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1 December 2024
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Cover Image
MDM2 suppresses p53 activity, leading to uncontrolled cell replication. The MDM2–p53 antagonist brigimadlin (BI 907828) disrupts the MDM2–p53 interaction, thereby restoring p53 function in TP53 wild-type tumors. See graphical abstract and the full article on page 1689. - PDF Icon PDF LinkTable of Contents
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ISSN 1535-7163
EISSN 1538-8514
Highlights
First Disclosures
Discovery and Characterization of Brigimadlin, a Novel and Highly Potent MDM2–p53 Antagonist Suitable for Intermittent Dose Schedules
Andreas Gollner; Dorothea Rudolph; Ulrike Weyer-Czernilofsky; Rosa Baumgartinger; Peter Jung; Harald Weinstabl; Jürgen Ramharter; Rolf Grempler; Jens Quant; Jörg Rinnenthal; Alejandro Pérez Pitarch; Bojana Golubovic; Daniel Gerlach; Gerd Bader; Kristiane Wetzel; Sebastian Otto; Christian Mandl; Guido Boehmelt; Darryl B. McConnell; Norbert Kraut; Patrizia Sini
Discovery of RGT-018: A Potent, Selective, and Orally Bioavailable SOS1 Inhibitor for KRAS-Driven Cancers
Fei Xiao; Kailiang Wang; Xinjuan Wang; Huijuan Li; Zhilong Hu; Xiaoming Ren; Wei Huang; Teng Feng; Lili Yao; Jing Lin; Chunlai Li; Zhuanzhuan Zhang; Liufeng Mei; Xiaotian Zhu; Wenge Zhong; Zhi Xie
Review
Small Molecule Therapeutics
Targeting the Synthetic Lethal Relationship between FOCAD and TUT7 Represents a Potential Therapeutic Opportunity for TUT4/7 Small-Molecule Inhibitors in Cancer
Robinson Triboulet; Khikmet Sadykov; Darren M. Harvey; David M. Wilson; Michael J. Steinbaugh; Christopher B. Mayo; Dillon Hawley; Andrew Madanjian; Corey Fyfe; Christina Bracken; Izarys Rivera-Rivera; Anna Ericsson; Andrew R. Snyder; Sarah K. Knutson; Ross L. Stein; Veronica Gibaja; Shomir Ghosh; Robert M. Campbell
Large Molecule Therapeutics
Integrated Imaging Probe and Bispecific Antibody Development Enables In Vivo Targeting of Glypican-3–Expressing Hepatocellular Carcinoma
Peiman Habibollahi; Alexey Gurevich; James Z. Hui; Kelly Weinfurtner; George McClung; Justin Adler; Michael C. Soulen; David E. Kaplan; Gregory J. Nadolski; Stephen J. Hunt; Andrew Tsourkas; Terence P. Gade
Fatty Acid Derivatization and Cyclization of the Immunomodulatory Peptide RP-182 Targeting CD206high Macrophages Improve Antitumor Activity
Sitanshu S. Singh; Raul Calvo; Anju Kumari; Rushikesh V. Sable; Yuhong Fang; Dingyin Tao; Xin Hu; Sarah Gray Castle; Saifun Nahar; Dandan Li; Emily Major; Tino W. Sanchez; Rintaro Kato; Xin Xu; Jian Zhou; Liang Liu; Christopher A. LeClair; Anton Simeonov; Bolormaa Baljinnyam; Mark J. Henderson; Juan Marugan; Udo Rudloff
Preclinical Characterization of ARX517, a Site-Specific Stable PSMA-Targeted Antibody–Drug Conjugate for the Treatment of Metastatic Castration-Resistant Prostate Cancer
Lillian K. Skidmore; David Mills; Ji Young Kim; Nick A. Knudsen; Jay D. Nelson; Manoj Pal; Jianing Wang; Kedar GC; Michael J. Gray; Wisam Barkho; Prathap Nagaraja Shastri; Mysore P. Ramprasad; Feng Tian; Daniel O’Connor; Ying J. Buechler; Shawn Shao-Hui Zhang
Targeting Drug Resistance
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