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1 October 2021
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Cover Image
Cover Image
This graphic depicts “decreased desmoplasia and increased PD-L1 targetability” after MAPK therapy in a proposed model showing alterations in the tumor microenvironment by activating the immune system and breaking down the stromal components, resulting in a release of cytokines and growth factors, along with a migration of inflammatory cells and macrophages. Read the full article on page 2026. - PDF Icon PDF LinkTable of Contents
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ISSN 1535-7163
EISSN 1538-8514
Highlights
MCT First Disclosures
ASTX029, a Novel Dual-mechanism ERK Inhibitor, Modulates Both the Phosphorylation and Catalytic Activity of ERK
Joanne M. Munck; Valerio Berdini; Luke Bevan; Jessica L. Brothwood; Juan Castro; Aurélie Courtin; Charlotte East; Roberta Ferraldeschi; Tom D. Heightman; Christopher J. Hindley; Justyna Kucia-Tran; John F. Lyons; Vanessa Martins; Sandra Muench; Christopher W. Murray; David Norton; Marc O'Reilly; Michael Reader; David C. Rees; Sharna J. Rich; Caroline J. Richardson; Alpesh D. Shah; Lukas Stanczuk; Neil T. Thompson; Nicola E. Wilsher; Alison J.-A. Woolford; Nicola G. Wallis
Reviews
Small Molecule Therapeutics
Selective Inhibition of the Second Bromodomain of BET Family Proteins Results in Robust Antitumor Activity in Preclinical Models of Acute Myeloid Leukemia
Lu Zhang; Tianyu Cai; Xiaoyu Lin; Xiaoli Huang; Mai H. Bui; Joshua P. Plotnik; Richard J. Bellin; Emily J. Faivre; Vinitha M. Kuruvilla; Lloyd T. Lam; Xin Lu; Zheng Zha; Weiguo Feng; Paul Hessler; Tamar Uziel; Qi Zhang; Antonio Cavazos; Lina Han; Debra C. Ferguson; Gaurav Mehta; Sriram S. Shanmugavelandy; Terrance J. Magoc; Jenny Rowe; Neal C. Goodwin; Kathleen A. Dorritie; Michael Boyiadzis; Daniel H. Albert; Keith F. McDaniel; Warren M. Kati; Marina Konopleva; Yu Shen
Protein Phosphatase 2A as a Therapeutic Target in Small Cell Lung Cancer
Tamara Mirzapoiazova; Gang Xiao; Bolot Mambetsariev; Mohd W. Nasser; Emily Miaou; Sharad S. Singhal; Saumya Srivastava; Isa Mambetsariev; Michael S. Nelson; Arin Nam; Amita Behal; Pranita Atri; Markus Muschen; François L.H. Tissot; James Miser; John S. Kovach; Martin Sattler; Surinder K. Batra; Prakash Kulkarni; Ravi Salgia
PAK4-NAMPT Dual Inhibition Sensitizes Pancreatic Neuroendocrine Tumors to Everolimus
Gabriel B. Mpilla; Md. Hafiz Uddin; Mohammed N. Al-Hallak; Amro Aboukameel; Yiwei Li; Steve H. Kim; Rafic Beydoun; Gregory Dyson; Erkan Baloglu; William T. Senapedis; Yosef Landesman; Kay-Uwe Wagner; Nerissa T. Viola; Bassel F. El-Rayes; Philip A. Philip; Ramzi M. Mohammad; Asfar S. Azmi
Preclinical and Early Clinical Development of PTC596, a Novel Small-Molecule Tubulin-Binding Agent
Finith Jernigan; Arthur Branstrom; John D. Baird; Liangxian Cao; Mandar Dali; Bansri Furia; Min Jung Kim; Kylie O'Keefe; Ronald Kong; Oscar L. Laskin; Joseph M. Colacino; Mark Pykett; Anna Mollin; Josephine Sheedy; Melissa Dumble; Young-Choon Moon; Richard Sheridan; Tobias Mühlethaler; Robert J. Spiegel; Andrea E. Prota; Michel O. Steinmetz; Marla Weetall
Pharmaceutical Interference of the EWS-FLI1–driven Transcriptome By Cotargeting H3K27ac and RNA Polymerase Activity in Ewing Sarcoma
Daniel A.R. Heisey; Sheeba Jacob; Timothy L. Lochmann; Richard Kurupi; Maninderjit S. Ghotra; Marissa L. Calbert; Mayuri Shende; Yuki Kato Maves; Jennifer E. Koblinski; Mikhail G. Dozmorov; Sosipatros A. Boikos; Cyril H. Benes; Anthony C. Faber
Hsp90 Inhibitor STA9090 Sensitizes Hepatocellular Carcinoma to Hyperthermia-Induced DNA Damage by Suppressing DNA-PKcs Protein Stability and mRNA Transcription
Lixia Liu; Yaotang Deng; Zhenming Zheng; Zihao Deng; Jinxin Zhang; Jieyou Li; Manfeng Liang; Xueqiong Zhou; Wenchong Tan; Hongjun Yang; Leonard M. Neckers; Fei Zou; Xuemei Chen
Potent Synergistic Effect on C-Myc–Driven Colorectal Cancers Using a Novel Indole-Substituted Quinoline with a Plk1 Inhibitor
Yanqi Xie; Wen Zhang; Lichao Guo; Liliia M. Kril; Kristin L. Begley; Vitaliy M. Sviripa; Xi Chen; Xifu Liu; Eun Y. Lee; Daheng He; Chi Wang; Tianyan Gao; Xiaoqi Liu; B. Mark Evers; David S. Watt; Chunming Liu
Itraconazole Exerts Its Antitumor Effect in Esophageal Cancer By Suppressing the HER2/AKT Signaling Pathway
Wei Zhang; Ankur S. Bhagwath; Zeeshan Ramzan; Taylor A. Williams; Indhumathy Subramaniyan; Vindhya Edpuganti; Raja Reddy Kallem; Kerry B. Dunbar; Peiguo Ding; Ke Gong; Samuel A. Geurkink; Muhammad S. Beg; James Kim; Qiuyang Zhang; Amyn A. Habib; Sung-Hee Choi; Ritu Lapsiwala; Gayathri Bhagwath; Jonathan E. Dowell; Shelby D. Melton; Chunfa Jie; William C. Putnam; Thai H. Pham; David H. Wang
T Cell–Mediated Antitumor Immunity Cooperatively Induced By TGFβR1 Antagonism and Gemcitabine Counteracts Reformation of the Stromal Barrier in Pancreatic Cancer
Dandan Li; Nicholas Schaub; Theresa M. Guerin; Tashinga E. Bapiro; Frances M. Richards; Vicky Chen; Keyur Talsania; Parimal Kumar; Debra J. Gilbert; Jerome J. Schlomer; Seong-Jin Kim; Rebecca Sorber; Yaroslav Teper; Wendy Bautista; Claudia Palena; Chan-Young Ock; Duncan I. Jodrell; Nathan Pate; Monika Mehta; Yongmei Zhao; Serguei Kozlov; Udo Rudloff
Large Molecule Therapeutics
Belantamab Mafodotin (GSK2857916) Drives Immunogenic Cell Death and Immune-mediated Antitumor Responses In Vivo
Rocio Montes de Oca; Alireza S. Alavi; Nick Vitali; Sabyasachi Bhattacharya; Christina Blackwell; Krupa Patel; Laura Seestaller-Wehr; Heather Kaczynski; Hong Shi; Eric Dobrzynski; Leslie Obert; Lyuben Tsvetkov; David C. Cooper; Heather Jackson; Paul Bojczuk; Sabrina Forveille; Oliver Kepp; Allan Sauvat; Guido Kroemer; Mark Creighton-Gutteridge; Jingsong Yang; Chris Hopson; Niranjan Yanamandra; Christopher Shelton; Patrick Mayes; Joanna Opalinska; Mary Barnette; Roopa Srinivasan; James Smothers; Axel Hoos
Valency of HER2 Targeting Antibodies Influences Tumor Cell Internalization and Penetration
Madeleine K. Ramos; Danielle Mandikian; Lauren N. Sermeño; Anna King; Alecia T. Dent; Jason Ho; Sheila Ulufatu; T. Noelle Lombana; Christoph Spiess; Mary Ann T. Go; Shang-Fan Yu; Amrita V. Kamath; Gregory Z. Ferl; C. Andrew Boswell
A Biparatopic Antibody–Drug Conjugate to Treat MET-Expressing Cancers, Including Those that Are Unresponsive to MET Pathway Blockade
John O. DaSilva; Katie Yang; Oliver Surriga; Thomas Nittoli; Arthur Kunz; Matthew C. Franklin; Frank J. Delfino; Shu Mao; Feng Zhao; Jason T. Giurleo; Marcus P. Kelly; Sosina Makonnen; Carlos Hickey; Pamela Krueger; Randi Foster; Zhaoyuan Chen; Marc W. Retter; Rabih Slim; Tara M. Young; William C. Olson; Gavin Thurston; Christopher Daly
Preclinical Assessment of a MUC12-Targeted BiTE (Bispecific T-cell Engager) Molecule
Elizabeth Pham; Matthias Friedrich; Famke Aeffner; Michael Lutteropp; Natalie F. Mariano; Petra Deegen; Christoph Dahlhoff; Franziska Vogel; Claudia Bluemel; John M. Harrold; Christian Brandl; Natalia Grinberg; Benno Rattel; Angela Coxon; Julie M. Bailis
Phase I Open-Label Study Evaluating the Safety, Pharmacokinetics, and Preliminary Efficacy of Dilpacimab in Patients with Advanced Solid Tumors
Michael S. Gordon; John Nemunaitis; Minal Barve; Zev A. Wainberg; Erika P. Hamilton; Ramesh K. Ramanathan; George W. Sledge, Jr; Huibin Yue; Susan E. Morgan-Lappe; Martha Blaney; Sreeneeranj Kasichayanula; Monica Motwani; Lan Wang; Louie Naumovski; John H. Strickler
Companion Diagnostic, Pharmacogenomic, and Cancer Biomarkers
A Comprehensive Circulating Tumor DNA Assay for Detection of Translocation and Copy-Number Changes in Pediatric Sarcomas
Avanthi Tayi Shah; Tej D. Azad; Marcus R. Breese; Jacob J. Chabon; Emily G. Hamilton; Krystal Straessler; David M. Kurtz; Stanley G. Leung; Aviv Spillinger; Heng-Yi Liu; Inge H. Behroozfard; Frederick M. Wittber; Florette K. Hazard; Soo-Jin Cho; Heike E. Daldrup-Link; Kieuhoa T. Vo; Arun Rangaswami; Allison Pribnow; Sheri L. Spunt; Norman J. Lacayo; Maximilian Diehn; Ash A. Alizadeh; E. Alejandro Sweet-Cordero
Targeting Drug Resistance
Targeting CDK4/6 Represents a Therapeutic Vulnerability in Acquired BRAF/MEK Inhibitor–Resistant Melanoma
Kelsey W. Nassar; Jennifer D. Hintzsche; Stacey M. Bagby; Veronica Espinoza; Christophe Langouët-Astrié; Carol M. Amato; Tugs-Saikhan Chimed; Mayumi Fujita; William Robinson; Aik Choon Tan; Rebecca E. Schweppe
Models and Technologies
Novel Humanized Mesothelin-Expressing Genetically Engineered Mouse Models Underscore Challenges in Delivery of Complex Therapeutics to Pancreatic Cancers
Brendan Hagerty; T. Norene O'Sullivan; Xianyu Zhang; N. Keith Collins; Wendi Custer Lawrence; Laura L. Bassel; Nathan Pate; Jian Xu; Theresa M. Guerin; Serguei Kozlov; Christine Alewine
Letters to the Editor
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