Elsevier

Drug Discovery Today

Volume 25, Issue 7, July 2020, Pages 1213-1222
Drug Discovery Today

Informatics
In silico design of telomerase inhibitors

https://doi.org/10.1016/j.drudis.2020.04.024Get rights and content
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open access

Highlights

  • Telomerase is still challenging and underexplored anticancer target.

  • Details of human telomerase molecular structure is still unrevealed.

  • In silico design of telomerase enzymatic inhibitors is still only at starting point.

Telomerase is a reverse transcriptase enzyme involved in DNA synthesis at the end of linear chromosomes. Unlike in most other cells, telomerase is reactivated most cancerous cells and, therefore, has become a promising new anticancer target. Despite extensive research, direct telomerase inhibitors have yet not been introduced to the clinics because of the complexity of this enzyme. Structures of this protein from simple organisms and human homology models are currently available and have been used in structure-based drug design efforts to find potential inhibitors. Different is silico strategies have been applied and different chemical groups have been explored. Here, we provide an overview of recent discoveries.

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