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1 April 2021
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Cover Image
Cover Image
In this issue of Molecular Cancer Therapeutics, Morris and colleagues disclose a novel fluorine-containing cytidine analog, F-aza-T-dCyd. F-aza-T-dCyd produced complete regressions in the HL-60 model pictured, as well as in xenografts of bladder and colon cancer. Their disclosure supports the continued development of F-aza-T-dCyd as a new therapeutic in a category that has seen five FDA approvals. Read the full manuscript on page 625. - PDF Icon PDF LinkTable of Contents
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ISSN 1535-7163
EISSN 1538-8514
Highlights
MCT First Disclosures
Author Choice
F-aza-T-dCyd (NSC801845), a Novel Cytidine Analog, in Comparative Cell Culture and Xenograft Studies with the Clinical Candidates T-dCyd, F-T-dCyd, and Aza-T-dCyd
Joel Morris; Donn G. Wishka; Omar D. Lopez; Vladimir Rudchenko; Guangfei Huang; Sierra N. Hoffman; Suzanne Borgel; Kyle Georgius; John Carter; Howard Stotler; Mark W. Kunkel; Jerry M. Collins; Melinda G. Hollingshead; Beverly A. Teicher
Review
Small Molecule Therapeutics
ERK Inhibitor LY3214996-Based Treatment Strategies for RAS-Driven Lung Cancer
Jens Köhler; Yutong Zhao; Jiaqi Li; Prafulla C. Gokhale; Hong L. Tiv; Aine R. Knott; Margaret K. Wilkens; Kara M. Soroko; Mika Lin; Chiara Ambrogio; Monica Musteanu; Atsuko Ogino; Jihyun Choi; Magda Bahcall; Arrien A. Bertram; Emily S. Chambers; Cloud P. Paweletz; Shripad V. Bhagwat; Jason R. Manro; Ramon V. Tiu; Pasi A. Jänne
ONC201 Shows Potent Anticancer Activity Against Medullary Thyroid Cancer via Transcriptional Inhibition of RET, VEGFR2, and IGFBP2
Rozita Bagheri-Yarmand; Ramona Dadu; Lei Ye; Yaashmin Shiny Jebaraj; Jade A. Martinez; Junsheng Ma; Rohinton S. Tarapore; Joshua E. Allen; Steven I. Sherman; Michelle D. Williams; Robert F. Gagel
PP2A-activating Drugs Enhance FLT3 Inhibitor Efficacy through AKT Inhibition–Dependent GSK-3β–Mediated c-Myc and Pim-1 Proteasomal Degradation
Mario Scarpa; Prerna Singh; Christopher M. Bailey; Jonelle K. Lee; Shivani Kapoor; Rena G. Lapidus; Sandrine Niyongere; Jaya Sangodkar; Yin Wang; Danilo Perrotti; Goutham Narla; Maria R. Baer
Targeting BET Proteins BRD2 and BRD3 in Combination with PI3K-AKT Inhibition as a Therapeutic Strategy for Ovarian Clear Cell Carcinoma
Shogo Shigeta; Goldie Y.L. Lui; Reid Shaw; Russell Moser; Kay E. Gurley; Grace Durenberger; Rachele Rosati; Robert L. Diaz; Tan A. Ince; Elizabeth M. Swisher; Carla Grandori; Christopher J. Kemp
Rapid Resistance of FGFR-driven Gastric Cancers to Regorafenib and Targeted FGFR Inhibitors can be Overcome by Parallel Inhibition of MEK
David K. Lau; Ian Y. Luk; Laura J. Jenkins; Andrew Martin; David S. Williams; Kael L. Schoffer; Fiona Chionh; Michael Buchert; Katrin Sjoquist; Alex Boussioutas; Sarah A. Hayes; Matthias Ernst; Andrew J. Weickhardt; Nick Pavlakis; Niall C. Tebbutt; John M. Mariadason
Large Molecule Therapeutics
Anti-LYPD1/CD3 T-Cell-Dependent Bispecific Antibody for the Treatment of Ovarian Cancer
Amy A. Lo; Jennifer Johnston; Ji Li; Danielle Mandikian; Maria Hristopoulos; Robyn Clark; Dorothee Nickles; Wei-Ching Liang; Kathy Hötzel; Debra Dunlap; Thinh Pham; Hao Cai; Meric Ovacik; Daniel Bravo-Perez; Elaine Mai; Dionysos Slaga; Diego Ellerman; James Ziai; Klara Totpal; Genee Lee; C. Andrew Boswell; Jian Payandeh; Yan Wu; Teemu T. Junttila
Cancer Biology and Translational Studies
Lipidome-based Targeting of STAT3-driven Breast Cancer Cells Using Poly-l-glutamic Acid–coated Layer-by-Layer Nanoparticles
Isidora Tošić; Lisa N. Heppler; Susana P. Egusquiaguirre; Natalie Boehnke; Santiago Correa; Daniel F. Costa; Elizabeth A. Grossman Moore; Sharmistha Pal; Douglas S. Richardson; Alexander R. Ivanov; Daphne A. Haas-Kogan; Daniel K. Nomura; Paula T. Hammond; David A. Frank
Models and Technologies
Author Choice
Isoform- and Phosphorylation-specific Multiplexed Quantitative Pharmacodynamics of Drugs Targeting PI3K and MAPK Signaling in Xenograft Models and Clinical Biopsies
William G. Herrick; Casey L. Kilpatrick; Melinda G. Hollingshead; Dominic Esposito; Geraldine O'Sullivan Coyne; Andrea M. Gross; Barry C. Johnson; Alice P. Chen; Brigitte C. Widemann; James H. Doroshow; Ralph E. Parchment; Apurva K. Srivastava
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