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Cell-Based Methods for the Identification of Myc-Inhibitory Small Molecules
Catherine A Burkhart1, Michelle Haber2, Murray D Norris2
1Buffalo BioLabs, Inc., Buffalo, NY, USA.
Methods in Molecular Biology (Clifton, N.J.)
|May 21, 2021
Summary
Researchers screened for small molecule inhibitors targeting the Myc family of transcription factors, which are crucial for tumor maintenance. This cell-based approach aims to overcome the challenge of targeting "undruggable" oncogenic transcription factors for cancer therapy.
Area of Science:
- Oncology
- Molecular Biology
- Drug Discovery
Background:
- Oncoproteins from dominant oncogenes are established chemotherapeutic targets.
- Oncogenic transcription factors, like Myc, are essential for tumor cell survival but historically considered difficult to target.
- The Myc family of transcription factors is implicated in the maintenance of most tumor types.
Purpose of the Study:
- To develop cell-based methods for identifying small molecule inhibitors of c-Myc.
- To screen diverse chemical libraries for compounds that specifically inhibit Myc functionality.
Main Methods:
- Utilized cell-based screening assays.
- Employed diverse small molecule libraries.
- Focused on Myc functionality and specificity for inhibitor identification.
Main Results:
- Successfully developed and applied cell-based approaches to identify potential c-Myc inhibitors.
- Demonstrated the feasibility of screening for inhibitors targeting oncogenic transcription factors.
Conclusions:
- Cell-based screening offers a viable strategy for discovering inhibitors of challenging targets like c-Myc.
- This approach holds promise for developing novel cancer chemotherapeutics targeting Myc-dependent tumors.
