08 February 2010

Two more potential HIV protease inhibitors

Distributed computing has helped to find a new cure for AIDS!Popular science blog "Just about science"
Scientists from the Scripps Research Institute in La Jolla (California) have discovered two chemical compounds that affect previously unknown sites of the HIV protease enzyme (human immunodeficiency virus) that causes the development of AIDS (acquired immunodeficiency syndrome).

The discovery will allow the development of new antiviral drugs that will increase the effectiveness of treatment of HIV strains resistant to existing drugs, as well as slow down the spread of resistant forms of the virus among patients.

The compounds identified by scientists from the Scripps Institute are associated with the HIV protease, which is the basis of the life cycle of this deadly virus. Drugs that block HIV protease are called "protease inhibitors" and are currently the main component of AIDS prevention drugs used in the modern scheme of its treatment with highly Active antiretroviral therapy (Highly Active Anti-Retroviral Therapy, HAART).

Compared to the nine HIV protease inhibitors already approved by the US Food and Drug Administration (FDA), the substances found are small chemical compounds that affect two previously unknown sites of the HIV protease molecule.

Alex L. Perryman, an employee of Professor Arthur Olson's laboratory from the Scripps Institute, tells about the discovery: "The experiments carried out confirmed my hypothesis, based on the results of computational modeling, that on the surface of the HIV protease, in addition to the active center, there are other sites that can selectively bind to inhibitors. The found medicinal substances will be used to strengthen the FDA-approved HIV protease active center inhibitors and restore their effectiveness against resistant HIV strains. Our strategy of involving inactive sites of biological targets may be useful in the search for drugs for other diseases, especially when there is resistance to known drugs."

Perryman and his colleagues from Olson's laboratory used the capabilities of the FightAIDS@Home distributed computing project, which is part of a group of projects managed by the World Community Grid association, in computer modeling. Therefore, the private owners of the FightAIDS@Home project can rightfully add themselves to the list of co-authors of the discovery of a new class of anti-HIV drugs.

There are currently about 33 million people living with HIV infection in the world. According to statistics from the World Health Organization, 2.7 million people were infected with HIV in 2008 alone. Although antiretroviral therapy has increased the duration and improved the quality of life of AIDS patients, there is an active spread of drug-resistant strains of HIV infection.

The research of new HIV protease inhibitors by scientists from the Scripps Institute was supported by a grant from the National Institutes of Health of the USA. Detailed research results will appear in the March issue of the journal Chemical Biology & Drug Design.

Portal "Eternal youth" http://vechnayamolodost.ru08.02.2010

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