Telomerase inhibitors: a patent review (2010–2015)

ABSTRACT

Introduction: Telomerase is a ribonucleoprotein that catalyses the addition of telomeric repeat sequences (having the sequence 5′-TTAGGG-3′ in humans) to the ends of chromosomes. Telomerase activity is detected in most types of human tumours, but it is almost undetectable in normal somatic cells. Therefore, telomerase is a promising therapeutic target. To date, the known inhibitors of telomerase include nucleoside analogues, oligonucleotides and G-quadruplex stabilizers. This review highlights recent advances in our understanding of telomerase inhibitors, the relationships between telomerase inhibitors, cancer, and fields such as inflammation.

Areas covered: This review summarizes new patents published on telomerase inhibitors from 2010 to 2015.

Expert opinion: The review provides a brief account of the background, development, and on-going issues involving telomerase inhibitors. In particular, this review emphasizes imetelstat (GRN163L) and some typical G-quadruplex stabilizers that participate in telomerase inhibition. Overall, the research scope of antineoplastic is becoming broader and telomerase inhibitors have been shown to be a promising therapeutic target. Therefore, novel antineoplastic agents with greater activity and higher specificity must be developed.

KEYWORDS:

• Telomere
• telomerase
• telomerase inhibitor
• antineoplastic
• imetelstat (GRN163L)
• diagnostic methods
• therapies

Article highlights

• Current telomerase inhibitor drugs cover a wide scope.

• Telomerase inhibitors play an essential role in bio-pharmaceuticals. Currently, they have become an important target for the design of antitumour drugs.

• There are many types of telomerase inhibitors that have been published in articles or patents. They can be categorized into different classes according to their function.

• It is possible that telomerase inhibitors are novel antineoplastic drugs.

This box summarizes key points contained in the article.

Declaration of interests

This work was supported by National Technology Support Program (No. 2015BAD16B07) and supported by Major Projects on Control and Rectification of Water Body Pollution (No. 2011ZX07204-001-2214 004). The author has no relevant affiliations or financial involvement with any organization or entity with a financial interest in or financial conflict with the subject matter or materials discussed in the manuscript. This includes employment, consultancies, honoraria, stock ownership or options, expert testimony, grants or patents received or pending, or royalties.