Table of Contents

Small Molecule Therapeutics

• Small Molecule Therapeutics | AuthorChoice

  AZD0364 Is a Potent and Selective ERK1/2 Inhibitor That Enhances Antitumor Activity in KRAS-Mutant Tumor Models when Combined with the MEK Inhibitor, Selumetinib

  Vikki Flemington, Emma J. Davies, David Robinson, Linda C. Sandin, Oona Delpuech, Pei Zhang, Lyndsey Hanson, Paul Farrington, Sigourney Bell, Katarzyna Falenta, Francis D. Gibbons, Nicola Lindsay, Aaron Smith, Joanne Wilson, Karen Roberts, Michael Tonge, Philip Hopcroft, Sophie E. Willis, Martine P. Roudier, Claire Rooney, Elizabeth A. Coker, Patricia Jaaks, Mathew J. Garnett, Stephen E. Fawell, Clifford D. Jones, Richard A. Ward, Iain Simpson, Sabina C. Cosulich, J. Elizabeth Pease and Paul D. Smith

  Mol Cancer Ther February 1 2021 20 (2) 238-249; DOI:10.1158/1535-7163.MCT-20-0002

  
  
• Small Molecule Therapeutics | AuthorChoice

  SAR439859, a Novel Selective Estrogen Receptor Degrader (SERD), Demonstrates Effective and Broad Antitumor Activity in Wild-Type and Mutant ER-Positive Breast Cancer Models

  Maysoun Shomali, Jane Cheng, Fangxian Sun, Malvika Koundinya, Zhuyan Guo, Andrew T. Hebert, Jessica McManus, Mikhail N. Levit, Dietmar Hoffmann, Albane Courjaud, Rosalia Arrebola, Hui Cao, Jack Pollard, Joon Sang Lee, Laurent Besret, Anne Caron, Dinesh S. Bangari, Pierre-Yves Abecassis, Laurent Schio, Youssef El-Ahmad, Frank Halley, Michel Tabart, Victor Certal, Fabienne Thompson, Gary McCort, Bruno Filoche-Rommé, Hong Cheng, Carlos Garcia-Echeverria, Laurent Debussche and Monsif Bouaboula

  Mol Cancer Ther February 1 2021 20 (2) 250-262; DOI:10.1158/1535-7163.MCT-20-0390

  
  
• Small Molecule Therapeutics

  Combinatorial Efficacy of Olaparib with Radiation and ATR Inhibitor Requires PARP1 Protein in Homologous Recombination–Proficient Pancreatic Cancer

  Leslie A. Parsels, Carl G. Engelke, Joshua Parsels, Sheryl A. Flanagan, Qiang Zhang, Daria Tanska, Daniel R. Wahl, Christine E. Canman, Theodore S. Lawrence and Meredith A. Morgan

  Mol Cancer Ther February 1 2021 20 (2) 263-273; DOI:10.1158/1535-7163.MCT-20-0365

  
  
• Small Molecule Therapeutics

  Leflunomide Suppresses the Growth of LKB1-Inactivated Tumors in the Immune-Competent Host and Attenuates Distant Cancer Metastasis

  Rui Jin, Boxuan Liu, Xiuju Liu, Yijian Fan, Wei Peng, Chunzi Huang, Adam Marcus, Gabriel Sica, Melissa Gilbert-Ross, Yuan Liu and Wei Zhou

  Mol Cancer Ther February 1 2021 20 (2) 274-283; DOI:10.1158/1535-7163.MCT-20-0567

  
  
• Small Molecule Therapeutics | AuthorChoice

  Inhibition of Intermedin (Adrenomedullin 2) Suppresses the Growth of Glioblastoma and Increases the Antitumor Activity of Temozolomide

  Luping Huang, Denian Wang, Zhongxue Feng, Huan Zhao, Fei Xiao, Yong'gang Wei, Heng Zhang, Hongyu Li, Lingmiao Kong, Min Li, Fei Liu, Haili Zhang and Wei Zhang

  Mol Cancer Ther February 1 2021 20 (2) 284-295; DOI:10.1158/1535-7163.MCT-20-0619

  
  
• Small Molecule Therapeutics

  Birinapant Enhances Gemcitabine's Antitumor Efficacy in Triple-Negative Breast Cancer by Inducing Intrinsic Pathway–Dependent Apoptosis

  Xuemei Xie, Jangsoon Lee, Huey Liu, Troy Pearson, Alexander Y. Lu, Debu Tripathy, Gayathri R. Devi, Chandra Bartholomeusz and Naoto T. Ueno

  Mol Cancer Ther February 1 2021 20 (2) 296-306; DOI:10.1158/1535-7163.MCT-19-1160

  
  
• Small Molecule Therapeutics | AuthorChoice

  Rigosertib Induces Mitotic Arrest and Apoptosis in RAS-Mutated Rhabdomyosarcoma and Neuroblastoma

  Joshua T. Kowalczyk, Xiaolin Wan, Edjay R. Hernandez, Ruibai Luo, Gaelyn C. Lyons, Kelli M. Wilson, Devorah C. Gallardo, Kristine A. Isanogle, Christina M. Robinson, Arnulfo Mendoza, Christine M. Heske, Jinqui-Qiu Chen, Xiaoling Luo, Alexander E. Kelly, Simone Difilippantinio, Robert W. Robey, Craig J. Thomas, Dan L. Sackett, Deborah K. Morrison, Paul A. Randazzo, Lisa M. Miller Jenkins and Marielle E. Yohe

  Mol Cancer Ther February 1 2021 20 (2) 307-319; DOI:10.1158/1535-7163.MCT-20-0525