Molecular Cancer Therapeutics: 19 (2)

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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Small Molecule Therapeutics

Large Molecule Therapeutics

Cancer Biology and Translational Studies

Companion Diagnostic, Pharmacogenomic, and Cancer Biomarkers

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