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1 December 2017
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Cover Image
ABOUT THE COVER
Sym015 is a mixture of the two anti-MET monoclonal antibodies, Hu9006 and Hu9338. The frontpage shows a space filling model of the Sym015 epitopes on the structure of the HGF-β:MET complex. Mutational analysis of the MET SEMA domain identified residues 89-162 in blade 2 as the epitope for Hu9338 (blue) and residues 171-233 in blade 3 as the epitope for Hu9006 (green). SEMA α, SEMA β and PSI domains are show in orange, cyan and red, respectively. HGF is shown in grey. - PDF Icon PDF LinkTable of Contents
- PDF Icon PDF LinkEditorial Board
ISSN 1535-7163
EISSN 1538-8514
Highlights
Commentary
Review
Small Molecule Therapeutics
Author Choice
The Irreversible Covalent Fibroblast Growth Factor Receptor Inhibitor PRN1371 Exhibits Sustained Inhibition of FGFR after Drug Clearance
Eleni Venetsanakos; Ken A. Brameld; Vernon T. Phan; Erik Verner; Timothy D. Owens; Yan Xing; Danny Tam; Jacob LaStant; Kwan Leung; Dane E. Karr; Ronald J. Hill; Mary E. Gerritsen; David M. Goldstein; Jens Oliver Funk; J. Michael Bradshaw
Author Choice
Discovery of a Highly Selective NAMPT Inhibitor That Demonstrates Robust Efficacy and Improved Retinal Toxicity with Nicotinic Acid Coadministration
Genshi Zhao; Colin F. Green; Yu-Hua Hui; Lourdes Prieto; Robert Shepard; Sucai Dong; Tao Wang; Bo Tan; Xueqian Gong; Lisa Kays; Robert L. Johnson; Wenjuan Wu; Shobha Bhattachar; Miriam Del Prado; James R. Gillig; Maria-Carmen Fernandez; Ken D. Roth; Sean Buchanan; Ming-Shang Kuo; Sandaruwan Geeganage; Timothy P. Burkholder
The Combination of Metformin and Valproic Acid Induces Synergistic Apoptosis in the Presence of p53 and Androgen Signaling in Prostate Cancer
Linh N.K. Tran; Ganessan Kichenadasse; Lisa M. Butler; Margaret M. Centenera; Katherine L. Morel; Rebecca J. Ormsby; Michael Z. Michael; Karen M. Lower; Pamela J. Sykes
Restricted Delivery of Talazoparib Across the Blood–Brain Barrier Limits the Sensitizing Effects of PARP Inhibition on Temozolomide Therapy in Glioblastoma
Sani H. Kizilbash; Shiv K. Gupta; Kenneth Chang; Ryo Kawashima; Karen E. Parrish; Brett L. Carlson; Katrina K. Bakken; Ann C. Mladek; Mark A. Schroeder; Paul A. Decker; Gaspar J. Kitange; Yuqiao Shen; Ying Feng; Andrew A. Protter; William F. Elmquist; Jann N. Sarkaria
Pharmacological Dual Inhibition of Tumor and Tumor-Induced Functional Limitations in a Transgenic Model of Breast Cancer
Ruizhong Wang; Poornima Bhat-Nakshatri; Maria B. Padua; Mayuri S Prasad; Manjushree Anjanappa; Max Jacobson; Courtney Finnearty; Victoria Sefcsik; Kyle McElyea; Rachael Redmond; George Sandusky; Narsimha Penthala; Peter A Crooks; Jianguo Liu; Teresa Zimmers; Harikrishna Nakshatri
Large Molecule Therapeutics
Simultaneous Targeting of Two Distinct Epitopes on MET Effectively Inhibits MET- and HGF-Driven Tumor Growth by Multiple Mechanisms
Michael M. Grandal; Serhiy Havrylov; Thomas T. Poulsen; Klaus Koefoed; Anna Dahlman; Gunther R. Galler; Paolo Conrotto; Sara Collins; Karsten W. Eriksen; Dafna Kaufman; George F.Vande Woude; Helle J. Jacobsen; Ivan D. Horak; Michael Kragh; Johan Lantto; Thomas Bouquin; Morag Park; Mikkel W. Pedersen
Cancer Biology and Translational Studies
CRISPR Genome-Wide Screening Identifies Dependence on the Proteasome Subunit PSMC6 for Bortezomib Sensitivity in Multiple Myeloma
Chang-Xin Shi; K. Martin Kortüm; Yuan Xiao Zhu; Laura A. Bruins; Patrick Jedlowski; Patrick G. Votruba; Moulun Luo; Robert A. Stewart; Jonathan Ahmann; Esteban Braggio; A. Keith Stewart
CCR5-Dependent Homing of T Regulatory Cells to the Tumor Microenvironment Contributes to Skin Squamous Cell Carcinoma Development
Carine Ervolino de Oliveira; Thaís Helena Gasparoto; Claudia Ramos Pinheiro; Nádia Ghinelli Amôr; Maria Renata Sales Nogueira; Ramon Kaneno; Gustavo Pompermaier Garlet; Vanessa Soares Lara; João Santana Silva; Karen Angélica Cavassani; Ana Paula Campanelli
Inhibition of the Receptor Tyrosine Kinase AXL Restores Paclitaxel Chemosensitivity in Uterine Serous Cancer
Marguerite L. Palisoul; Jeanne M. Quinn; Emily Schepers; Ian S. Hagemann; Lei Guo; Kelsey Reger; Andrea R. Hagemann; Carolyn K. McCourt; Premal H. Thaker; Matthew A. Powell; David G. Mutch; Katherine C. Fuh
Companion Diagnostic, Pharmacogenomic, and Cancer Biomarkers
Models and Technologies
A Murine Model for Quantitative, Real-Time Evaluation of Convection-Enhanced Delivery (RT-CED) Using an 18[F]-Positron Emitting, Fluorescent Derivative of Dasatinib
Melinda Wang; Harikrishna Kommidi; Umberto Tosi; Hua Guo; Zhiping Zhou; Melanie E. Schweitzer; Linda Y. Wu; Ranjodh Singh; Shengqi Hou; Benedict Law; Richard Ting; Mark M. Souweidane
Acknowledgment to Reviewers
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