Cell-Based Methods for the Identification of Myc-Inhibitory Small Molecules

• Published in: Methods in molecular biology (Clifton, N.J.) Vol. 2318; p. 337
• Main Authors: Burkhart, Catherine A, Haber, Michelle, Norris, Murray D, Gudkov, Andrei V, Nikiforov, Mikhail A
• Format: Journal Article
• Language: English
• Published: United States 2021
• Subjects: Cell Line, Tumor; Drug Screening Assays, Antitumor - methods; Genes, myc - drug effects; Genes, myc - genetics; Genes, myc - physiology; Humans; Oncogene Proteins - drug effects; Oncogene Proteins - metabolism; Proto-Oncogene Proteins c-myc - antagonists & inhibitors; Proto-Oncogene Proteins c-myc - genetics; Proto-Oncogene Proteins c-myc - metabolism; Small Molecule Libraries - pharmacology; Transcription Factors - drug effects; Transcription Factors - metabolism; Small molecules; Functional screening; MYCN; c-Myc; Cell-based assays
• ISSN: 1940-6029
• DOI: 10.1007/978-1-0716-1476-1_19

Oncoproteins encoded by dominant oncogenes have long been considered as targets for chemotherapeutic intervention. However, oncogenic transcription factors have often been dismissed as "undruggable." Members of the Myc family of transcription factors have been identified as promising targets for cancer chemotherapy in multiple publications reporting the requirement of Myc proteins for maintenance of almost every type of tumor. Here, we describe cell-based approaches to identify c-Myc small molecule inhibitors by screening complex libraries of diverse small molecules based on Myc functionality and specificity.