Office of Technology Transfer – University of Michigan

Novel Inhibition of HIV Protease

Technology #3813

Background

Acquired immune deficiency syndrome (AIDS) is a collection of symptoms and infections resulting from the specific damage to the immune system caused by the human immunodeficiency virus (HIV), affecting over 30 million people worldwide. AIDS is the most severe acceleration of infection with HIV, which is a retrovirus that primarily infects vital organs of the human immune system. In the absence of antiretroviral therapy, the median time of progression from HIV infection to AIDS is nine to ten years, and the median survival time after developing AIDS is less than a year, although the rate of clinical disease progression varies widely amongst individuals. While treatments for AIDS and HIV exist to slow the virus' progression, there is no known cure to date.

Technology

Researchers at the University of Michigan have developed methods for inhibiting the function of HIV protease (HIVp), which is an enzyme critical to the function of the virus. In particular, compounds inhibit or block the biological activity of HIVp, thereby inhibiting or terminating the HIV replication. The researchers identified a novel targeting region of HIVp, defined by a lower portion, an upper portion, and distal contacts. It was found that small molecules can bind within the new site and prevent the “flaps” of the HIVp from properly folding to close the binding site, thereby blocking the formation of the reactive form of HIVp and inhibiting the activity of the HIVp. The compounds, as well as pharmaceutical compositions that contain these compounds and optionally other anti-viral agents as active ingredients, are suitable for treating patients or hosts infected with the HIV virus, and may also find use in diagnostic and research settings.

Applications and Advantages

Applications

  • Treatment of patients or hosts infected with HIV
  • Drug screening
  • Diagnostics for disorders associated with HIV protease

Advantages

  • Small molecule inhibitors of HIVp activity
  • Compounds not limited to a particular manner of binding with HIVp