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HIV-protease inhibitors for the treatment of cancer: Repositioning HIV protease inhibitors while developing more potent NO-hybridized derivatives?

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  • Danijela Maksimovic-Ivanic
  • Paolo Fagone
  • James McCubrey
  • Klaus Bendtzen
  • Sanja Mijatovic
  • Ferdinando Nicoletti
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The possible use of HIV protease inhibitors (HIV-PI) as new therapeutic option for the treatment of cancer primarily originated from their success in treating HIV-related Kaposi's sarcoma (KS). While these findings were initially attributed to immune reconstitution and better control of oncogenic viral infections, the number of reports on solid tumors, KS, lymphoma, fibrosarcoma, multiple myeloma and prostate cancer suggest other mechanisms for the anti-neoplastic activity of PIs. However, a major drawback for the possible adoption of HIV-PIs in the therapy of cancer relies on their relatively weak anticancer potency and important side effects. This has propelled several groups to generate derivatives of HIV-PIs for anticancer use, through modifications such as attachment of different moieties, ligands and transporters, including saquinavir-loaded folic acid conjugated nanoparticles and nitric oxide (NO) derivatives of HIV-PIs. In this article, we discuss the current preclinical and clinical evidences for the potential use of HIV-PIs, and of novel derivatives, such as saquinavir-NO in the treatment of cancer.

Original languageEnglish
JournalRadiation Oncology Investigations
Volume140
Issue number8
Pages (from-to)1713-1726
Number of pages14
ISSN0020-7136
DOIs
Publication statusPublished - 15 Apr 2017

    Research areas

  • Antiretroviral Therapy, Highly Active, HIV Infections, HIV Protease Inhibitors, HIV-1, Humans, Neoplasms, Nitric Oxide, Saquinavir, Sarcoma, Kaposi, Journal Article, Review

ID: 52406931