Targeting telomerase for its advent in cancer therapeutics

Area of Science:

• Biochemistry
• Molecular Biology
• Oncology

Background:

• Telomerase is a reverse transcriptase enzyme essential for maintaining telomere length at chromosomal ends.
• It plays a critical role in cell aging, proliferation, and is implicated in unrestricted cell growth in cancers.
• Targeting telomerase is a significant strategy in developing novel anticancer therapies.

Purpose of the Study:

• To review the biochemistry of telomerase.
• To explore the therapeutic potential of natural and synthetic compounds, vaccines, and oncolytic viruses in suppressing telomerase activity.
• To provide a reference for structure-activity relationships of telomerase inhibitors and their clinical trial status.

Main Methods:

• Literature review of telomerase biochemistry and inhibitors.
• Analysis of structure-activity relationships for various natural and synthetic telomerase inhibitors.
• Compilation of data on clinical trials for telomerase-targeting therapies.

Main Results:

• Telomerase's role in cancer progression is confirmed, highlighting its potential as a therapeutic target.
• Various natural and synthetic compounds, alongside novel approaches like vaccines and oncolytic viruses, demonstrate potential for telomerase inhibition.
• Structure-activity relationship data and clinical trial updates are provided for medicinal chemists and researchers.

Conclusions:

• Inhibiting telomerase, particularly human TERT (hTERT) via promoter suppression, is a viable strategy for cancer treatment.
• The development of specific and pharmacokinetically improved telomerase inhibitors is crucial for advancing anticancer drug design.
• This review serves as a comprehensive resource on telomerase inhibitors and their therapeutic applications in oncology.