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Published on: November 9, 2020
Molecular targeting of E3 ligases--a therapeutic approach for cancer
Manikandan Lakshmanan1, Usha Bughani, Senthil Duraisamy
1Ranbaxy Laboratories Ltd, New Drug Discovery Research, R&D-III, Sector-18, Plot No. 20, Gurgaon-122015, India.
Background:
The ubiquitin-proteasomal degradation pathway plays a critical role in protein degradation and regulates a wide variety of cellular functions. This highly conserved post-translational modification of proteolytic processes is mainly carried out by substrate-specific E3 ligases. The deregulation of E3 ligases contributes to cancer development and their overexpression is often associated with poor prognosis.
Objectives:
We review the current understanding of E3 ligases, their functional role in cancer pathogenesis, current progress and development of certain ubiquitin E3 ligases as targets for therapeutic intervention.
Methods:
Preclinical and clinical data for E3 ligase inhibitors available in the public domain are discussed.
Conclusions:
With the growing understanding of their role in cancer development and progression, E3 ligases have emerged as potential anticancer targets for therapeutic intervention.
Insights
E3 ligases are crucial for protein degradation and their dysregulation drives cancer. Targeting these ubiquitin ligases shows promise as a new anticancer therapeutic strategy.
Area of Science:
- Biochemistry
- Molecular Biology
- Oncology
Background:
- The ubiquitin-proteasomal degradation pathway is vital for cellular function, regulated by E3 ligases.
- E3 ligase deregulation is linked to cancer development and poor patient prognosis.
Purpose of the Study:
- To review the current understanding of E3 ligases.
- To explore their role in cancer pathogenesis.
- To discuss their therapeutic potential as anticancer targets.
Main Methods:
- Review of preclinical and clinical data on E3 ligase inhibitors.
- Analysis of publicly available data.
Main Results:
- E3 ligases are key regulators in cancer development.
- Targeting E3 ligases represents a promising therapeutic avenue.
Conclusions:
- E3 ligases are emerging as significant anticancer targets.
- Further understanding of their role supports therapeutic intervention.
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