Table of Contents

Small Molecule Therapeutics

• Small Molecule Therapeutics

  ASR490, a Small Molecule, Overrides Aberrant Expression of Notch1 in Colorectal Cancer

  Ashish Tyagi, Balaji Chandrasekaran, Venkatesh Kolluru, Becca V. Baby, Cibi A. Sripathi, Murali K. Ankem, Srinivasa R. Ramisetti, Venkat R. Chirasani, Nikolay V. Dokholyan, Arun K. Sharma and Chendil Damodaran

  Mol Cancer Ther December 1 2020 19 (12) 2422-2431; DOI:10.1158/1535-7163.MCT-19-0949

  
  
• Small Molecule Therapeutics

  Development of Tumor-Targeting IRE-1 Inhibitors for B-cell Cancer Therapy

  Andong Shao, Qin Xu, Walker T. Spalek, Christopher F. Cain, Chang Won Kang, Chih-Hang Anthony Tang, Juan R. Del Valle and Chih-Chi Andrew Hu

  Mol Cancer Ther December 1 2020 19 (12) 2432-2444; DOI:10.1158/1535-7163.MCT-20-0127

  
  
• Small Molecule Therapeutics

  MP-Pt(IV): A MAOB-Sensitive Mitochondrial-Specific Prodrug for Treating Glioblastoma

  Sudhir Raghavan, David S. Baskin and Martyn A. Sharpe

  Mol Cancer Ther December 1 2020 19 (12) 2445-2453; DOI:10.1158/1535-7163.MCT-20-0420

  
  
• Small Molecule Therapeutics | AuthorChoice

  Repurposing of a Thromboxane Receptor Inhibitor Based on a Novel Role in Metastasis Identified by Phenome-Wide Association Study

  Thomas A. Werfel, Donna J. Hicks, Bushra Rahman, Wendy E. Bendeman, Matthew T. Duvernay, Jae G. Maeng, Heidi Hamm, Robert R. Lavieri, Meghan M. Joly, Jill M. Pulley, David L. Elion, Dana M. Brantley-Sieders and Rebecca S. Cook

  Mol Cancer Ther December 1 2020 19 (12) 2454-2464; DOI:10.1158/1535-7163.MCT-19-1106

  
  
• Small Molecule Therapeutics

  Glutaminase Inhibitors Induce Thiol-Mediated Oxidative Stress and Radiosensitization in Treatment-Resistant Cervical Cancers

  Ramachandran Rashmi, Kay Jayachandran, Jin Zhang, Vishnu Menon, Naoshad Muhammad, Michael Zahner, Fiona Ruiz, Sisi Zhang, Kevin Cho, Yuting Wang, Xiaojing Huang, Yi Huang, Michael L. McCormick, Buck E. Rogers, Douglas R. Spitz, Gary J. Patti and Julie K. Schwarz

  Mol Cancer Ther December 1 2020 19 (12) 2465-2475; DOI:10.1158/1535-7163.MCT-20-0271

  
  
• Small Molecule Therapeutics | AuthorChoice

  HIV Protease Inhibitors Block HPV16-Induced Murine Cervical Carcinoma and Promote Vessel Normalization in Association with MMP-9 Inhibition and TIMP-3 Induction

  Yaqi Qiu, Federica Maione, Stefania Capano, Claudia Meda, Orietta Picconi, Serena Brundu, Alberto Pisacane, Anna Sapino, Clelia Palladino, Giovanni Barillari, Paolo Monini, Federico Bussolino, Barbara Ensoli, Cecilia Sgadari and Enrico Giraudo

  Mol Cancer Ther December 1 2020 19 (12) 2476-2489; DOI:10.1158/1535-7163.MCT-20-0055

  
  
• Small Molecule Therapeutics | AuthorChoice

  Inhibition of EZH2 Enhances the Antitumor Efficacy of Metformin in Prostate Cancer

  Yifan Kong, Yanquan Zhang, Fengyi Mao, Zhuangzhuang Zhang, Zhiguo Li, Ruixin Wang, Jinghui Liu and Xiaoqi Liu

  Mol Cancer Ther December 1 2020 19 (12) 2490-2501; DOI:10.1158/1535-7163.MCT-19-0874

  
  
• Small Molecule Therapeutics

  Selective Vulnerability to Pyrimidine Starvation in Hematologic Malignancies Revealed by AG-636, a Novel Clinical-Stage Inhibitor of Dihydroorotate Dehydrogenase

  Gabrielle McDonald, Victor Chubukov, John Coco, Kevin Truskowski, Rohini Narayanaswamy, Sung Choe, Mya Steadman, Erin Artin, Anil K. Padyana, Lei Jin, Sebastien Ronseaux, Charles Locuson, Zi-Peng Fan, Tabea Erdmann, Alan Mann, Sebastian Hayes, Mark Fletcher, Kavitha Nellore, Siva Sanjeeva Rao, Hosahalli Subramanya, K. Satish Reddy, Sunil K. Panigrahi, Thomas Antony, Sreevalsam Gopinath, Zhihua Sui, Nelamangala Nagaraja, Lenny Dang, Georg Lenz, Jonathan Hurov, Scott A. Biller, Josh Murtie, Kevin M. Marks and Danielle B. Ulanet

  Mol Cancer Ther December 1 2020 19 (12) 2502-2515; DOI:10.1158/1535-7163.MCT-20-0550

  
  
• Small Molecule Therapeutics

  A Precision Medicine Drug Discovery Pipeline Identifies Combined CDK2 and 9 Inhibition as a Novel Therapeutic Strategy in Colorectal Cancer

  Jason A. Somarelli, Roham Salman Roghani, Ali Sanjari Moghaddam, Beatrice C. Thomas, Gabrielle Rupprecht, Kathryn E. Ware, Erdem Altunel, John B. Mantyh, So Young Kim, Shannon J. McCall, Xiling Shen, Christopher R. Mantyh and David S. Hsu

  Mol Cancer Ther December 1 2020 19 (12) 2516-2527; DOI:10.1158/1535-7163.MCT-20-0454

  
  
• Small Molecule Therapeutics

  Implication of ZNF217 in Accelerating Tumor Development and Therapeutically Targeting ZNF217-Induced PI3K–AKT Signaling for the Treatment of Metastatic Osteosarcoma

  Branden A. Smeester, Garrett M. Draper, Nicholas J. Slipek, Alex T. Larsson, Natalie Stratton, Emily J. Pomeroy, Kelsie L. Becklin, Kenta Yamamoto, Kyle B. Williams, Kanut Laoharawee, Joseph J. Peterson, Juan E. Abrahante, Susan K. Rathe, Lauren J. Mills, Margaret R. Crosby, Wendy A. Hudson, Eric P. Rahrmann, David A. Largaespada and Branden S. Moriarity

  Mol Cancer Ther December 1 2020 19 (12) 2528-2541; DOI:10.1158/1535-7163.MCT-20-0369

  
  
• Small Molecule Therapeutics

  A Combination of BRD4 and HDAC3 Inhibitors Synergistically Suppresses Glioma Stem Cell Growth by Blocking GLI1/IL6/STAT3 Signaling Axis

  Qian Wang, Shengnan Jia, Ding Wang, Xuyang Chen, Dhan V. Kalvakolanu, Hongwu Zheng, Xiaodong Wei, Naiyan Wen, Hang Liang, Baofeng Guo and Ling Zhang

  Mol Cancer Ther December 1 2020 19 (12) 2542-2553; DOI:10.1158/1535-7163.MCT-20-0037