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Published on: October 30, 2013
Chemical intervention strategies targeting MYC for cancer therapy
Dan Wu1, Yuxuan Zhu2, Mengjie Ye1
1Jiangsu Key Laboratory of Drug Design and Optimization and State Key Laboratory of Natural Medicines, China Pharmaceutical University, Nanjing 210009, China; Department of Medicinal Chemistry, School of Pharmacy, China Pharmaceutical University, Nanjing 210009, China.
Abstract:
MYC, a multifunctional transcription factor overexpressed in cancers, has a crucial role in tumor initiation, maintenance, and progression. However, because of the lack of enzymatic activity and small molecule-binding sites, MYC has been considered a challenging target, against which there are currently no clinically approved drugs. In this review, we outline the biological functions and regulatory networks of MYC, discuss potential chemical intervention strategies for its inhibition, and summarize reported therapeutic molecules, to provide insights for future developments targeting MYC for cancer therapy.
Insights
MYC is a key cancer-driving transcription factor, but difficult to target. This review explores MYC
Area of Science:
- Oncology
- Molecular Biology
- Drug Discovery
Background:
- The MYC oncoprotein is frequently overexpressed in various cancers.
- MYC plays a critical role in tumor initiation, maintenance, and progression.
- MYC lacks enzymatic activity and small molecule-binding sites, presenting a significant therapeutic challenge.
Purpose of the Study:
- To review the biological functions and regulatory networks of MYC.
- To discuss potential chemical strategies for MYC inhibition.
- To summarize existing therapeutic molecules targeting MYC for cancer treatment.
Main Methods:
- Literature review of MYC's biological roles.
- Analysis of chemical intervention strategies against MYC.
- Compilation of reported MYC-targeting therapeutic agents.
Main Results:
- MYC's multifaceted roles in cancer development are detailed.
- Various approaches for chemical inhibition of MYC are explored.
- A summary of current and potential MYC-targeting drugs is presented.
Conclusions:
- MYC remains a challenging but crucial target for cancer therapy.
- Understanding MYC's biology and regulatory networks is key to developing effective drugs.
- This review provides insights for future development of MYC-targeted cancer treatments.
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