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1 May 2024
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ZD060519 is a camptothecin-based topoisomerase 1 inhibitor designed for antibody drug conjugates. This payload was selected from a library of ∼100 analogs for its optimal potency, permeability, and other drug-like characteristics. Antibodies conjugated with ZD06519 display tumor-specific cytotoxicity in vitro, bystander activity, efficacy in multiple CDX and PDX models, and noteworthy tolerability in rodents and non-human primates. See graphical abstract and read the full article on page 606. - PDF Icon PDF LinkTable of Contents
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ISSN 1535-7163
EISSN 1538-8514
Highlights
First Disclosures
Pharmacological Characterization of SDX-7320/Evexomostat: A Novel Methionine Aminopeptidase Type 2 Inhibitor with Anti-tumor and Anti-metastatic Activity
Peter Cornelius; Benjamin A. Mayes; John S. Petersen; David J. Turnquist; Pierre J. Dufour; Andrew J. Dannenberg; James M. Shanahan; Bradley J. Carver
Design and Evaluation of ZD06519, a Novel Camptothecin Payload for Antibody Drug Conjugates
Mark E. Petersen; Michael G. Brant; Manuel Lasalle; Samir Das; Renee Duan; Jodi Wong; Tong Ding; Kaylee J. Wu; Dayananda Siddappa; Chen Fang; Wen Zhang; Alex M. L. Wu; Truman Hirkala-Schaefer; Graham A. E. Garnett; Vincent Fung; Luying Yang; Andrea Hernandez Rojas; Samuel O. Lawn; Stuart D. Barnscher; Jamie R. Rich; Raffaele Colombo
Commentary
Reviews
Small Molecule Therapeutics
The Antipsychotic Drug Penfluridol Inhibits N-Linked Glycoprotein Processing and Enhances T-cell–Mediated Tumor Immunity
Wenlong Xu; Yuqi Wang; Na Zhang; Xiaofeng Lin; Di Zhu; Cheng Shen; Xiaobo Wang; Haiyang Li; Jinjiang Xue; Qian Yu; Xinyi Lu; Lu Zhou; Qingli He; Zhijun Tang; Shaodan He; Jianjun Fan; Jianbo Pan; Jiangjiang Tang; Wei Jiang; Mingliang Ye; Fanghui Lu; Zengxia Li; Yongjun Dang
Differential Distribution of the DNA-PKcs Inhibitor Peposertib Selectively Radiosensitizes Patient-derived Melanoma Brain Metastasis Xenografts
Jianxiang Ji; Sonja Dragojevic; Cameron M. Callaghan; Emily J. Smith; Surabhi Talele; Wenjuan Zhang; Margaret A. Connors; Ann C. Mladek; Zeng Hu; Katrina K. Bakken; Paige P. Sarkaria; Brett L. Carlson; Danielle M. Burgenske; Paul A. Decker; Mohammad Abdur Rashid; Mi-hyeon Jang; Shiv K. Gupta; Jeanette E. Eckel-Passow; William F. Elmquist; Jann N. Sarkaria
4′-Ethynyl-2′-Deoxycytidine (EdC) Preferentially Targets Lymphoma and Leukemia Subtypes by Inducing Replicative Stress
Marissa L. Calbert; Gurushankar Chandramouly; Clare M. Adams; Magali Saez-Ayala; Tatiana Kent; Mrityunjay Tyagi; V.S.S. Abhinav Ayyadevara; Yifan Wang; John J. Krais; John Gordon; Jessica Atkins; Monika M. Toma; Stéphane Betzi; Andrew S. Boghossian; Matthew G. Rees; Melissa M. Ronan; Jennifer A. Roth; Aaron R. Goldman; Nicole Gorman; Ramkrishna Mitra; Wayne E. Childers; Xavier Graña; Tomasz Skorski; Neil Johnson; Christian Hurtz; Xavier Morelli; Christine M. Eischen; Richard T. Pomerantz
Targeting Drug Resistance
Darolutamide Added to Docetaxel Augments Antitumor Effect in Models of Prostate Cancer through Cell Cycle Arrest at the G1–S Transition
Stefan A.J. Buck; Annelies Van Hemelryk; Corrina de Ridder; Debra Stuurman; Sigrun Erkens-Schulze; Sem van ’t Geloof; Wilma J. Teubel; Stijn L.W. Koolen; Elena S. Martens-Uzunova; Martin E. van Royen; Ronald de Wit; Ron H.J. Mathijssen; Wytske M. van Weerden
Companion Diagnostic, Pharmacogenomic, and Cancer Biomarkers
Correction
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