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1 June 2021
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An X-ray crystal structure of auto-palmitoylation inhibitor VT105 bound to TEAD3. On page 986, researchers at Vivace Therapeutics report discovery and optimization of TEAD auto-palmitoylation inhibitors that selectively inhibit proliferation and tumor growth of NF2-deficient mesothelioma. These auto-palmitoylation inhibitors present an opportunity to treat cancers and other diseases that arise from abnormal inactivation of the Hippo signaling pathway.Close Modal - PDF Icon PDF LinkTable of Contents
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ISSN 1535-7163
EISSN 1538-8514
Highlights
Review
Small Molecule Therapeutics
The KRASG12C Inhibitor MRTX849 Reconditions the Tumor Immune Microenvironment and Sensitizes Tumors to Checkpoint Inhibitor Therapy
David M. Briere; Shuai Li; Andrew Calinisan; Niranjan Sudhakar; Ruth Aranda; Lauren Hargis; David H. Peng; Jiehui Deng; Lars D. Engstrom; Jill Hallin; Sole Gatto; Julio Fernandez-Banet; Adam Pavlicek; Kwok-Kin Wong; James G. Christensen; Peter Olson
Expanding the Repertoire for “Large Small Molecules”: Prodrug ABBV-167 Efficiently Converts to Venetoclax with Reduced Food Effect in Healthy Volunteers
Ahmed Hamed Salem; Zhi-Fu Tao; Orlando F. Bueno; Jie Chen; Shuang Chen; Rohinton Edalji; Steven W. Elmore; Keith M. Fournier; Kaid C. Harper; Richard Hong; Gary J. Jenkins; Jianguo Ji; Russell A. Judge; John C. Kalvass; Russell C. Klix; Yi-Yin Ku; Joel D. Leverson; Richard A. Marks; Kennan C. Marsh; Rajeev M. Menon; Chang H. Park; Darren C. Phillips; Yu-Ming Pu; Saul H. Rosenberg; Yeshwant D. Sanzgiri; Ahmad Y. Sheikh; Yi Shi; Deanne Stolarik; Ahmed A. Suleiman; Xilu Wang; Geoff G.Z. Zhang; Nathaniel D. Catron; Andrew J. Souers
In Vivo Efficacy of Tesevatinib in EGFR-Amplified Patient-Derived Xenograft Glioblastoma Models May Be Limited by Tissue Binding and Compensatory Signaling
Sani H. Kizilbash; Shiv K. Gupta; Karen E. Parrish; Janice K. Laramy; Minjee Kim; Gautham Gampa; Brett L. Carlson; Katrina K. Bakken; Ann C. Mladek; Mark A. Schroeder; Paul A. Decker; William F. Elmquist; Jann N. Sarkaria
Conophylline Inhibits Hepatocellular Carcinoma by Inhibiting Activated Cancer-associated Fibroblasts Through Suppression of G Protein–coupled Receptor 68
Takahiro Yamanaka; Norifumi Harimoto; Takehiko Yokobori; Ryo Muranushi; Kouki Hoshino; Kei Hagiwara; Dolgormaa Gantumur; Tadashi Handa; Norihiro Ishii; Mariko Tsukagoshi; Takamichi Igarashi; Akira Watanabe; Norio Kubo; Kenichiro Araki; Kazuo Umezawa; Ken Shirabe
Enhancing Proteotoxic Stress in Leiomyosarcoma Cells Triggers Mitochondrial Dysfunctions, Cell Death, and Antitumor Activity in vivo
Luca Iuliano; Sara Drioli; Ymera Pignochino; Claudia Maria Cafiero; Martina Minisini; Francesca D'Este; Raffaella Picco; Emiliano Dalla; Giorgia Giordano; Giovanni Grignani; Eros Di Giorgio; Fabio Benedetti; Fulvia Felluga; Claudio Brancolini
Activity of Combined Androgen Receptor Antagonism and Cell Cycle Inhibition in Androgen Receptor Positive Triple Negative Breast Cancer
Jessica L. Christenson; Kathleen I. O'Neill; Michelle M. Williams; Nicole S. Spoelstra; Kenneth L. Jones; G. Devon Trahan; Jordan Reese; Elaina T. Van Patten; Anthony Elias; Joel R. Eisner; Jennifer K. Richer
Macrophage Activation Status Rather than Repolarization Is Associated with Enhanced Checkpoint Activity in Combination with PI3Kγ Inhibition
Larissa S. Carnevalli; Molly A. Taylor; Matthew King; Anna M.L. Coenen-Stass; Adina M. Hughes; Sigourney Bell; Theresa A. Proia; Yanjun Wang; Antonio Ramos-Montoya; Neha Wali; Danielle Carroll; Maneesh Singh; Michele Moschetta; Pablo Morentin Gutierrez; Cristina Gardelli; Susan E. Critchlow; Teresa Klinowska; Stephen E. Fawell; Simon T. Barry
Large Molecule Therapeutics
Novel TGFβ Inhibitors Ameliorate Oral Squamous Cell Carcinoma Progression and Improve the Antitumor Immune Response of Anti–PD-L1 Immunotherapy
Nils Ludwig; Łukasz Wieteska; Cynthia S. Hinck; Saigopalakrishna S. Yerneni; Juliana H. Azambuja; Richard J. Bauer; Torsten E. Reichert; Andrew P. Hinck; Theresa L. Whiteside
Calicheamicin Antibody–Drug Conjugates with Improved Properties
Breanna S. Vollmar; Chris Frantz; Melissa M. Schutten; Fiona Zhong; Geoffrey del Rosario; Mary Ann T. Go; Shang-Fan Yu; Douglas D. Leipold; Amrita V. Kamath; Carl Ng; Keyang Xu; Josefa dela Cruz-Chuh; Katherine R. Kozak; Jinhua Chen; Zijin Xu; John Wai; Pragya Adhikari; Hans K. Erickson; Peter S. Dragovich; Andrew G. Polson; Thomas H. Pillow
A Novel Therapeutic Anti-ErbB3, ISU104 Exhibits Potent Antitumorigenic Activity by Inhibiting Ligand Binding and ErbB3 Heterodimerization
Mirim Hong; Youngki Yoo; Miyoung Kim; Ju Yeon Kim; Jeong Seok Cha; Myung Kyung Choi; Uijin Kim; Kyungyong Kim; Youngsoo Sohn; Donggoo Bae; Hyun-Soo Cho; Seung-Beom Hong
Companion Diagnostic, Pharmacogenomic, and Cancer Biomarkers
RNA-Binding Protein Polymorphisms as Novel Biomarkers to Predict Outcomes of Metastatic Colorectal Cancer: A Meta-analysis from TRIBE, FIRE-3, and MAVERICC
Hiroyuki Arai; Shu Cao; Francesca Battaglin; Jingyuan Wang; Natsuko Kawanishi; Ryuma Tokunaga; Fotios Loupakis; Sebastian Stintzing; Shivani Soni; Wu Zhang; Christoph Mancao; Bodour Salhia; Shannon M. Mumenthaler; Chiara Cremolini; Volker Heinemann; Alfredo Falcone; Joshua Millstein; Heinz-Josef Lenz
Cancer Biology and Translational Studies
Author Choice
High-Throughput Screening Identifies Idasanutlin as a Resensitizing Drug for Venetoclax-Resistant Neuroblastoma Cells
Lindy Vernooij; Laurel T. Bate-Eya; Lindy K. Alles; Jasmine Y. Lee; Bianca Koopmans; Hunter C. Jonus; Nil A. Schubert; Linda Schild; Daphne Lelieveld; David A. Egan; Mark Kerstjens; Ronald W. Stam; Jan Koster; Kelly C. Goldsmith; Jan J. Molenaar; M. Emmy M. Dolman
Targeted Therapy to β3 Integrin Reduces Chemoresistance in Breast Cancer Bone Metastases
Gregory C. Fox; Xinming Su; Jennifer L. Davis; Yalin Xu; Kristin A. Kwakwa; Michael H. Ross; Francesca Fontana; Jingyu Xiang; Alison K. Esser; Elizabeth Cordell; Kristen Pagliai; Ha X. Dang; Jothilingam Sivapackiam; Sheila A. Stewart; Christopher A. Maher; Suzanne J. Bakewell; James A.J. Fitzpatrick; Vijay Sharma; Samuel Achilefu; Deborah J. Veis; Gregory M. Lanza; Katherine N. Weilbaecher
Models and Technologies
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