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Molecular Cancer Therapeutics
Molecular Cancer Therapeutics
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Table of Contents

Highlights

  • Highlights
    Selected Articles from This Issue
    Mol Cancer Ther February 1 2020 19 (2) 323-323;

Small Molecule Therapeutics

  • Small Molecule Therapeutics | AuthorChoice
    ERK Inhibitor LY3214996 Targets ERK Pathway–Driven Cancers: A Therapeutic Approach Toward Precision Medicine
    Shripad V. Bhagwat, William T. McMillen, Shufen Cai, Baohui Zhao, Matthew Whitesell, Weihua Shen, Lisa Kindler, Robert S. Flack, Wenjuan Wu, Bryan Anderson, Yan Zhai, Xiu-Juan Yuan, Meghann Pogue, Robert D. Van Horn, Xi Rao, Denis McCann, Andrew J. Dropsey, Jason Manro, Jennie Walgren, Eunice Yuen, Michael J. Rodriguez, Gregory D. Plowman, Ramon V. Tiu, Sajan Joseph and Sheng-Bin Peng
    Mol Cancer Ther February 1 2020 19 (2) 325-336; DOI:10.1158/1535-7163.MCT-19-0183

  • Small Molecule Therapeutics | AuthorChoice
    Targeting of β-Catenin Reverses Radioresistance of Cervical Cancer with the PIK3CA-E545K Mutation
    Wei Jiang, Yutuan Wu, Tiancong He, Hanting Zhu, Guihao Ke, Libing Xiang and Huijuan Yang
    Mol Cancer Ther February 1 2020 19 (2) 337-347; DOI:10.1158/1535-7163.MCT-19-0309

  • Small Molecule Therapeutics
    An Orally Available Tubulin Inhibitor, VERU-111, Suppresses Triple-Negative Breast Cancer Tumor Growth and Metastasis and Bypasses Taxane Resistance
    Shanshan Deng, Raisa I. Krutilina, Qinghui Wang, Zongtao Lin, Deanna N. Parke, Hilaire C. Playa, Hao Chen, Duane D. Miller, Tiffany N. Seagroves and Wei Li
    Mol Cancer Ther February 1 2020 19 (2) 348-363; DOI:10.1158/1535-7163.MCT-19-0536

  • Small Molecule Therapeutics
    Therapeutic Targeting of MDR1 Expression by RORγ Antagonists Resensitizes Cross-Resistant CRPC to Taxane via Coordinated Induction of Cell Death Programs
    Yongqiang Wang, Zenghong Huang, Christopher Z. Chen, Chengfei Liu, Christopher P. Evans, Allen C. Gao, Fangjian Zhou and Hong-Wu Chen
    Mol Cancer Ther February 1 2020 19 (2) 364-374; DOI:10.1158/1535-7163.MCT-19-0327

  • Small Molecule Therapeutics
    A Potent Blood–Brain Barrier-Permeable Mutant IDH1 Inhibitor Suppresses the Growth of Glioblastoma with IDH1 Mutation in a Patient-Derived Orthotopic Xenograft Model
    Yukino Machida, Makoto Nakagawa, Hironori Matsunaga, Masayuki Yamaguchi, Yoko Ogawara, Yutaka Shima, Kazutsune Yamagata, Takuo Katsumoto, Ayuna Hattori, Masato Itoh, Takahiko Seki, Yumi Nishiya, Koichi Nakamura, Kanae Suzuki, Tomoki Imaoka, Daichi Baba, Makoto Suzuki, Oltea Sampetrean, Hideyuki Saya, Koichi Ichimura and Issay Kitabayashi
    Mol Cancer Ther February 1 2020 19 (2) 375-383; DOI:10.1158/1535-7163.MCT-18-1349

  • Small Molecule Therapeutics
    Ibrutinib Potentiates Antihepatocarcinogenic Efficacy of Sorafenib by Targeting EGFR in Tumor Cells and BTK in Immune Cells in the Stroma
    Cho-Hao Lin, Khadija H. Elkholy, Nissar A. Wani, Ding Li, Peng Hu, Juan M. Barajas, Lianbo Yu, Xiaoli Zhang, Samson T. Jacob, Wasif N. Khan, Xue-Feng Bai, Anne M. Noonan and Kalpana Ghoshal
    Mol Cancer Ther February 1 2020 19 (2) 384-396; DOI:10.1158/1535-7163.MCT-19-0135

  • Small Molecule Therapeutics
    The Novel Glutamine Antagonist Prodrug JHU395 Has Antitumor Activity in Malignant Peripheral Nerve Sheath Tumor
    Kathryn M. Lemberg, Liang Zhao, Ying Wu, Vijayabhaskar Veeravalli, Jesse Alt, Joanna Marie H. Aguilar, Ranjeet P. Dash, Jenny Lam, Lukáš Tenora, Chabely Rodriguez, Michael T. Nedelcovych, Cory Brayton, Pavel Majer, Jaishri O. Blakeley, Rana Rais and Barbara S. Slusher
    Mol Cancer Ther February 1 2020 19 (2) 397-408; DOI:10.1158/1535-7163.MCT-19-0319

  • Small Molecule Therapeutics
    Selective PRMT5 Inhibitors Suppress Human CD8+ T Cells by Upregulation of p53 and Impairment of the AKT Pathway Similar to the Tumor Metabolite MTA
    Carolin Dorothea Strobl, Stefanie Schaffer, Tabea Haug, Simon Völkl, Katrin Peter, Katrin Singer, Martin Böttcher, Dimitrios Mougiakakos, Andreas Mackensen and Michael Aigner
    Mol Cancer Ther February 1 2020 19 (2) 409-419; DOI:10.1158/1535-7163.MCT-19-0189

  • Small Molecule Therapeutics
    A Novel Sulforaphane-Regulated Gene Network in Suppression of Breast Cancer–Induced Osteolytic Bone Resorption
    Subrata K. Pore, Eun-Ryeong Hahm, Su-Hyeong Kim, Krishna B. Singh, Lea Nyiranshuti, Joseph D. Latoche, Carolyn J. Anderson, Juraj Adamik, Deborah L. Galson, Kurt R. Weiss, Rebecca J. Watters, Boeun Lee, Prashant N. Kumta and Shivendra V. Singh
    Mol Cancer Ther February 1 2020 19 (2) 420-431; DOI:10.1158/1535-7163.MCT-19-0611

  • Small Molecule Therapeutics
    The Existence of MTH1-independent 8-oxodGTPase Activity in Cancer Cells as a Compensatory Mechanism against On-target Effects of MTH1 Inhibitors
    Govindi J. Samaranayake, Clara I. Troccoli, Ling Zhang, Mai Huynh, Christina J. Jayaraj, Debin Ji, Lisa McPherson, Yoshiyuki Onishi, Dao M. Nguyen, David J. Robbins, Mahsa Karbaschi, Marcus S. Cooke, Antonio Barrientos, Eric T. Kool and Priyamvada Rai
    Mol Cancer Ther February 1 2020 19 (2) 432-446; DOI:10.1158/1535-7163.MCT-19-0437

  • Small Molecule Therapeutics
    Development of a Novel Multi-Isoform ALDH Inhibitor Effective as an Antimelanoma Agent
    Saketh S. Dinavahi, Raghavendra Gowda, Krishne Gowda, Christopher G. Bazewicz, Venkat R. Chirasani, Madhu Babu Battu, Arthur Berg, Nikolay V. Dokholyan, Shantu Amin and Gavin P. Robertson
    Mol Cancer Ther February 1 2020 19 (2) 447-459; DOI:10.1158/1535-7163.MCT-19-0360

  • Small Molecule Therapeutics
    A Phase I Study of LY3009120, a Pan-RAF Inhibitor, in Patients with Advanced or Metastatic Cancer
    Ryan J. Sullivan, Antoine Hollebecque, Keith T. Flaherty, Geoffrey I. Shapiro, Jordi Rodon Ahnert, Michael J. Millward, Wei Zhang, Ling Gao, Amanda Sykes, Melinda D. Willard, Danni Yu, Andrew E. Schade, KrisAnne Crowe, Daniel L. Flynn, Michael D. Kaufman, James R. Henry, Sheng-Bin Peng, Karim A. Benhadji, Ilaria Conti, Michael S. Gordon, Ramon V. Tiu and David S. Hong
    Mol Cancer Ther February 1 2020 19 (2) 460-467; DOI:10.1158/1535-7163.MCT-19-0681

  • Small Molecule Therapeutics | AuthorChoice
    On-Target Pharmacodynamic Activity of the PI3K Inhibitor Copanlisib in Paired Biopsies from Patients with Malignant Lymphoma and Advanced Solid Tumors
    Franck Morschhauser, Jean-Pascal Machiels, Gilles Salles, Sylvie Rottey, Simon A.J. Rule, David Cunningham, Frederic Peyrade, Christophe Fruchart, Hendrik-Tobias Arkenau, Isabelle Genvresse, Li Liu, Karl Köchert, Kui Shen, Christoph Kneip, Carol E. Peña, Joachim Grevel, Jun Zhang, Galia Cisternas, Susanne Reschke, Camille Granvil and Ahmad Awada
    Mol Cancer Ther February 1 2020 19 (2) 468-478; DOI:10.1158/1535-7163.MCT-19-0466

  • Small Molecule Therapeutics | AuthorChoice
    Inhibition of Y Box Binding Protein 1 Suppresses Cell Growth and Motility in Colorectal Cancer
    Areumnuri Kim, Sehwan Shim, Young-heon Kim, Min-Jung Kim, Sunhoo Park and Jae Kyung Myung
    Mol Cancer Ther February 1 2020 19 (2) 479-489; DOI:10.1158/1535-7163.MCT-19-0265

Large Molecule Therapeutics

  • Large Molecule Therapeutics
    10D1F, an Anti-HER3 Antibody That Uniquely Blocks the Receptor Heterodimerization Interface, Potently Inhibits Tumor Growth Across a Broad Panel of Tumor Models
    Dipti Thakkar, Vicente Sancenon, Marvin M. Taguiam, Siyu Guan, Zhihao Wu, Eric Ng, Konrad H. Paszkiewicz, Piers J. Ingram and Jerome D. Boyd-Kirkup
    Mol Cancer Ther February 1 2020 19 (2) 490-501; DOI:10.1158/1535-7163.MCT-19-0515

  • Large Molecule Therapeutics | AuthorChoice
    Anticancer Activity of ZnO Nanoparticles against Human Small-Cell Lung Cancer in an Orthotopic Mouse Model
    Ryosuke Tanino, Yoshihiro Amano, Xuexia Tong, Rong Sun, Yukari Tsubata, Mamoru Harada, Yasuhisa Fujita and Takeshi Isobe
    Mol Cancer Ther February 1 2020 19 (2) 502-512; DOI:10.1158/1535-7163.MCT-19-0018

  • Large Molecule Therapeutics
    Toxicology and Pharmacokinetic Studies in Mice and Nonhuman Primates of the Nontoxic, Efficient, Targeted Hexameric FasL: CTLA4-FasL
    Efi Makdasi, Shira Amsili, Alexandra Aronin, Tatyana B. Prigozhina, Kobi Tzdaka, Yosi Meir Gozlan, Liat Ben Gigi–Tamir, Jitka Yehudith Sagiv, Fanny Shkedy, Noam Shani, Mark L. Tykocinski and Michal Dranitzki Elhalel
    Mol Cancer Ther February 1 2020 19 (2) 513-524; DOI:10.1158/1535-7163.MCT-19-0558

Cancer Biology and Translational Studies

  • Cancer Biology and Translational Studies | AuthorChoice
    Dual-Mechanism ERK1/2 Inhibitors Exploit a Distinct Binding Mode to Block Phosphorylation and Nuclear Accumulation of ERK1/2
    Andrew M. Kidger, Joanne M. Munck, Harpreet K. Saini, Kathryn Balmanno, Emma Minihane, Aurelie Courtin, Brent Graham, Marc O'Reilly, Richard Odle and Simon J. Cook
    Mol Cancer Ther February 1 2020 19 (2) 525-539; DOI:10.1158/1535-7163.MCT-19-0505

  • Cancer Biology and Translational Studies
    Exportin 1 Inhibition Induces Nerve Growth Factor Receptor Expression to Inhibit the NF-κB Pathway in Preclinical Models of Pediatric High-Grade Glioma
    John A. DeSisto, Patrick Flannery, Rakeb Lemma, Amrita Pathak, Shelby Mestnik, Natalie Philips, Natalie J. Bales, Trinayan Kashyap, Erin Moroze, Sujatha Venkataraman, Andrew L. Kung, Bruce D. Carter, Yosef Landesman, Rajeev Vibhakar and Adam L. Green
    Mol Cancer Ther February 1 2020 19 (2) 540-551; DOI:10.1158/1535-7163.MCT-18-1319

  • Cancer Biology and Translational Studies | AuthorChoice
    Functional Genomic Screen in Mesothelioma Reveals that Loss of Function of BRCA1-Associated Protein 1 Induces Chemoresistance to Ribonucleotide Reductase Inhibition
    Agata Okonska, Saskja Bühler, Vasundhara Rao, Manuel Ronner, Maxime Blijlevens, Ida H. van der Meulen-Muileman, Renee X. de Menezes, Martin Wipplinger, Kathrin Oehl, Egbert F. Smit, Walter Weder, Rolf A. Stahel, Lorenza Penengo, Victor W. van Beusechem and Emanuela Felley-Bosco
    Mol Cancer Ther February 1 2020 19 (2) 552-563; DOI:10.1158/1535-7163.MCT-19-0356

  • Cancer Biology and Translational Studies
    Ceramide–Rubusoside Nanomicelles, a Potential Therapeutic Approach to Target Cancers Carrying p53 Missense Mutations
    Sachin K. Khiste, Zhijun Liu, Kartik R. Roy, Mohammad B. Uddin, Salman B. Hosain, Xin Gu, Sami Nazzal, Ronald A. Hill and Yong-Yu Liu
    Mol Cancer Ther February 1 2020 19 (2) 564-574; DOI:10.1158/1535-7163.MCT-19-0366

  • Cancer Biology and Translational Studies
    Radiation Responses of 2D and 3D Glioblastoma Cells: A Novel, 3D-specific Radioprotective Role of VEGF/Akt Signaling through Functional Activation of NHEJ
    Natividad Gomez-Roman, Ming Y Chong, Sandeep K. Chahal, Seamus P. Caragher, Mark R. Jackson, Katrina H. Stevenson, Sidhartha A. Dongre and Anthony J. Chalmers
    Mol Cancer Ther February 1 2020 19 (2) 575-589; DOI:10.1158/1535-7163.MCT-18-1320

  • Cancer Biology and Translational Studies
    Dual mTORC1/2 Inhibition Sensitizes Testicular Cancer Models to Cisplatin Treatment
    Ximena Rosas-Plaza, Gerda de Vries, Gert Jan Meersma, Albert J.H. Suurmeijer, Jourik A. Gietema, Marcel A.T.M. van Vugt and Steven de Jong
    Mol Cancer Ther February 1 2020 19 (2) 590-601; DOI:10.1158/1535-7163.MCT-19-0449

  • Cancer Biology and Translational Studies
    Amplification of the Mutation-Carrying BRCA2 Allele Promotes RAD51 Loading and PARP Inhibitor Resistance in the Absence of Reversion Mutations
    Pyoung Hwa Park, Tomomi M. Yamamoto, Hua Li, Allen L. Alcivar, Bing Xia, Yifan Wang, Andrea J. Bernhardy, Kristen M. Turner, Andrew V. Kossenkov, Zachary L. Watson, Kian Behbakht, Silvia Casadei, Elizabeth M. Swisher, Paul S. Mischel, Neil Johnson and Benjamin G. Bitler
    Mol Cancer Ther February 1 2020 19 (2) 602-613; DOI:10.1158/1535-7163.MCT-17-0256

  • Cancer Biology and Translational Studies
    Targeting the MET Receptor Tyrosine Kinase as a Strategy for Radiosensitization in Locoregionally Advanced Head and Neck Squamous Cell Carcinoma
    Lluís Nisa, Paola Francica, Roland Giger, Matúš Medo, Olgun Elicin, Manja Friese-Hamim, Claudia Wilm, Christopher Stroh, Beat Bojaxhiu, Aurélie Quintin, Marco D. Caversaccio, Matthias S. Dettmer, Mélanie Buchwalder, Tess M. Brodie, Daniel M. Aebersold, Yitzhak Zimmer, Thomas E. Carey and Michaela Medová
    Mol Cancer Ther February 1 2020 19 (2) 614-626; DOI:10.1158/1535-7163.MCT-18-1274

  • Cancer Biology and Translational Studies
    Rational Combination Therapy for Melanoma with Dinaciclib by Targeting BAK-Dependent Cell Death
    Xiaoou Xu, Shizuka Eshima, Shinichiro Kato, David E. Fisher, Hiroaki Sakurai, Yoshihiro Hayakawa and Satoru Yokoyama
    Mol Cancer Ther February 1 2020 19 (2) 627-636; DOI:10.1158/1535-7163.MCT-19-0451

  • Cancer Biology and Translational Studies
    A Synergistic Anticancer FAK and HDAC Inhibitor Combination Discovered by a Novel Chemical–Genetic High-Content Phenotypic Screen
    John C. Dawson, Bryan Serrels, Adam Byron, Morwenna T. Muir, Ashraff Makda, Amaya García-Muñoz, Alex von Kriegsheim, Daniel Lietha, Neil O. Carragher and Margaret C. Frame
    Mol Cancer Ther February 1 2020 19 (2) 637-649; DOI:10.1158/1535-7163.MCT-19-0330

  • Cancer Biology and Translational Studies | AuthorChoice
    Serum- and Glucocorticoid-inducible Kinase 1 is Essential for Osteoclastogenesis and Promotes Breast Cancer Bone Metastasis
    Zheng Zhang, Qian Xu, Chao Song, Baoguo Mi, Honghua Zhang, Honglei Kang, Huiyong Liu, Yunlong Sun, Jia Wang, Zhuowei Lei, Hanfeng Guan and Feng Li
    Mol Cancer Ther February 1 2020 19 (2) 650-660; DOI:10.1158/1535-7163.MCT-18-0783

  • Cancer Biology and Translational Studies
    CRISPR Screening Identifies WEE1 as a Combination Target for Standard Chemotherapy in Malignant Pleural Mesothelioma
    Duo Xu, Shun-Qing Liang, Haitang Yang, Rémy Bruggmann, Sabina Berezowska, Zhang Yang, Thomas Michael Marti, Sean Ralph Robert Hall, Yanyun Gao, Gregor J. Kocher, Ralph A. Schmid and Ren-Wang Peng
    Mol Cancer Ther February 1 2020 19 (2) 661-672; DOI:10.1158/1535-7163.MCT-19-0724

Companion Diagnostic, Pharmacogenomic, and Cancer Biomarkers

  • Companion Diagnostic, Pharmacogenomic, and Cancer Biomarkers
    PET Imaging of the EPR Effect in Tumor Xenografts Using Small 15 nm Diameter Polyethylene Glycols Labeled with Zirconium-89
    Denis R. Beckford Vera, Shaun D. Fontaine, Henry F. VanBrocklin, Brian R. Hearn, Ralph Reid, Gary W. Ashley and Daniel V. Santi
    Mol Cancer Ther February 1 2020 19 (2) 673-679; DOI:10.1158/1535-7163.MCT-19-0709

  • Companion Diagnostic, Pharmacogenomic, and Cancer Biomarkers | AuthorChoice
    Estrogen Receptor Pathway Activity Score to Predict Clinical Response or Resistance to Neoadjuvant Endocrine Therapy in Primary Breast Cancer
    Márcia A. Inda, Erik J. Blok, Peter J.K. Kuppen, Ayoub Charehbili, Eveline C. den Biezen-Timmermans, Anne van Brussel, Sevgi E. Fruytier, Elma Meershoek-Klein Kranenbarg, Susan Kloet, Bart van der Burg, John W.M. Martens, Andrew H. Sims, Arran K. Turnbull, J. Michael Dixon, Wim Verhaegh, Judith R. Kroep, Cornelis J.H. van de Velde and Anja van de Stolpe
    Mol Cancer Ther February 1 2020 19 (2) 680-689; DOI:10.1158/1535-7163.MCT-19-0318

  • Companion Diagnostic, Pharmacogenomic, and Cancer Biomarkers
    Mutations and Response to Rapalogs in Patients with Metastatic Renal Cell Carcinoma
    Amin H. Nassar, Lana Hamieh, Kathryn P. Gray, Aaron R. Thorner, Andre P. Fay, Kathryn D. Lasseter, Sarah Abou Alaiwi, Pier Vitale Nuzzo, Ronan Flippot, Katherine M. Krajewski, Sabina Signoretti, Toni K. Choueiri and David J. Kwiatkowski
    Mol Cancer Ther February 1 2020 19 (2) 690-696; DOI:10.1158/1535-7163.MCT-19-0642

Models and Technologies

  • Models and Technologies
    Therapeutic Breast Reconstruction Using Gene Therapy–Delivered IFNγ Immunotherapy
    Christopher R. Davis, Peter A. Than, Sacha M.L. Khong, Melanie Rodrigues, Michael W. Findlay, Daniel J. Navarrete, Shadi Ghali, Jayant S. Vaidya and Geoffrey C. Gurtner
    Mol Cancer Ther February 1 2020 19 (2) 697-705; DOI:10.1158/1535-7163.MCT-19-0315

  • Models and Technologies
    Hyaluronidase-Expressing Salmonella Effectively Targets Tumor-Associated Hyaluronic Acid in Pancreatic Ductal Adenocarcinoma
    Nancy D. Ebelt, Edith Zuniga, Kevin B. Passi, Lukas J. Sobocinski and Edwin R. Manuel
    Mol Cancer Ther February 1 2020 19 (2) 706-716; DOI:10.1158/1535-7163.MCT-19-0556

  • Models and Technologies
    The First Clinical Use of a Recombinant Lactococcus lactis Expressing Human Papillomavirus Type 16 E7 Oncogene Oral Vaccine: A Phase I Safety and Immunogenicity Trial in Healthy Women Volunteers
    Amir Hossein Mohseni, Sedigheh Taghinezhad-S and Hossein Keyvani
    Mol Cancer Ther February 1 2020 19 (2) 717-727; DOI:10.1158/1535-7163.MCT-19-0375

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Molecular Cancer Therapeutics: 19 (2)
February 2020
Volume 19, Issue 2
  • Table of Contents
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Issue Highlights

  • 10D1F, an Anti-HER3 Antibody That Uniquely Blocks the Receptor Heterodimerization Interface, Potently Inhibits Tumor Growth Across a Broad Panel of Tumor Models
  • ERK Inhibitor LY3214996 Targets ERK Pathway–Driven Cancers: A Therapeutic Approach Toward Precision Medicine
  • Dual-Mechanism ERK1/2 Inhibitors Exploit a Distinct Binding Mode to Block Phosphorylation and Nuclear Accumulation of ERK1/2
  • Therapeutic Breast Reconstruction Using Gene Therapy–Delivered IFNγ Immunotherapy

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  • CD137 Agonist mAb with Reduced Liver Toxicity
  • Truncated BRCA2 Contributes to PARPi Resistance
  • ERPAS to Predict Response to Endocrine Therapy
  • CDK8/19 Inhibitors Enhance NK-Cell–Mediated Cancer Therapy
  • Sialoglycan mAb for Cancer Immunotherapy
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Molecular Cancer Therapeutics
eISSN: 1538-8514
ISSN: 1535-7163

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