vaughan; Mona El-Bahrawy; Justin Stebbing; Chiara Recchi; Hani Gabra
Ormeloxifene Suppresses Prostate Tumor Growth and Metastatic Phenotypes via Inhibition of Oncogenic β-catenin Signaling and EMT Progression
Bilal Bin Hafeez; Aditya Ganju; Mohammed Sikander; Vivek K. Kashyap; Zubair Bin Hafeez; Neeraj Chauhan; Shabnam Malik; Andrew E. Massey; Manish K. Tripathi; Fathi T. Halaweish; Nadeem Zafar; Man M. Singh; Murali M. Yallapu; Subhash C. Chauhan; Meena Jaggi
Bypassing Drug Resistance Mechanisms of Prostate Cancer with Small Molecules that Target Androgen Receptor–Chromatin Interactions
Kush Dalal; Meixia Che; Nanette S. Que; Aishwariya Sharma; Rendong Yang; Nada Lallous; Hendrik Borgmann; Deniz Ozistanbullu; Ronnie Tse; Fuqiang Ban; Huifang Li; Kevin J. Tam; Mani Roshan-Moniri; Eric LeBlanc; Martin E. Gleave; Daniel T. Gewirth; Scott M. Dehm; Artem Cherkasov; Paul S. Rennie
Inactivation of the Kinase Domain of CDK10 Prevents Tumor Growth in a Preclinical Model of Colorectal Cancer, and Is Accompanied by Downregulation of Bcl-2
Louis-Bastien Weiswald; Mohammad R. Hasan; John C.T. Wong; Clarissa C. Pasiliao; Mahbuba Rahman; Jianhua Ren; Yaling Yin; Samuel Gusscott; Sophie Vacher; Andrew P. Weng; Hagen F. Kennecke; Ivan Bièche; David F. Schaeffer; Donald T. Yapp; Isabella T. Tai
Author Choice
Decitabine Priming Enhances Mucin 1 Inhibition Mediated Disruption of Redox Homeostasis in Cutaneous T-Cell Lymphoma
Salvia Jain; Abigail Washington; Rebecca Karp Leaf; Parul Bhargava; Rachael A. Clark; Thomas S. Kupper; Dina Stroopinsky; Athalia Pyzer; Leandra Cole; Myrna Nahas; Arie Apel; Jacalyn Rosenblatt; Jon Arnason; Donald Kufe; David Avigan
Companion Diagnostics and Cancer Biomarkers
Author Choice
Modulation of Plasma Metabolite Biomarkers of the MAPK Pathway with MEK Inhibitor RO4987655: Pharmacodynamic and Predictive Potential in Metastatic Melanoma
Joo Ern Ang; Akos Pal; Yasmin J. Asad; Alan T. Henley; Melanie Valenti; Gary Box; Alexis de haven Brandon; Victoria L. Revell; Debra J. Skene; Miro Venturi; Ruediger Rueger; Valerie Meresse; Suzanne A. Eccles; Johann S. de Bono; Stanley B. Kaye; Paul Workman; Udai Banerji; Florence I. Raynaud
Letter to the Editor
Retraction
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