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Published on: January 22, 2019
Cell-based methods for the identification of MYC-inhibitory small molecules
Catherine A Burkhart1, Michelle Haber, Murray D Norris
1Cleveland BioLabs, Inc., Buffalo, NY, USA.
Methods in Molecular Biology (Clifton, N.J.)
|September 6, 2013
Summary
Researchers developed cell-based methods to find small molecule inhibitors targeting the Myc oncoprotein. This approach aims to overcome the challenge of targeting oncogenic transcription factors for cancer therapy.
Area of Science:
- Oncology
- Molecular Biology
- Drug Discovery
Background:
- Oncoproteins from dominant oncogenes are established therapeutic targets.
- Oncogenic transcription factors, like Myc, are crucial for tumor maintenance but historically deemed 'undruggable'.
- Myc family proteins are implicated in nearly all tumor types, presenting a significant therapeutic opportunity.
Purpose of the Study:
- To establish cell-based screening approaches for identifying novel small molecule inhibitors of c-Myc.
- To address the challenge of targeting oncogenic transcription factors in cancer chemotherapy.
Main Methods:
- Development of cell-based assays focused on Myc functionality.
- Screening of diverse, complex small molecule libraries.
- Selection of inhibitors based on Myc specificity and functional impact.
Main Results:
- Successful identification of small molecules that inhibit Myc functionality through cell-based screening.
- Demonstration of a viable strategy for targeting oncogenic transcription factors.
Conclusions:
- Cell-based screening is an effective strategy for discovering inhibitors of challenging targets like Myc.
- This work provides a foundation for developing new cancer therapeutics targeting Myc.
