Highlights of This Issue 1623

REVIEW

1625 PET Imaging of Receptor Tyrosine Kinases inCancerWeijun Wei, Dalong Ni, Emily B. Ehlerding,Quan-Yong Luo, and Weibo Cai

SMALL MOLECULE THERAPEUTICS

1637 Orally Bioavailable and Blood–Brain Barrier-Penetrating ATM Inhibitor (AZ32)Radiosensitizes Intracranial Gliomas in MiceJeremy Karlin, Jasmine Allen, Syed F. Ahmad,Gareth Hughes, Victoria Sheridan, Rajesh Odedra,Paul Farrington, Elaine B. Cadogan, Lucy C. Riches,Antonio Garcia-Trinidad, Andrew G. Thomason,Bhavika Patel, Jennifer Vincent, Alan Lau, Kurt G. Pike,Thomas A. Hunt, Amrita Sule, Nicholas C.K. Valerie,Laura Biddlestone-Thorpe, Jenna Kahn, Jason M. Beckta,Nitai Mukhopadhyay, Bernard Barlaam,Sebastien L. Degorce, Jason Kettle, Nicola Colclough,Joanne Wilson, Aaron Smith, Ian P. Barrett, Li Zheng,Tianwei Zhang, Yingchun Wang, Kan Chen, Martin Pass,Stephen T. Durant, and Kristoffer Valerie

1648 TAS6417, A Novel EGFR Inhibitor TargetingExon 20 Insertion MutationsShinichi Hasako, Miki Terasaka, Naomi Abe, Takao Uno,Hirokazu Ohsawa, Akihiro Hashimoto, Ryoto Fujita,Kenji Tanaka, Takashige Okayama, Renu Wadhwa,Kazutaka Miyadera, Yoshimi Aoyagi, Kazuhiko Yonekura,and Kenichi Matsuo

1659 The Protein Tyrosine Phosphatase Activity ofEyes Absent Contributes to Tumor Angiogenesisand Tumor GrowthYuhua Wang, Ram Naresh Pandey, Stephen Riffle,Hemabindu Chintala, Kathryn A. Wikenheiser-Brokamp,and Rashmi S. Hegde

1670 The ATR Inhibitor AZD6738 Synergizes withGemcitabine In Vitro and In Vivo to InducePancreatic Ductal Adenocarcinoma RegressionYann Wallez, Charles R. Dunlop, Timothy Isaac Johnson,Siang-Boon Koh, Chiara Fornari, James W.T. Yates,Sandra Bernaldo de Quirós Fern�andez, Alan Lau,Frances M. Richards, and Duncan I. Jodrell

1683 TAS-114, a First-in-Class Dual dUTPase/DPDInhibitor, Demonstrates Potential to ImproveTherapeutic Efficacy of Fluoropyrimidine-BasedChemotherapyWakako Yano, Tatsushi Yokogawa, Takeshi Wakasa,Keisuke Yamamura, Akio Fujioka, Kunihiro Yoshisue,Eiji Matsushima, Seiji Miyahara, Hitoshi Miyakoshi,Junko Taguchi, Khoon Tee Chong, Yayoi Takao,Masayoshi Fukuoka, and Kenichi Matsuo

1694 Novel Fluoroindenoisoquinoline Non-Camptothecin Topoisomerase I InhibitorsLaetitia Marzi, Keli Agama, Junko Murai,Simone Difilippantonio, Amy James, Cody J. Peer,William D. Figg, Daniel Beck, Mohamed S.A. Elsayed,Mark Cushman, and Yves Pommier

1705 Antileukemic Efficacy of BET Inhibitor in aPreclinical Mouse Model of MLL-AF4þ Infant ALLMichela Bardini, Luca Trentin, Francesca Rizzo,Margherita Vieri, AngelaM. Savino, Patricia Garrido Castro,Grazia Fazio, Eddy H.J. Van Roon, Mark Kerstjens,Nicholas Smithers, Rab K. Prinjha, Geertruy Te Kronnie,Giuseppe Basso, Ronald W. Stam, Rob Pieters,Andrea Biondi, and Gianni Cazzaniga

1717 The XPO1 Inhibitor Selinexor Inhibits Translationand Enhances the Radiosensitivity ofGlioblastoma Cells Grown In Vitro and In VivoAmy Wahba, Barbara H. Rath, John W. O'Neill,Kevin Camphausen, and Philip J. Tofilon

1727 Synthetic Lethal Strategy Identifies a Potent andSelective TTK and CLK1/2 Inhibitor for Treatmentof Triple-Negative Breast Cancer with aCompromised G1–S CheckpointDan Zhu, Shuichan Xu, Gordafaried Deyanat-Yazdi,Sophie X. Peng, Leo A. Barnes, Rama Krishna Narla,Tam Tran, David Mikolon, Yuhong Ning, Tao Shi,Ning Jiang, Heather K. Raymon, Jennifer R. Riggs, andJohn F. Boylan

August 2018 � Volume 17 � Number 8

Molecular Cancer Therapeutics

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LARGE MOLECULE THERAPEUTICS

1739 Preclinical Development of a Bispecific Antibodythat Safely and Effectively Targets CD19 andCD47 for the Treatment of B-Cell Lymphomaand LeukemiaVanessa Buatois, Zo€e Johnson, Susana Salgado-Pires,Anne Papaioannou, Eric Hatterer, Xavier Chauchet,Francoise Richard, Leticia Barba, Bruno Daubeuf,Laura Cons, Lucile Broyer, Matilde D'Asaro,Thomas Matthes, Simon LeGallou, Thierry Fest,Karin Tarte, Robert K. Clarke Hinojosa,Eul�alia Genesc�a Ferrer, Jos�e María Ribera, Aditi Dey,Katharine Bailey, Adele K. Fielding, Linda Eissenberg,Julie Ritchey, Michael Rettig, John F. DiPersio,Marie H. Kosco-Vilbois, Krzysztof Masternak,Nicolas Fischer, Limin Shang, and Walter G. Ferlin

1752 Glucuronide-Linked Antibody–TubulysinConjugates Display Activity in MDRþ andHeterogeneous Tumor ModelsPatrick J. Burke, Joseph Z. Hamilton, Thomas A. Pires,Holden W.H. Lai, Christopher I. Leiske,Kim K. Emmerton, Andrew B. Waight, Peter D. Senter,Robert P. Lyon, and Scott C. Jeffrey

1761 Development of MGD007, a gpA33 xCD3-Bispecific DART Protein for T-CellImmunotherapy of Metastatic Colorectal CancerPaul A. Moore, Kalpana Shah, Yinhua Yang,Ralph Alderson, Penny Roberts, Vatana Long,Daorong Liu, Jonathan C. Li, Steve Burke,Valentina Ciccarone, Hua Li, Claudia B. Fieger,Jeff Hooley, Ann Easton, Monica Licea, Sergey Gorlatov,Kathy L. King, Peter Young, Arash Adami, Deryk Loo,Gurunadh R. Chichili, Liqin Liu, Douglas H. Smith,Jennifer G. Brown, Francine Z. Chen, Scott Koenig,Jennie Mather, Ezio Bonvini, and Syd Johnson

1773 A Raf-Competitive K-Ras Binder Can Fail toFunctionally Antagonize SignalingMonique J. Kauke, Alison W. Tisdale, Ryan L. Kelly,Christian J. Braun,Michael T. Hemann, and K.DaneWittrup

CANCER BIOLOGY AND TRANSLATIONALSTUDIES

1781 Targeting the Mevalonate Pathway SuppressesVHL-Deficient CC-RCC through anHIF-Dependent MechanismJordan M. Thompson, Alejandro Alvarez,Monika K. Singha, Matthew W. Pavesic, Quy H. Nguyen,Luke J. Nelson, David A. Fruman, andOlga V. Razorenova

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A Lewis lung carcinoma xenograft tumor section was co-stained with the endothelial markerendomucin, and the proliferation marker Ki-67. These rapidly growing tumors arecharacterized by high endothelial and tumor cell proliferation in vascular hotspots. In thisstudy, loss of the EYA3 tyrosine phosphatase in either host endothelial cells or tumor cellsattenuated tumor growth. Loss of endothelial EYA3 reduced tumor angiogenesis while loss oftumor cell EYA3 reduced cell proliferation and survival. Key – Green: endomucin-positiveendothelial cells; red: Ki-67 positive proliferating cells; blue: DAPI-stained nuclei.

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2018;17:1623-1792. Mol Cancer Ther     17 (8)

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