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1 April 2022
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Cover Image
Cover Image
In this volume of Molecular Cancer Therapeutics, Cole and colleagues have identified a novel small molecule, (+)-JJ-74-138, that directly binds to the androgen receptor (AR) and non-competitively inhibits AR activity. Non-competitive AR inhibitor (+)-JJ-74-138 suppresses AR activity by preferentially increasing degradation of unliganded AR in the nucleus, inhibiting liganded AR recruitment to promoters, and inhibiting both AR and ARv7 transcriptional activity. Read the full article on page 483. - PDF Icon PDF LinkTable of Contents
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ISSN 1535-7163
EISSN 1538-8514
Highlights
MCT First Disclosures
Review
Small Molecule Therapeutics
Acquired Resistance to EZH2 Inhibitor GSK343 Promotes the Differentiation of Human DLBCL Cell Lines toward an ABC-Like Phenotype
Samuel E.J. Preston; Audrey Emond; Filippa Pettersson; Daphné Dupéré-Richer; Madelyn Jean Abraham; Alberto Riva; Mena Kinal; Ryan N. Rys; Nathalie A. Johnson; Koren K. Mann; Sonia V. del Rincón; Jonathan D. Licht; Wilson H. Miller, Jr
Dual G9A/EZH2 Inhibition Stimulates Antitumor Immune Response in Ovarian High-Grade Serous Carcinoma
Pavlina Spiliopoulou; Sarah Spear; Hasan Mirza; Ian Garner; Lynn McGarry; Fabio Grundland-Freile; Zhao Cheng; Darren P. Ennis; Nayana Iyer; Sophie McNamara; Marina Natoli; Susan Mason; Karen Blyth; Peter D. Adams; Patricia Roxburgh; Matthew J. Fuchter; Bob Brown; Iain A. McNeish
A Prostate-Specific Membrane Antigen—Targeted Near-Infrared Conjugate for Identifying Pulmonary Squamous Cell Carcinoma during Resection
Gregory T. Kennedy; Feredun S. Azari; Elizabeth Bernstein; Bilal Nadeem; Ashley E. Chang; Alix Segil; Neil Sullivan; Isvita Marfatia; Azra Din; Charuhas Desphande; John C. Kucharczuk; Philip S. Low; Sunil Singhal
The DNA-PK Inhibitor AZD7648 Sensitizes Patient-Derived Ovarian Cancer Xenografts to Pegylated Liposomal Doxorubicin and Olaparib Preventing Abdominal Metastases
Alessia Anastasia; Giulia Dellavedova; Antonio Ramos-Montoya; Neil James; Giovanna Chiorino; Massimo Russo; Hana Baakza; Joanne Wilson; Carmen Ghilardi; Elaine B. Cadogan; Raffaella Giavazzi; Maria Rosa Bani
PhAc-ALGP-Dox, a Novel Anticancer Prodrug with Targeted Activation and Improved Therapeutic Index
Andrea Casazza; Lawrence Van Helleputte; Britt Van Renterghem; Peter Pokreisz; Natalie De Geest; Marzia De Petrini; Tom Janssens; Marijke Pellens; Marjan Diricx; Carla Riera-Domingo; Agnieszka Wozniak; Massimiliano Mazzone; Patrick Schöffski; Olivier Defert; Geert Reyns; Nele Kindt
Large Molecule Therapeutics
Preclinical Development of ADCT-601, a Novel Pyrrolobenzodiazepine Dimer-based Antibody–drug Conjugate Targeting AXL-expressing Cancers
Francesca Zammarchi; Karin EG. Havenith; Simon Chivers; Paul Hogg; Francois Bertelli; Peter Tyrer; Narinder Janghra; Halla W. Reinert; John A. Hartley; Patrick H. van Berkel
Functional Genomic Identification of Predictors of Sensitivity and Mechanisms of Resistance to Multivalent Second-Generation TRAIL-R2 Agonists
Vera Grinkevitch; Mark Wappett; Nyree Crawford; Stacey Price; Andrea Lees; Christopher McCann; Katherine McAllister; Jochen Prehn; Jamie Young; Jess Bateson; Lewis Gallagher; Magali Michaut; Vivek Iyer; Aikaterini Chatzipli; Syd Barthorpe; Daniel Ciznadija; Ido Sloma; Amy Wesa; David A. Tice; Lodewyk Wessels; Mathew Garnett; Daniel B. Longley; Ultan McDermott; Simon S. McDade
Microneedle-mediated Intratumoral Delivery of Anti-CTLA-4 Promotes cDC1-dependent Eradication of Oral Squamous Cell Carcinoma with Limited irAEs
Mara Gilardi; Robert Saddawi-Konefka; Victoria H. Wu; Miguel Angel Lopez-Ramirez; Zhiyong Wang; Fernando Soto; Dana J. Ramms; Marco Proietto; Zbigniew Mikulski; Haruka Miki; Andrew Sharabi; Daniel Kupor; Ricardo Rueda; Daniel P. Hollern; Joseph Wang; J. Silvio Gutkind
A First-in-Human, Phase I, Multicenter, Open-Label, Dose-Escalation Study of PCA062: An Antibody–Drug Conjugate Targeting P-Cadherin, in Patients With Solid Tumors
Matteo Duca; Darren Wan-Teck Lim; Vivek Subbiah; Shunji Takahashi; John Sarantopoulos; Andrea Varga; Joseph A. D'Alessio; Tinya Abrams; Qing Sheng; Eugene Youchin Tan; Maria Santos Rosa; Juan Gonzalez-Maffe; Janna Sand-Dejmek; Claire Fabre; Miguel Martin
DS-7300a, a DNA Topoisomerase I Inhibitor, DXd-Based Antibody–Drug Conjugate Targeting B7-H3, Exerts Potent Antitumor Activities in Preclinical Models
Michiko Yamato; Jun Hasegawa; Takanori Maejima; Chiharu Hattori; Kazuyoshi Kumagai; Akiko Watanabe; Yumi Nishiya; Tomoko Shibutani; Tetsuo Aida; Ichiro Hayakawa; Takashi Nakada; Yuki Abe; Toshinori Agatsuma
Companion Diagnostic, Pharmacogenomic, and Cancer Biomarkers
Targeting Drug Resistance
HER2 Mediates PSMA/mGluR1-Driven Resistance to the DS-7423 Dual PI3K/mTOR Inhibitor in PTEN Wild-type Prostate Cancer Models
Valentí Gómez; Myria Galazi; Gregory Weitsman; James Monypenny; Fahad Al-Salemee; Paul R. Barber; Kenrick Ng; Richard Beatson; Bálint Szokol; László Orfi; Greg Mullen; Bart Vanhaesebroeck; Simon Chowdhury; Hing Y. Leung; Tony Ng
Models and Technologies
Tumor Targeting with Bacterial Shiga Toxin B Subunit in Genetic Porcine Models for Colorectal Cancer and Osteosarcoma
Maximilian Ehrenfeld; Anna Schrade; Tatiana Flisikowska; Markus Perl; Noah-David Hirsch; Anna Sichler; Laura Geyer; Krzysztof Flisikowski; Dirk Wilhelm; Sebastian Johannes Schober; Ludger Johannes; Angelika Schnieke; Klaus-Peter Janssen
Correction
Correction: Protein Phosphatase 2A as a Therapeutic Target in Small Cell Lung Cancer
Tamara Mirzapoiazova; Gang Xiao; Bolot Mambetsariev; Mohd W. Nasser; Emily Miaou; Sharad S. Singhal; Saumya Srivastava; Isa Mambetsariev; Michael S. Nelson; Arin Nam; Amita Behal; Leonidas D. Arvanitis; Pranita Atri; Markus Muschen; François L.H. Tissot; James Miser; John S. Kovach; Martin Sattler; Surinder K. Batra; Prakash Kulkarni; Ravi Salgia
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