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1 December 2011
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Cover Image
Cover Image
Human lung microvascular cells cocultured with human diploid fibroblasts form extensive networks of tubules in response to VEGF that can be visualized by immunostaining for CD31, an endothelial cell marker. In the presence of cabozantinib (XL184), a small-molecule kinase inhibitor with potent activity toward MET and VEGF receptor 2, it was found that tubule formation was inhibited in the absence of cytotoxicity. Similarly, cabozantinib inhibited tubule formation in response to conditioned media derived from tumor cell cultures, suggesting that secreted tumor cell-derived proangiogenic growth factors are unable to circumvent inhibition of tubule formation by cabozantinib. For details, see article by Yakes and colleagues on page 2298. - PDF Icon PDF LinkTable of Contents
ISSN 1535-7163
EISSN 1538-8514
Highlights
Review
Therapeutic Discovery
Characterization of the Cellular and Antitumor Effects of MPI-0479605, a Small-Molecule Inhibitor of the Mitotic Kinase Mps1
Keith D. Tardif; Aaron Rogers; Jared Cassiano; Bruce L. Roth; Daniel M. Cimbora; Rena McKinnon; Ashley Peterson; Thomas B. Douce; Rosann Robinson; Irene Dorweiler; Thaylon Davis; Mark A. Hess; Kirill Ostanin; Damon I. Papac; Vijay Baichwal; Ian McAlexander; J. Adam Willardsen; Michael Saunders; Hoarau Christophe; D. Vijay Kumar; Daniel A. Wettstein; Robert O. Carlson; Brandi L. Williams
Preclinical Development
Cabozantinib (XL184), a Novel MET and VEGFR2 Inhibitor, Simultaneously Suppresses Metastasis, Angiogenesis, and Tumor Growth
F. Michael Yakes; Jason Chen; Jenny Tan; Kyoko Yamaguchi; Yongchang Shi; Peiwen Yu; Fawn Qian; Felix Chu; Frauke Bentzien; Belinda Cancilla; Jessica Orf; Andrew You; A. Douglas Laird; Stefan Engst; Lillian Lee; Justin Lesch; Yu-Chien Chou; Alison H. Joly
Reduced Expression of the Androgen Receptor by Third Generation of Antisense Shows Antitumor Activity in Models of Prostate Cancer
Yixian Zhang; Stephen Castaneda; Melissa Dumble; Maoliang Wang; Mary Mileski; Zhengxing Qu; Steven Kim; Victoria Shi; Patricia Kraft; Ying Gao; Jenny Pak; Puja Sapra; Raj Bandaru; Hong Zhao; Robert L. Vessella; Ivan D. Horak; Lee M. Greenberger
The Clinically Active PARP Inhibitor AG014699 Ameliorates Cardiotoxicity but Does Not Enhance the Efficacy of Doxorubicin, despite Improving Tumor Perfusion and Radiation Response in Mice
Majid Ali; Marzieh Kamjoo; Huw D. Thomas; Suzanne Kyle; Ivanda Pavlovska; Muhammed Babur; Brian A. Telfer; Nicola J. Curtin; Kaye J. Williams
The Bcl-2/Bcl-XL/Bcl-w Inhibitor, Navitoclax, Enhances the Activity of Chemotherapeutic Agents In Vitro and In Vivo
Jun Chen; Sha Jin; Vivek Abraham; Xiaoli Huang; Bernard Liu; Michael J. Mitten; Paul Nimmer; Xiaoyu Lin; Morey Smith; Yu Shen; Alexander R. Shoemaker; Stephen K. Tahir; Haichao Zhang; Scott L. Ackler; Saul H. Rosenberg; Heather Maecker; Deepak Sampath; Joel D. Leverson; Chris Tse; Steven W. Elmore
Dual Inhibition of Tumor Energy Pathway by 2-Deoxyglucose and Metformin Is Effective against a Broad Spectrum of Preclinical Cancer Models
Jae-Ho Cheong; Eun Sung Park; Jiyong Liang; Jennifer B. Dennison; Dimitra Tsavachidou; Catherine Nguyen-Charles; Kwai Wa Cheng; Hassan Hall; Dong Zhang; Yiling Lu; Murali Ravoori; Vikas Kundra; Jaffer Ajani; Ju-Seog Lee; Waun Ki Hong; Gordon B. Mills
Death Receptor Pathway Activation and Increase of ROS Production by the Triple Epigenetic Inhibitor UVI5008
Angela Nebbioso; Raquel Pereira; Harshal Khanwalkar; Filomena Matarese; José García-Rodríguez; Marco Miceli; Colin Logie; Valerie Kedinger; Felicetto Ferrara; Hendrik G. Stunnenberg; Angel R. de Lera; Hinrich Gronemeyer; Lucia Altucci
Molecular Medicine in Practice
GDC-0980 Is a Novel Class I PI3K/mTOR Kinase Inhibitor with Robust Activity in Cancer Models Driven by the PI3K Pathway
Jeffrey J. Wallin; Kyle A. Edgar; Jane Guan; Megan Berry; Wei Wei Prior; Leslie Lee; John D. Lesnick; Cristina Lewis; Jim Nonomiya; Jodie Pang; Laurent Salphati; Alan G. Olivero; Daniel P. Sutherlin; Carol O'Brien; Jill M. Spoerke; Sonal Patel; Letitia Lensun; Robert Kassees; Leanne Ross; Mark R. Lackner; Deepak Sampath; Marcia Belvin; Lori S. Friedman
Reviewers
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