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University of Pittsburgh School of
Medicine researchers report they have developed a way to track—and perhaps
block—the activity of Nef, an HIV protein that is critical to HIV replication.
According to researcher Thomas Smithgall, Ph.D., the team reasoned it might be
possible to stop HIV replication by preventing Nef’s “usual interactions with
other proteins.”
The researchers linked Nef to Hck—an
enzyme activated in HIV-infected cells—and screened close to 250,000 compounds
for a compound that would block Nef’s role in replication. The automated
screening procedure identified a promising compound, B9, which interrupts Nef’s
role in HIV replication by preventing two Nef molecules from forming “dimers,”
an essential step in the HIV replication process.
The team believes their discovery of
the point where B9 binds to Nef could lead to the invention of new drugs that
could prevent HIV from developing into AIDS. Smithgall says test-tube and cell
culture experiments confirm this spot is an HIV “Achilles heel” that could be a
target for drugs that stop the virus from replicating. The University of
Pittsburgh Drug Discovery Institute is working to find a formula similar to B9
that can be tested with animals.
The full report, “Effector Kinase
Coupling Enables High-Throughput Screens for Direct HIV-1 Nef Antagonists with
Antiretroviral Activity,” was published online in the journal Chemistry &
Biology (2013; 20(1):82–-91).
The Friends of AIDS Foundation is
dedicated to enhancing the quality of life for HIV positive individuals and
empowering people to make healthy choices to prevent the spread of the HIV
virus. To learn more about The Friends of AIDS Foundation, please visit: http://www.friendsofaids.org.
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