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Telomerase as an anti-cancer target: current status and future prospects
1CRC Biomolecular Structure Unit, Institute of Cancer Research, Sutton, Surrey, UK.
Abstract:
As is common with a newly discovered cancer-associated gene/protein, there is a lag between the elucidation of its cellular and molecular biology and appropriate therapeutic intervention. Telomerase represents an interesting and promising anticancer drug target but poses a particular drug discovery challenge. It is unclear at present what is the optimum means of targeting this complex ribonucleoprotein and associated telomeric DNA and binding proteins: various strategies are actively being explored. Some recent data (e.g. 2-5A antisense against telomeric RNA, targeting TRF2, introduction of dominant-negative hTERT into cells) has raised doubts over the previously presumption of a requirement for prolonged enzyme inhibition with gradual telomere erosion, especially in tumour cells with relatively short telomeres. Highly potent and selective in vivo inhibitors are required to validate the target and address these critical issues.
Insights
Targeting telomerase, a cancer-associated protein, presents challenges for drug discovery. New research questions the need for prolonged inhibition, highlighting the need for potent in vivo inhibitors to validate telomerase as an anticancer target.
Area of Science:
- Oncology
- Molecular Biology
- Drug Discovery
Background:
- Cancer-associated genes require time for therapeutic development.
- Telomerase is a promising anticancer target but difficult to drug.
- Current strategies for targeting telomerase are under active investigation.
Purpose of the Study:
- To explore optimal strategies for targeting telomerase.
- To address challenges in telomerase-based cancer drug discovery.
- To investigate recent findings that question established therapeutic approaches.
Main Methods:
- Exploring various strategies for targeting telomerase.
- Investigating 2-5A antisense against telomeric RNA.
- Examining the targeting of TRF2 and dominant-negative hTERT introduction.
Main Results:
- Recent data raises doubts about the necessity of prolonged telomerase inhibition.
- The effectiveness of gradual telomere erosion is questioned, particularly in tumors with short telomeres.
- The need for potent and selective in vivo inhibitors is highlighted.
Conclusions:
- Further research is required to determine the optimal method for targeting telomerase.
- Potent and selective in vivo inhibitors are crucial for validating telomerase as a therapeutic target.
- New approaches may be needed to overcome existing challenges in telomerase-targeted cancer therapy.