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1 October 2016
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Cover Image
ABOUT THE COVER
A liposomal platform encapsulating both the third generation P-gp inhibitor tariquidar and paclitaxel was developed to overcome paclitaxel resistance in ovarian cancer cells. Liposomal paclitaxel-treated cells had a diffuse pattern of β-tubulin expression (shown in green). Treatment with liposomal tariquidar/paclitaxel resulted in cell rounding and ring-like β-tubulin formations around the nucleus. The liposomal encapsulated tariquidar and paclitaxel synergistically inhibited cell viability, blocked proliferation, and caused G2–M arrest in paclitaxel-resistant ovarian cancer cell lines. For details, see the article by Zhang, Sriraman, and colleagues on page 2282. - PDF Icon PDF LinkTable of Contents
ISSN 1535-7163
EISSN 1538-8514
Highlights
Small Molecule Therapeutics
Debio 0617B Inhibits Growth of STAT3-Driven Solid Tumors through Combined Inhibition of JAK, SRC, and Class III/V Receptor Tyrosine Kinases
Maximilien Murone; Anne Vaslin Chessex; Antoine Attinger; Raghuveer Ramachandra; Shankar J. Shetty; Girish Daginakatte; Saumitra Sengupta; Sivapriya Marappan; Samiulla Dhodheri; Stefania Rigotti; Yogeshwar Bachhav; Silvano Brienza; Peter Traxler; Marc Lang; Michel Aguet; Vincent Zoete; Olivier Michielin; Courtney Nicholas; Faye M. Johnson; Murali Ramachandra; Andres McAllister
Author Choice
Characterization of LY3023414, a Novel PI3K/mTOR Dual Inhibitor Eliciting Transient Target Modulation to Impede Tumor Growth
Michele C. Smith; Mary M. Mader; James A. Cook; Philip Iversen; Rose Ajamie; Everett Perkins; Laura Bloem; Yvonne Y. Yip; David A. Barda; Philip P. Waid; Douglas J. Zeckner; Debra A. Young; Manuel Sanchez-Felix; Gregory P. Donoho; Volker Wacheck
Trabectedin Is Active against Malignant Pleural Mesothelioma Cell and Xenograft Models and Synergizes with Chemotherapy and Bcl-2 Inhibition In Vitro
Mir A. Hoda; Christine Pirker; Yawen Dong; Karin Schelch; Petra Heffeter; Kushtrim Kryeziu; Sushilla van Schoonhoven; Thomas Klikovits; Viktoria Laszlo; Anita Rozsas; Judit Ozsvar; Walter Klepetko; Balazs Döme; Michael Grusch; Balazs Hegedüs; Walter Berger
Inhibition of Breast Cancer Metastasis by Presurgical Treatment with an Oral Matrix Metalloproteinase Inhibitor: A Preclinical Proof-of-Principle Study
Arthur Winer; Maxwell Janosky; Beth Harrison; Judy Zhong; Dariush Moussai; Pinar Siyah; Nina Schatz-Siemers; Jennifer Zeng; Sylvia Adams; Paolo Mignatti
Pharmacological Profile of BI 847325, an Orally Bioavailable, ATP-Competitive Inhibitor of MEK and Aurora Kinases
Patrizia Sini; Ulrich Gürtler; Stephan K. Zahn; Christoph Baumann; Dorothea Rudolph; Rosa Baumgartinger; Eva Strauss; Christian Haslinger; Ulrike Tontsch-Grunt; Irene C. Waizenegger; Flavio Solca; Gerd Bader; Andreas Zoephel; Matthias Treu; Ulrich Reiser; Pilar Garin-Chesa; Guido Boehmelt; Norbert Kraut; Jens Quant; Günther R. Adolf
Author Choice
Lurbinectedin Specifically Triggers the Degradation of Phosphorylated RNA Polymerase II and the Formation of DNA Breaks in Cancer Cells
Gema Santamaría Nuñez; Carlos Mario Genes Robles; Christophe Giraudon; Juan Fernando Martínez-Leal; Emmanuel Compe; Frédéric Coin; Pablo Aviles; Carlos María Galmarini; Jean-Marc Egly
Large Molecule Therapeutics
Cancer Biology and Signal Transduction
FLIP: A Targetable Mediator of Resistance to Radiation in Non–Small Cell Lung Cancer
Kylie A. McLaughlin; Zsuzsanna Nemeth; Conor A. Bradley; Luke Humphreys; Izabela Stasik; Catherine Fenning; Joanna Majkut; Catherine Higgins; Nyree Crawford; Caitriona Holohan; Patrick G. Johnston; Timothy Harrison; Gerard G. Hanna; Karl T. Butterworth; Kevin M. Prise; Daniel B. Longley
Author Choice
The Tyrosine Kinase Inhibitor Imatinib Augments Extracellular Fluid Exchange and Reduces Average Collagen Fibril Diameter in Experimental Carcinoma
P. Olof Olsson; Renata Gustafsson; René in 't Zandt; Tomas Friman; Marco Maccarana; Emil Tykesson; Åke Oldberg; Kristofer Rubin; Sebastian Kalamajski
Author Choice
TP53 Alterations Correlate with Response to VEGF/VEGFR Inhibitors: Implications for Targeted Therapeutics
Jennifer J. Wheler; Filip Janku; Aung Naing; Yali Li; Bettzy Stephen; Ralph Zinner; Vivek Subbiah; Siqing Fu; Daniel Karp; Gerald S. Falchook; Apostolia M. Tsimberidou; Sarina Piha-Paul; Roosevelt Anderson; Danxia Ke; Vincent Miller; Roman Yelensky; J. Jack Lee; David Hong; Razelle Kurzrock
Companion Diagnostics and Cancer Biomarkers
Author Choice
EGFR and RB1 as Dual Biomarkers in HPV-Negative Head and Neck Cancer
Tim N. Beck; Rachel Georgopoulos; Elena I. Shagisultanova; David Sarcu; Elizabeth A. Handorf; Cara Dubyk; Miriam N. Lango; John A. Ridge; Igor Astsaturov; Ilya G. Serebriiskii; Barbara A. Burtness; Ranee Mehra; Erica A. Golemis
Models and Technologies
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