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Repositioning HIV protease inhibitors as cancer therapeutics

Publication ,  Journal Article
Bernstein, WB; Dennis, PA
Published in: Current Opinion in HIV and AIDS
November 1, 2008

PURPOSE OF REVIEW: Although designed to target only the HIV protease, HIV protease inhibitors induce toxicities in patients such as insulin resistance and lipodystrophy that suggest that protease inhibitors have other targets in mammalian cells. Akt controls insulin signaling and is an important target in cancer, but no Akt inhibitors are approved as cancer therapeutics. These observations have prompted the study of HIV protease inhibitors as inhibitors of Akt and possible cancer therapeutics. This review will highlight the latest advances in repositioning HIV protease inhibitors as cancer therapeutics. RECENT FINDINGS: Although protease inhibitors can inhibit Akt activation and the proliferation of over 60 cancer cell lines, as well as improve sensitivity to radiation or chemotherapy, these effects do not always correlate with Akt inhibition. Other important processes, such as the induction of endoplasmic reticulum stress, appear critical to the biological activity of protease inhibitors. These impressive and surprising preclinical data have prompted clinical testing of nelfinavir as a lead HIV protease inhibitor in cancer patients. SUMMARY: Although mechanisms of action for the antitumor effects of HIV protease inhibitors are complex, their broad spectrum of activity, minimal toxicity, and wide availability make protease inhibitors ideal candidates for repositioning as cancer therapeutics. © 2008 Lippincott Williams & Wilkins, Inc.

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Published In

Current Opinion in HIV and AIDS

DOI

EISSN

1746-6318

ISSN

1746-630X

Publication Date

November 1, 2008

Volume

3

Issue

6

Start / End Page

666 / 675

Related Subject Headings

  • Virology
  • 4202 Epidemiology
  • 3207 Medical microbiology
  • 3202 Clinical sciences
  • 1117 Public Health and Health Services
 

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Bernstein, W. B., & Dennis, P. A. (2008). Repositioning HIV protease inhibitors as cancer therapeutics. Current Opinion in HIV and AIDS, 3(6), 666–675. https://doi.org/10.1097/COH.0b013e328313915d
Bernstein, W. B., and P. A. Dennis. “Repositioning HIV protease inhibitors as cancer therapeutics.” Current Opinion in HIV and AIDS 3, no. 6 (November 1, 2008): 666–75. https://doi.org/10.1097/COH.0b013e328313915d.
Bernstein WB, Dennis PA. Repositioning HIV protease inhibitors as cancer therapeutics. Current Opinion in HIV and AIDS. 2008 Nov 1;3(6):666–75.
Bernstein, W. B., and P. A. Dennis. “Repositioning HIV protease inhibitors as cancer therapeutics.” Current Opinion in HIV and AIDS, vol. 3, no. 6, Nov. 2008, pp. 666–75. Scopus, doi:10.1097/COH.0b013e328313915d.
Bernstein WB, Dennis PA. Repositioning HIV protease inhibitors as cancer therapeutics. Current Opinion in HIV and AIDS. 2008 Nov 1;3(6):666–675.

Published In

Current Opinion in HIV and AIDS

DOI

EISSN

1746-6318

ISSN

1746-630X

Publication Date

November 1, 2008

Volume

3

Issue

6

Start / End Page

666 / 675

Related Subject Headings

  • Virology
  • 4202 Epidemiology
  • 3207 Medical microbiology
  • 3202 Clinical sciences
  • 1117 Public Health and Health Services