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1 July 2020
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Cover Image
Cover Image
In this month's edition, Bennett and colleagues disclose BT5528, a Bicycle toxin-conjugate targeting EphA2. On the cover, BT5528 is shown bound to EphA2 on the surface of HT1080 fibrosarcoma cells in a High Content Screening assay. BT5528 provided persistent toxins to tumor cells while avoiding systemic exposure and has entered a Phase I clinical trial (NCT04180371). Read the First Disclosure on page 1385.Close Modal - PDF Icon PDF LinkTable of Contents
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ISSN 1535-7163
EISSN 1538-8514
Highlights
MCT First Disclosures
Small Molecule Therapeutics
Author Choice
The Dysregulated Pharmacology of Clinically Relevant ESR1 Mutants is Normalized by Ligand-activated WT Receptor
Kaitlyn J. Andreano; Jennifer G. Baker; Sunghee Park; Rachid Safi; Sandeep Artham; Steffi Oesterreich; Rinath Jeselsohn; Myles Brown; Sarah Sammons; Suzanne E. Wardell; Ching-yi Chang; John D. Norris; Donald P. McDonnell
Combined Targeting of the BRD4–NUT–p300 Axis in NUT Midline Carcinoma by Dual Selective Bromodomain Inhibitor, NEO2734
Chevaun D. Morrison-Smith; Tatiana M. Knox; Ivona Filic; Kara M. Soroko; Benjamin K. Eschle; Margaret K. Wilkens; Prafulla C. Gokhale; Francis Giles; Andrew Griffin; Bill Brown; Geoffrey I. Shapiro; Beth E. Zucconi; Philip A. Cole; Madeleine E. Lemieux; Christopher A. French
Author Choice
Targeting the PI3K/AKT Pathway Overcomes Enzalutamide Resistance by Inhibiting Induction of the Glucocorticoid Receptor
Remi Adelaiye-Ogala; Berkley E. Gryder; Yen Thi Minh Nguyen; Aian Neil Alilin; Adlai R. Grayson; Wardah Bajwa; Keith H. Jansson; Michael L. Beshiri; Supreet Agarwal; Jose Antonio Rodriguez-Nieves; Brian Capaldo; Kathleen Kelly; David J. VanderWeele
Large Molecule Therapeutics
Companion Diagnostic, Pharmacogenomic, and Cancer Biomarkers
Author Choice
Early Assessment of Molecular Progression and Response by Whole-genome Circulating Tumor DNA in Advanced Solid Tumors
Andrew A. Davis; Wade T. Iams; David Chan; Michael S. Oh; Robert W. Lentz; Neil Peterman; Alex Robertson; Abhik Shah; Rohith Srivas; Timothy J. Wilson; Nicole J. Lambert; Peter S. George; Becky Wong; Haleigh W. Wood; Jason C. Close; Ayse Tezcan; Ken Nesmith; Haluk Tezcan; Young Kwang Chae
Cancer Biology and Translational Studies
Functional miRNA Screening Identifies Wide-ranging Antitumor Properties of miR-3622b-5p and Reveals a New Therapeutic Combination Strategy in Ovarian Tumor Organoids
Mégane Vernon; Bernard Lambert; Matthieu Meryet-Figuière; Emilie Brotin; Louis-Bastien Weiswald; Hippolyte Paysant; Nicolas Vigneron; Anaïs Wambecke; Edwige Abeilard; Florence Giffard; Marie-Hélène Louis; Cécile Blanc-Fournier; Pascal Gauduchon; Laurent Poulain; Christophe Denoyelle
EWS-FLI1–regulated Serine Synthesis and Exogenous Serine are Necessary for Ewing Sarcoma Cellular Proliferation and Tumor Growth
Sameer H. Issaq; Arnulfo Mendoza; Ria Kidner; Tracy I. Rosales; Damien Y. Duveau; Christine M. Heske; Jason M. Rohde; Matthew B. Boxer; Craig J. Thomas; Ralph J. DeBerardinis; Lee J. Helman
Author Choice
DCLK1-Isoform2 Alternative Splice Variant Promotes Pancreatic Tumor Immunosuppressive M2-Macrophage Polarization
Parthasarathy Chandrakesan; Janani Panneerselvam; Randal May; Nathaniel Weygant; Dongfeng Qu; William R. Berry; Kamille Pitts; Ben Z. Stanger; Chinthalapally V. Rao; Michael S. Bronze; Courtney W. Houchen
Blockade of Cell Volume Regulatory Protein NKCC1 Increases TMZ-Induced Glioma Apoptosis and Reduces Astrogliosis
Lanxin Luo; Xiudong Guan; Gulnaz Begum; Dawei Ding; Jenesis Gayden; Md Nabiul Hasan; Victoria M. Fiesler; Jacob Dodelson; Gary Kohanbash; Baoli Hu; Nduka M. Amankulor; Wang Jia; Maria G. Castro; Baoshan Sun; Dandan Sun
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