What is it about?

We describe using medicinal chemistry principles, including the concept of mimicking the biomolecule netropsin, which contains a guanidine, to improve the efficacy of large, antiviral polyamides active against high-risk, cancer-causing forms of human papillomavirus (HPV). We showed in previous work that this class of molecules causes strand breakage of the double-stranded viral DNA genome and nuclease digestion of that genome. Here, we report some of the most active compounds found to date against HPV.

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Why is it important?

Anti-HPV compounds are important because they are potential drugs for the treatment of patients who are infected with HPV, for example, because they were not vaccinated or because the vaccine they received did not protect against the HPV to which they were exposed. Anti-HPV drugs could prevent the progression of a high-risk viral infection to cancer, or could decrease the likelihood of that progression, and could also eliminate genital warts if active against low-risk HPVs. So far, we have focused on testing our compounds against high-risk, cancer-causing HPVs of the types that cause cervical, head and neck, and other cancers. There is no current, credible, specific antiviral drug for HPV that is highly effective and low in toxicity. Decreasing the amount of virus for HPV16 was shown to decrease the occurrence of cancer.


We continue to show that large charged molecules are taken up well by human keratinocytes and show excellent anti-HPV activity and that medicinal chemistry principles can continue to improve their efficacy.

Professor James Keane Bashkin
University of Missouri-St. Louis

Read the Original

This page is a summary of: β-Alanine and N-terminal cationic substituents affect polyamide–DNA binding, Organic & Biomolecular Chemistry, January 2017, Royal Society of Chemistry,
DOI: 10.1039/c7ob02513k.
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