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SIRT1 inhibitor for the therapy of HPV-associated pathologies

Antineoplastic therapyEX527HPVInhibitors/Antagonist SIRT1Sirtuine

Introduction

The technology consists in the use of SIRT1 enzyme’s inhibitors or antagonists for the prevention and/or treatment of diseases induced by human papillomavirus (HPV). The molecule EX527, already known in the pharmacopoeia, has proven effective in the treatment of HPV-associated tumors, acting on the regulation of some oncoproteins, leading to the inhibition of SIRT1 with subsequent regression of the tumor mass.

Technical features

Human papillomaviruses (HPVs) are viruses widely spread in the population, some have a high neoplastic risk and are associated to the development of tumors of the anogenital and head-neck district. In these tumors, the over-expression of the cellular protein SIRT1 is evident. The molecule EX527, already known for the treatment of Huntington’s disease, has proved to be an excellent inhibitor of SIRT1. The inhibition effect of SIRT1 led to the regulation of oncoprotein levels with subsequent reduction of the tumor mass. Nowaday, the treatment of these tumors is highly invasive and with devastating effects on patients, as it involves radiation therapy, chemotherapy or surgery. For this reason, alternative antiviral therapy with reduced side effects will be an improvement for patients. It has also been shown that the inhibition of SIRT1 induces a cell cycle arrest, thus increasing the sensitivity of current therapeutic treatments.

Possible Applications

  • Treatment of HPV-associated tumors;
  • Treatment of HPV-associated pathologies;
  • In the prevention of HPV-associated diseases.

Advantages

  • Use of EX527, EU approved orphan drug;
  • Low invasive therapy;
  • Reduced collateral effects:
  • Increased efficacy with respect to the current therapies;
  • Reduction of SIRT1 levels;
  • Inhibiting the expression of E6 and E7 oncoproteins.