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1 November 2022
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ST101 Mechanism of Action: C/EBPβ drives tumor progression by inducing expression of target genes responsible for survival and proliferation. ST101, a first-in-class C/EBPβ antagonist, prevents its dimerization and enhances ubiquitin-proteasome dependent C/EBPβ degradation. The result of ST101 exposure is attenuated expression of C/EBPβ target genes and selective cytotoxicity in tumor cells while normal cells are not impacted. ST101 is currently being evaluated in the Phase 2 portion of an ongoing Phase 1-2 clinical study in patients with advanced unresectable and metastatic solid tumors (NCT04478279). Clinical proof-of-concept has been shown with a mRANO-confirmed partial response in a patient with recurrent GBM, a durable RECIST 1.1-confirmed partial response in a patient with cutaneous melanoma and long-lasting stable disease in several additional patients. Read the full article on page 1632. - PDF Icon PDF LinkTable of Contents
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ISSN 1535-7163
EISSN 1538-8514
Highlights
Editorial
The AACR Journals: Advancing Progress Toward the AACR's 115-Year Mission
Kenneth C. Anderson; Lewis C. Cantley; Riccardo Dalla-Favera; Chi Van Dang; Luis A. Diaz; Raymond N. DuBois; Keith T. Flaherty; Philip D. Greenberg; Massimo Loda; Elaine R. Mardis; Elizabeth A. Platz; Michael N. Pollak; Robert D. Schreiber; Lillian L. Siu; Beverly A. Teicher
MCT First Disclosures
Review
Small Molecule Therapeutics
Sustained Supratherapeutic Paclitaxel Delivery Enhances Irreversible Sarcoma Cell Death
William A. Blessing; Christopher S. Digesu; Rong Liu; David A. Mahvi; Aya Tal-mason; Anil Kumar; Krista J. Hachey; Aaron H. Colby; Jenny T. Korunes-Miller; Natalie Agar; Michael S. Regan; Angela Shih; Chandrajit P. Raut; Mark W. Grinstaff; Yolonda L. Colson
Establishment and Evaluation of Dual HDAC/BET Inhibitors as Therapeutic Options for Germ Cell Tumors and Other Urological Malignancies
Aaron Burmeister; Alexa Stephan; Leandro A. Alves Avelar; Melanie R. Müller; Andrea Seiwert; Stefan Höfmann; Fabian Fischer; Hector Torres-Gomez; Michèle J. Hoffmann; Guenter Niegisch; Felix Bremmer; Patrick Petzsch; Karl Köhrer; Peter Albers; Thomas Kurz; Margaretha A. Skowron; Daniel Nettersheim
p53 Pathway Inactivation Drives SMARCB1-deficient p53-wildtype Epithelioid Sarcoma Onset Indicating Therapeutic Vulnerability Through MDM2 Inhibition
Felix Oppel; Senyao Shao; Sarah Gendreizig; Mark W. Zimmerman; Matthias Schürmann; Viyof Ful Flavian; Peter Goon; Susan N. Chi; Jon C. Aster; Holger Sudhoff; A. Thomas Look
Large Molecule Therapeutics
PLX038: A Long-Acting Topoisomerase I Inhibitor With Robust Antitumor Activity in ATM-Deficient Tumors and Potent Synergy With PARP Inhibitors
Anish Thomas; Shaun D. Fontaine; Morgan E. Diolaiti; Parth Desai; Rajesh Kumar; Nobuyuki Takahashi; Linda Sciuto; Samantha Nichols; Alan Ashworth; Felix Y. Feng; Gary W. Ashley; Minh Nguyen; Yves Pommier; Daniel V. Santi
Targeting Drug Resistance
Tumor-Infiltrating Myeloid Cells Confer De Novo Resistance to PD-L1 Blockade through EMT–Stromal and Tgfβ-Dependent Mechanisms
Haocheng Yu; John P. Sfakianos; Li Wang; Yang Hu; Jorge Daza; Matthew D. Galsky; Harkirat S. Sandhu; Olivier Elemento; Bishoy M. Faltas; Adam M. Farkas; Nina Bhardwaj; Jun Zhu; David J. Mulholland
Letter to the Editor
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NOTICE: This notice serves to inform the reader that, in 2023, AACR received a donation by Pfizer of the rights to royalties from the sale—within the United States—of Bavencio® (avelumab), a pharmaceutical owned by Merck. None of these funds are being, or will be, used to directly support any specific publication or author. If an individual article is published that deals with this particular drug, such article will include standard financial disclosures per AACR journal policy. For more detail regarding AACR’s established policies for authors, please go to https://aacrjournals.org/pages/editorial-policies#coi.