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Volume 21, Issue 5
1 May 2022
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    Effect of 200 nmol/L tucatinib on the internalization of HER2 in EFM192A cells. Cells were labeled by AF647-conjugated Herceptin at 21 μg/mL post 30-minute incubation with tucatinib and imaged for up to 52 hours. Read the article by O'Brien and colleagues on page 751.
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ISSN 1535-7163
EISSN 1538-8514

Highlights

Selected Articles from This Issue
View articletitled, Selected Articles from This Issue
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Small Molecule Therapeutics

Inhibition of Oxidized Nucleotide Sanitation By TH1579 and Conventional Chemotherapy Cooperatively Enhance Oxidative DNA Damage and Survival in AML
Anders Centio; Montserrat Estruch; Kristian Reckzeh; Kumar Sanjiv; Camilla Vittori; Sophia Engelhard; Ulrika Warpman Berglund; Thomas Helleday; Kim Theilgaard-Mönch
View articletitled, Inhibition of Oxidized Nucleotide Sanitation By TH1579 and Conventional Chemotherapy Cooperatively Enhance Oxidative DNA Damage and Survival in AML
Supplementary data
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Therapeutic Targeting of EZH2 and BET BRD4 in Pediatric Rhabdoid Tumors
Yukitomo Ishi; Yongzhan Zhang; Ali Zhang; Takahiro Sasaki; Andrea Piunti; Amreena Suri; Jun Watanabe; Kouki Abe; Xingyao He; Hiroaki Katagi; Pankaj Bhalla; Manabu Natsumeda; Lihua Zou; Ali Shilatifard; Rintaro Hashizume
View articletitled, Therapeutic Targeting of EZH2 and BET BRD4 in Pediatric Rhabdoid Tumors
Supplementary data
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Adoptive Transfer of Anti-Nucleolin T Cells Combined with PD-L1 Inhibition against Triple-Negative Breast Cancer
Suyanee Thongchot; Niphat Jirapongwattana; Piriya Luangwattananun; Wannasiri Chiraphapphaiboon; Nisa Chuangchot; Doonyapat Sa-nguanraksa; Pornchai O-Charoenrat; Peti Thuwajit; Pa-thai Yenchitsomanus; Chanitra Thuwajit
View articletitled, Adoptive Transfer of Anti-Nucleolin T Cells Combined with PD-L1 Inhibition against Triple-Negative Breast Cancer
Supplementary data
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Diaminobutoxy-substituted Isoflavonoid (DBI-1) Enhances the Therapeutic Efficacy of GLUT1 Inhibitor BAY-876 by Modulating Metabolic Pathways in Colon Cancer Cells
Lichao Guo; Wen Zhang; Yanqi Xie; Xi Chen; Emma E. Olmstead; Mengqiang Lian; Baochen Zhang; Yekaterina Y. Zaytseva; B. Mark Evers; H. Peter Spielmann; Xifu Liu; David S. Watt; Chunming Liu
View articletitled, Diaminobutoxy-substituted Isoflavonoid (DBI-1) Enhances the Therapeutic Efficacy of GLUT1 Inhibitor BAY-876 by Modulating Metabolic Pathways in Colon Cancer Cells
Supplementary data
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Tucatinib has Selective Activity in HER2-Positive Cancers and Significant Combined Activity with Approved and Novel Breast Cancer–Targeted Therapies
Neil A. O'Brien; Holly K.T. Huang; Martina S.J. McDermott; Athena M. Madrid; Tong Luo; Raul Ayala; Shawnt Issakhanian; Ke Wei Gong; Ming Lu; Jun Zhang; Dennis J. Slamon
View articletitled, Tucatinib has Selective Activity in HER2-Positive Cancers and Significant Combined Activity with Approved and Novel Breast Cancer–Targeted Therapies
Supplementary data
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Concurrent Inhibition of ERK and Farnesyltransferase Suppresses the Growth of HRAS Mutant Head and Neck Squamous Cell Carcinoma
Sehrish Javaid; Antje Schaefer; Craig M. Goodwin; Victoria V. Nguyen; Frances L. Massey; Mariaelena Pierobon; Da'Jhnae Gambrell-Sanders; Andrew M. Waters; Kathryn N. Lambert; J. Nathaniel Diehl; G. Aaron Hobbs; Kris C. Wood; Emanuel F. Petricoin, III; Channing J. Der; Adrienne D. Cox
View articletitled, Concurrent Inhibition of ERK and Farnesyltransferase Suppresses the Growth of HRAS Mutant Head and Neck Squamous Cell Carcinoma
Supplementary data
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Dual Fluorescence Isogenic Synthetic Lethal Kinase Screen and High-Content Secondary Screening for MUC16/CA125-Selective Agents
Thapi D. Rao; Mengyao Xu; Stephanie Eng; Guangli Yang; Robin Manson; Nestor Rosales; Raj Kumar; Irva E. Veillard; Qin Zhou; Alexia Iasonos; Ouathek Ouerfelli; Hakim Djaballah; David R. Spriggs; Oladapo O. Yeku
View articletitled, Dual Fluorescence Isogenic Synthetic Lethal Kinase Screen and High-Content Secondary Screening for MUC16/CA125-Selective Agents
Supplementary data
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A Preclinical Study to Repurpose Spironolactone for Enhancing Chemotherapy Response in Bladder Cancer
Dongbo Xu; Qiang Cao; Li Wang; Jianmin Wang; Bo Xu; Kristopher Attwood; Lei Wei; Yue Wu; Gary J. Smith; Eriko Katsuta; Kazuaki Takabe; Gurkamal Chatta; Khurshid A. Guru; David W. Goodrich; Qiang J. Li
View articletitled, A Preclinical Study to Repurpose Spironolactone for Enhancing Chemotherapy Response in Bladder Cancer
Supplementary data
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Large Molecule Therapeutics

Triple Targeting of HER Receptors Overcomes Heregulin-mediated Resistance to EGFR Blockade in Colorectal Cancer
Alexander Rau; Nicole Janssen; Lennart Kühl; Thomas Sell; Svetlana Kalmykova; Thomas E. Mürdter; Marc-H. Dahlke; Christine Sers; Markus Morkel; Matthias Schwab; Roland E. Kontermann; Monilola A. Olayioye
View articletitled, Triple Targeting of HER Receptors Overcomes Heregulin-mediated Resistance to EGFR Blockade in Colorectal Cancer
Supplementary data
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Proteolytic pan-RAS Cleavage Leads to Tumor Regression in Patient-derived Pancreatic Cancer Xenografts
Vania Vidimar; Minyoung Park; Caleb K. Stubbs; Nana K. Ingram; Wenan Qiang; Shanshan Zhang; Demirkan Gursel; Roman A. Melnyk; Karla J.F. Satchell
View articletitled, Proteolytic pan-RAS Cleavage Leads to Tumor Regression in Patient-derived Pancreatic Cancer Xenografts
Supplementary data
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Models and Technologies

CD74-NRG1 Fusions Are Oncogenic In Vivo and Induce Therapeutically Tractable ERBB2:ERBB3 Heterodimerization
Lisa Werr; Dennis Plenker; Marcel A. Dammert; Carina Lorenz; Johannes Brägelmann; Hannah L. Tumbrink; Sebastian Klein; Anna Schmitt; Reinhard Büttner; Thorsten Persigehl; Kevan M. Shokat; F. Thomas Wunderlich; Alison M. Schram; Martin Peifer; Martin L. Sos; H. Christian Reinhardt; Roman K. Thomas
View articletitled, CD74-NRG1 Fusions Are Oncogenic <em>In Vivo</em> and Induce Therapeutically Tractable ERBB2:ERBB3 Heterodimerization
Supplementary data
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Targeting Drug Resistance

Optimal Strategy and Benefit of Pulsed Therapy Depend On Tumor Heterogeneity and Aggressiveness at Time of Treatment Initiation
Deepti Mathur; Bradford P. Taylor; Walid K. Chatila; Howard I. Scher; Nikolaus Schultz; Pedram Razavi; Joao B. Xavier
View articletitled, Optimal Strategy and Benefit of Pulsed Therapy Depend On Tumor Heterogeneity and Aggressiveness at Time of Treatment Initiation
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The Irreversible FLT3 Inhibitor FF-10101 Is Active Against a Diversity of FLT3 Inhibitor Resistance Mechanisms
Timothy T. Ferng; Daisuke Terada; Makoto Ando; Theodore C. Tarver; Fihr Chaudhary; Kimberly C. Lin; Aaron C. Logan; Catherine C. Smith
View articletitled, The Irreversible FLT3 Inhibitor FF-10101 Is Active Against a Diversity of FLT3 Inhibitor Resistance Mechanisms
Supplementary data
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Corrections

Correction: HLA Polymorphisms Are Associated With Treatment-Free Remission Following Discontinuation of Tyrosine Kinase Inhibitors in Chronic Myeloid Leukemia
Hiroshi Ureshino; Takero Shindo; Hidenori Tanaka; Hiroh Saji; Shinya Kimura
View articletitled, Correction: <em>HLA</em> Polymorphisms Are Associated With Treatment-Free Remission Following Discontinuation of Tyrosine Kinase Inhibitors in Chronic Myeloid Leukemia
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Correction: A Novel Small Molecule Aurora Kinase Inhibitor Attenuates Breast Tumor Initiating Cells and Overcomes Drug Resistance
Fei-Meng Zheng; Zi-Jie Long; Zhi-Jie Hou; Yu Luo; Ling-Zhi Xu; Jiang-Long Xia; Xiao-Ju Lai; Ji-Wei Liu; Xi Wang; Muhammad Kamran; Min Yan; Shu-Juan Shao; Eric W.-F. Lam; Shao-Wu Wang; Gui Lu; Quentin Liu
View articletitled, Correction: A Novel Small Molecule Aurora Kinase Inhibitor Attenuates Breast Tumor Initiating Cells and Overcomes Drug Resistance
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