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Updated: Nov 25, 2025

Defining Gene Functions in Tumorigenesis by Ex vivo Ablation of Floxed Alleles in Malignant Peripheral Nerve Sheath Tumor Cells
Published on: August 25, 2021
The Molecular 'Myc-anisms' Behind Myc-Driven Tumorigenesis and the Relevant Myc-Directed Therapeutics
Jessica McAnulty1, Analisa DiFeo1
1Department of Pathology, University of Michigan, Ann Arbor, MI 48109, USA.
Abstract:
MYC, a well-studied proto-oncogene that is overexpressed in >20% of tumors across all cancers, is classically known as "undruggable" due to its crucial roles in cell processes and its lack of a drug binding pocket. Four decades of research and creativity led to the discovery of a myriad of indirect (and now some direct!) therapeutic strategies targeting Myc. This review explores the various mechanisms in which Myc promotes cancer and highlights five key therapeutic approaches to disrupt Myc, including transcription, Myc-Max dimerization, protein stability, cell cycle regulation, and metabolism, in order to develop more specific Myc-directed therapies.
Insights
Myc, a proto-oncogene overexpressed in many cancers, is challenging to target. This review explores five key therapeutic strategies to disrupt Myc
Area of Science:
- Oncology
- Molecular Biology
- Drug Discovery
Background:
- The MYC proto-oncogene is overexpressed in over 20% of human cancers.
- MYC is considered
- undruggable
- due to its essential cellular functions and lack of a defined drug-binding pocket.
Purpose of the Study:
- To review the mechanisms by which MYC drives cancer progression.
- To highlight key therapeutic strategies for targeting MYC.
- To inform the development of novel MYC-directed cancer therapies.
Main Methods:
- Literature review of MYC's role in cancer.
- Analysis of established and emerging therapeutic strategies targeting MYC.
- Categorization of therapies based on the targeted mechanism.
Main Results:
- MYC promotes cancer through various mechanisms, including transcriptional regulation, protein interactions, and metabolic reprogramming.
- Five key therapeutic approaches to disrupt MYC are identified: targeting transcription, MYC-MAX dimerization, protein stability, cell cycle regulation, and metabolism.
- Both indirect and direct therapeutic strategies have been developed.
Conclusions:
- Despite its historical
- undruggable
- status, significant progress has been made in developing MYC-targeting therapies.
- Further research into these five key therapeutic areas holds promise for more specific and effective cancer treatments.
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