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1 January 2024
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SWTX-143, a TEAD palmitoylation pocket inhibitor, blocks Hippo pathway output and caused tumor regression in preclinical models of mesothelioma, a cancer that is frequently driven by mutations in Hippo pathway components. Read the full article on page 3. - PDF Icon PDF LinkTable of Contents
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ISSN 1535-7163
EISSN 1538-8514
Highlights
First Disclosure
A Novel Irreversible TEAD Inhibitor, SWTX-143, Blocks Hippo Pathway Transcriptional Output and Causes Tumor Regression in Preclinical Mesothelioma Models
Hanne Hillen; Aurélie Candi; Bart Vanderhoydonck; Weronika Kowalczyk; Leticia Sansores-Garcia; Elena C. Kesikiadou; Leen Van Huffel; Lore Spiessens; Marnik Nijs; Erik Soons; Wanda Haeck; Hugo Klaassen; Wim Smets; Stéphane A. Spieser; Arnaud Marchand; Patrick Chaltin; Fabrice Ciesielski; Francois Debaene; Lei Chen; Adeela Kamal; Stephen L. Gwaltney; Matthias Versele; Georg A. Halder
Review
Small Molecule Therapeutics
Targeting DNA Repair and Survival Signaling in Diffuse Intrinsic Pontine Gliomas to Prevent Tumor Recurrence
Monika Sharma; Ivana Barravecchia; Robert Teis; Jeanette Cruz; Rachel Mumby; Elizabeth K. Ziemke; Carlos E. Espinoza; Varunkumar Krishnamoorthy; Brian Magnuson; Mats Ljungman; Carl Koschmann; Joya Chandra; Christopher E. Whitehead; Judith S. Sebolt-Leopold; Stefanie Galban
Bruton's Tyrosine Kinase Inhibitors with Distinct Binding Modes Reveal Differential Functional Impact on B-Cell Receptor Signaling
Wei Li; Renata Sano; Mutiah Apatira; Felix DeAnda; Tarikere Gururaja; Muhua Yang; Greta Lundgaard; Chin Pan; Jing Liu; Yongjiao Zhai; Woo Hyun Yoon; Longcheng Wang; Chris Tse; Andrew J. Souers; Chih-Hung Lee
Delivery versus Potency in Treating Brain Tumors: BI-907828, a MDM2-p53 Antagonist with Limited BBB Penetration but Significant In Vivo Efficacy in Glioblastoma
Wenjuan Zhang; Rachael A. Vaubel; Ju-Hee Oh; Ann C. Mladek; Surabhi Talele; Wenqiu Zhang; Katie L. Waller; Danielle M. Burgenske; Jann N. Sarkaria; William F. Elmquist
Large Molecule Therapeutics
Targeting NANOG and FAK via Cx26-derived Cell-penetrating Peptides in Triple-negative Breast Cancer
Erin E. Mulkearns-Hubert; Emily Esakov Rhoades; Salma Ben-Salem; Rashmi Bharti; Nicole Hajdari; Sadie Johnson; Alex Myers; Iris Nira Smith; Smarajit Bandyopadhyay; Charis Eng; Erinn Downs; Justin D. Lathia; Ofer Reizes
Brentuximab Vedotin–Driven Microtubule Disruption Results in Endoplasmic Reticulum Stress Leading to Immunogenic Cell Death and Antitumor Immunity
Ryan A. Heiser; Anthony T. Cao; Weiping Zeng; Michelle Ulrich; Patrick Younan; Martha E. Anderson; Esther S. Trueblood; Mechthild Jonas; Robert Thurman; Che-Leung Law; Shyra J. Gardai
Site-Specific Dolasynthen Antibody–Drug Conjugates Exhibit Consistent Pharmacokinetic Profiles across a Wide Range of Drug-to-Antibody Ratios
Susan M. Clardy; Alex Uttard; Bingfan Du; Kalli C. Catcott; Kelly L. Lancaster; Elizabeth Ditty; Jack Sadowsky; Jeffrey Zurita; Naniye Malli; LiuLiang Qin; Stephen P. Bradley; Kenneth Avocetien; Tyler Carter; Dokyong Kim; Mark Nazzaro; Ling Xu; Thomas H. Pillow; Neelie T. Zacharias; Gail D. Lewis; Rebecca K. Rowntree; Radha Iyengar; David H. Lee; Marc Damelin; Dorin Toader; Timothy B. Lowinger
Targeting Drug Resistance
Companion Diagnostic, Pharmacogenomic, and Cancer Biomarkers
SLFN11 is a BRCA Independent Biomarker for the Response to Platinum-Based Chemotherapy in High-Grade Serous Ovarian Cancer and Clear Cell Ovarian Carcinoma
Hidehiko Akashi; Nozomi Yachida; Haruka Ueda; Manako Yamaguchi; Kaoru Yamawaki; Ryo Tamura; Kazuaki Suda; Tatsuya Ishiguro; Sosuke Adachi; Yoshikazu Nagase; Yutaka Ueda; Masashi Ueda; Kaoru Abiko; Masahiro Kagabu; Tsukasa Baba; Hirofumi Nakaoka; Takayuki Enomoto; Junko Murai; Kosuke Yoshihara
Acknowledgment to Reviewers
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