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Volume 21, Issue 1
1 January 2022
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    Cover Image

    issue cover
    In this issue of Molecular Cancer Therapeutics, Jensen-Pergakes and colleagues disclose the structure of the SAM-competitve PRMT5 inibitor PF-06939999. This crystal structure of PRMT5/MEP50 shows PF-0693999 (cyan) bound to a large portion of the S-adenosyl-homocysteine (SAH, in magenta) binding pocket. PF-06939999 demonstrated potent anti-proliferative activity in preclinical NSCLC tumors. Read the full study on page 3.
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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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MCT First Disclosures

SAM-Competitive PRMT5 Inhibitor PF-06939999 Demonstrates Antitumor Activity in Splicing Dysregulated NSCLC with Decreased Liability of Drug Resistance
Kristen Jensen-Pergakes; John Tatlock; Karen A. Maegley; Indrawan J. McAlpine; Michele McTigue; Tao Xie; Christopher P. Dillon; Yuli Wang; Shinji Yamazaki; Noah Spiegel; Manli Shi; Amy Nemeth; Natalie Miller; Eleanore Hendrickson; Hieu Lam; John Sherrill; Chi-Yeh Chung; Elizabeth A. McMillan; Shannon Karlicek Bryant; Prakash Palde; John Braganza; Alexei Brooun; Ya-Li Deng; Vesta Goshtasbi; Susan E. Kephart; Robert A. Kumpf; Wei Liu; Ryan L. Patman; Eugene Rui; Stephanie Scales; Michelle Tran-Dube; Fen Wang; Martin Wythes; Thomas A. Paul
View articletitled, SAM-Competitive PRMT5 Inhibitor PF-06939999 Demonstrates Antitumor Activity in Splicing Dysregulated NSCLC with Decreased Liability of Drug Resistance
Supplementary data
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Reviews

Exploiting Canonical TGFβ Signaling in Cancer Treatment
Qi Liu; Genwen Chen; Jade Moore; Ines Guix; Dimitris Placantonakis; Mary Helen Barcellos-Hoff
View articletitled, Exploiting Canonical TGFβ Signaling in Cancer Treatment
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DIRAS3: An Imprinted Tumor Suppressor Gene that Regulates RAS and PI3K-driven Cancer Growth, Motility, Autophagy, and Tumor Dormancy
Gamze Bildik; Xiaowen Liang; Margie N. Sutton; Robert C. Bast, Jr; Zhen Lu
View articletitled, DIRAS3: An Imprinted Tumor Suppressor Gene that Regulates RAS and PI3K-driven Cancer Growth, Motility, Autophagy, and Tumor Dormancy
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Small Molecule Therapeutics

AXL Inhibitor TP-0903 Reduces Metastasis and Therapy Resistance in Pancreatic Cancer
Yuqing Zhang; Emily N. Arner; Ali Rizvi; Jason E. Toombs; Huocong Huang; Steven L. Warner; Jason M. Foulks; Rolf A. Brekken
View articletitled, AXL Inhibitor TP-0903 Reduces Metastasis and Therapy Resistance in Pancreatic Cancer
Supplementary data
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Triple Targeting of Breast Tumors Driven by Hormonal Receptors and HER2
Elena Shagisultanova; Lyndsey S. Crump; Michelle Borakove; Jessica K. Hall; Aryana R. Rasti; Benjamin A. Harrison; Peter Kabos; Traci R. Lyons; Virginia F. Borges
View articletitled, Triple Targeting of Breast Tumors Driven by Hormonal Receptors and HER2
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Targeting CD99 Compromises the Oncogenic Effects of the Chimera EWS–FLI1 by Inducing Reexpression of Zyxin and Inhibition of GLI1 Activity
Tommaso Balestra; Maria Cristina Manara; Maria Antonella Laginestra; Michela Pasello; Alessandra De Feo; Cristian Bassi; Clara Guerzoni; Lorena Landuzzi; Pier-Luigi Lollini; Davide Maria Donati; Massimo Negrini; Mauro Magnani; Katia Scotlandi
View articletitled, Targeting CD99 Compromises the Oncogenic Effects of the Chimera EWS–FLI1 by Inducing Reexpression of Zyxin and Inhibition of GLI1 Activity
Supplementary data
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The Novel Dual Topoisomerase Inhibitor P8-D6 Shows Anti-myeloma Activity In Vitro and In Vivo
Katja Klausz; Christian Kellner; Carina Lynn Gehlert; Steffen Krohn; Hauke Wilcken; Inken Floerkemeier; Andreas Günther; Dirk O. Bauerschlag; Bernd Clement; Martin Gramatzki; Matthias Peipp
View articletitled, The Novel Dual Topoisomerase Inhibitor P8-D6 Shows Anti-myeloma Activity <em>In Vitro</em> and <em>In Vivo</em>
Supplementary data
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Radiosensitizing Pancreatic Cancer via Effective Autophagy Inhibition
Taha Yazal; Justine Bailleul; Yangjingyi Ruan; David Sung; Fang-I Chu; Daisy Palomera; Amy Dao; Anahita Sehgal; Vibha Gurunathan; Laila Aryan; Mansoureh Eghbali; Erina Vlashi
View articletitled, Radiosensitizing Pancreatic Cancer via Effective Autophagy Inhibition
Supplementary data
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Anti-apoptotic MCL1 Protein Represents Critical Survival Molecule for Most Burkitt Lymphomas and BCL2-negative Diffuse Large B-cell Lymphomas
Magdalena Klanova; Dmitry Kazantsev; Eva Pokorna; Tomas Zikmund; Jana Karolova; Matej Behounek; Nicol Renesova; Dana Sovilj; Cristina D. Kelemen; Karel Helman; Radek Jaksa; Ondrej Havranek; Ladislav Andera; Marek Trneny; Pavel Klener
View articletitled, Anti-apoptotic MCL1 Protein Represents Critical Survival Molecule for Most Burkitt Lymphomas and BCL2-negative Diffuse Large B-cell Lymphomas
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The Mitochondrial Disruptor Devimistat (CPI-613) Synergizes with Genotoxic Anticancer Drugs in Colorectal Cancer Therapy in a Bim-Dependent Manner
Carina Arnold; Philipp Demuth; Nina Seiwert; Simon Wittmann; Kerstin Boengler; Birgit Rasenberger; Markus Christmann; Magdalena Huber; Thomas Brunner; Michael Linnebacher; Jörg Fahrer
View articletitled, The Mitochondrial Disruptor Devimistat (CPI-613) Synergizes with Genotoxic Anticancer Drugs in Colorectal Cancer Therapy in a Bim-Dependent Manner
Supplementary data
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Large Molecule Therapeutics

A FZD7-specific Antibody–Drug Conjugate Induces Ovarian Tumor Regression in Preclinical Models
Myan Do; Christina C.N. Wu; Pooja R. Sonavane; Edwin F. Juarez; Stephen R. Adams; Jason Ross; Alessandra Rodriguez y Baena; Charmi Patel; Jill P. Mesirov; Dennis A. Carson; Sunil J. Advani; Karl Willert
View articletitled, A FZD7-specific Antibody–Drug Conjugate Induces Ovarian Tumor Regression in Preclinical Models
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Intraperitoneal Pretargeted Radioimmunotherapy for Colorectal Peritoneal Carcinomatosis
Christopher S. Chandler; Meghan M. Bell; Sebastian K. Chung; Darren R. Veach; Edward K. Fung; Blesida Punzalan; Daniela Burnes Vargas; Mitesh Patel; Hong Xu; Hong-fen Guo; Brian H. Santich; Pat B. Zanzonico; Sébastien Monette; Garrett M. Nash; Andrea Cercek; Achim Jungbluth; Neeta Pandit-Taskar; Nai Kong V. Cheung; Steven M. Larson; Sarah M. Cheal
View articletitled, Intraperitoneal Pretargeted Radioimmunotherapy for Colorectal Peritoneal Carcinomatosis
Supplementary data
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Enhanced Antitumor Responses of Tumor Antigen-Specific TCR T Cells Genetically Engineered to Produce IL7 and CCL19
Yoshihiro Tokunaga; Takahiro Sasaki; Shunsuke Goto; Keishi Adachi; Yukimi Sakoda; Koji Tamada
View articletitled, Enhanced Antitumor Responses of Tumor Antigen-Specific TCR T Cells Genetically Engineered to Produce IL7 and CCL19
Supplementary data
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Combination Therapy of Hepatocellular Carcinoma by GPC3-Targeted Bispecific Antibody and Irinotecan is Potent in Suppressing Tumor Growth in Mice
Xin Chen; Yanmin Chen; Rong Liang; Lanxin Xiang; Jingwen Li; Yuankui Zhu; Huixia He; Le Huang; Dianbao Zuo; Weihang Li; Xinjun Liang; Shuang Dong; Sheng Hu; Mitchell Ho; Mingqian Feng
View articletitled, Combination Therapy of Hepatocellular Carcinoma by GPC3-Targeted Bispecific Antibody and Irinotecan is Potent in Suppressing Tumor Growth in Mice
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The Road to Personalized Myeloma Medicine: Patient-specific Single-domain Antibodies for Anti-idiotypic Radionuclide Therapy
Janik Puttemans; Benoit Stijlemans; Marleen Keyaerts; Sam Vander Meeren; Wim Renmans; Karel Fostier; Pieterjan Debie; Heleen Hanssens; Magdalena Rodak; Marek Pruszynski; Kim De Veirman; Karin Vanderkerken; Tony Lahoutte; Alfred Morgenstern; Frank Bruchertseifer; Nick Devoogdt; Matthias D'Huyvetter
View articletitled, The Road to Personalized Myeloma Medicine: Patient-specific Single-domain Antibodies for Anti-idiotypic Radionuclide Therapy
Supplementary data
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Targeting Drug Resistance

Vertical Inhibition of the RAF–MEK–ERK Cascade Induces Myogenic Differentiation, Apoptosis, and Tumor Regression in H/NRASQ61X Mutant Rhabdomyosarcoma
Natalia Garcia; Vanessa Del Pozo; Marielle E. Yohe; Craig M. Goodwin; Terry J. Shackleford; Long Wang; Kunal Baxi; Yidong Chen; Anna T. Rogojina; Sara M. Zimmerman; Cody J. Peer; William D. Figg; Myron S. Ignatius; Kris C. Wood; Peter J. Houghton; Angelina V. Vaseva
View articletitled, Vertical Inhibition of the RAF–MEK–ERK Cascade Induces Myogenic Differentiation, Apoptosis, and Tumor Regression in <em>H/NRAS<sup>Q61X</sup></em> Mutant Rhabdomyosarcoma
Supplementary data
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Overcoming Gemcitabine Resistance in Pancreatic Cancer Using the BCL-XL–Specific Degrader DT2216
Dinesh Thummuri; Sajid Khan; Patrick W. Underwood; Peiyi Zhang; Janet Wiegand; Xuan Zhang; Vivekananda Budamagunta; Amin Sobh; Abderrahmane Tagmount; Alexander Loguinov; Andrea N. Riner; Ashwin S. Akki; Elizabeth Williamson; Robert Hromas; Christopher D. Vulpe; Guangrong Zheng; Jose G. Trevino; Daohong Zhou
View articletitled, Overcoming Gemcitabine Resistance in Pancreatic Cancer Using the BCL-X<sub>L</sub>–Specific Degrader DT2216
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Targeting DNMTs to Overcome Enzalutamide Resistance in Prostate Cancer
Elia Farah; Zhuangzhuang Zhang; Sagar M. Utturkar; Jinpeng Liu; Timothy L. Ratliff; Xiaoqi Liu
View articletitled, Targeting DNMTs to Overcome Enzalutamide Resistance in Prostate Cancer
Supplementary data
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Anastrozole Regulates Fatty Acid Synthase in Breast Cancer
Junmei Cairns; James N. Ingle; Krishna R. Kalari; Matthew P. Goetz; Richard M. Weinshilboum; Huanyao Gao; Hu Li; Mehrab Ghanat Bari; Liewei Wang
View articletitled, Anastrozole Regulates Fatty Acid Synthase in Breast Cancer
Supplementary data
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Companion Diagnostic, Pharmacogenomic, and Cancer Biomarkers

HSP90-Specific nIR Probe Identifies Aggressive Prostate Cancers: Translation from Preclinical Models to a Human Phase I Study
Takuya Osada; Erika J. Crosby; Kensuke Kaneko; Joshua C. Snyder; Joshua D. Ginzel; Chaitanya R. Acharya; Xiao-Yi Yang; Thomas J. Polascik; Ivan Spasojevic; Rendon C. Nelson; Amy Hobeika; Zachary C. Hartman; Leonard M. Neckers; Andre Rogatko; Philip F. Hughes; Jiaoti Huang; Michael A. Morse; Timothy Haystead; H. Kim Lyerly
View articletitled, HSP90-Specific nIR Probe Identifies Aggressive Prostate Cancers: Translation from Preclinical Models to a Human Phase I Study
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Association of Homologous Recombination–DNA Damage Response Gene Mutations with Immune Biomarkers in Gastroesophageal Cancers
Michael Cerniglia; Joanne Xiu; Axel Grothey; Michael J. Pishvaian; Yasmine Baca; Jimmy J. Hwang; John L. Marshall; Ari M. VanderWalde; Anthony F. Shields; Heinz-Josef Lenz; W. Michael Korn; Mohamed Salem; Philip A. Philip; Richard M. Goldberg; Jia Zeng; Sunnie S. Kim
View articletitled, Association of Homologous Recombination–DNA Damage Response Gene Mutations with Immune Biomarkers in Gastroesophageal Cancers
Supplementary data
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Letters to the Editor

Novel Peptide Camptothecin Drug-linkers for Potent ADCs—Letter
David M. Goldenberg; Robert M. Sharkey; Serengulam V. Govindan; Thomas M. Cardillo
View articletitled, Novel Peptide Camptothecin Drug-linkers for Potent ADCs—Letter
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Novel Peptide Camptothecin Drug-linkers for Potent ADCs—Reply
Scott Jeffrey; Peter Senter
View articletitled, Novel Peptide Camptothecin Drug-linkers for Potent ADCs—Reply
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Acknowledgment to Reviewers

Acknowledgment to Reviewers
View articletitled, Acknowledgment to Reviewers
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  • Online ISSN 1538-8514
  • Print ISSN 1535-7163

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