CONTACT: GARY GALLUZZO
100 Old Public Library
Iowa City IA 52242
(319) 384-0009; fax (319) 384-0024
Release: June 16, 2000
UI chemistry professor discovers potential HIV inhibitor
IOWA CITY, Iowa -- University of Iowa chemistry professor Vasu Nair and
researchers at the National Cancer Institute (NCI) in Bethesda, Md. have discovered
potential HIV-inhibiting molecules that could one day prove therapeutically
significant in the treatment of AIDS.
Nair's findings appear in a paper scheduled for publication in the June
21 issue of the Journal of the American Chemical Society. Nair says that although
his National Institutes of Health-funded discovery is at an early stage of
development and years away from any potential human testing, it is significant
for its ability to stop HIV and for the way in which it attacks the virus.
"The single most devastating step in the attack of human cells by the
HIV virus is the incorporation, or integration, of viral DNA into human chromosomal
DNA. We have found small, stable molecules that inhibit this integration,"
he says. "In five to 10 years time, one of the molecules or a closely
related compound could become a drug targeted at the key step in the integration
of viral DNA into human DNA. That would be a major advance toward strictly
limiting the progression of AIDS."
The way in which the molecules work is analogous to the way in which glue
can be used to prevent a key from opening a lock. Specifically, the integration
of viral DNA occurs through a complex chemical process made possible by a
viral enzyme, called "HIV integrase," that acts as a key to open
human DNA for this incursion. Once the viral DNA has entered human chromosomal
DNA, it cannot be stopped, as it exploits human cellular chemistry to reproduce
itself and destroy the immune system. However, the molecules discovered by
Nair and his colleagues block this integration by attaching themselves to
the HIV "key" so that it no longer has the necessary capability
to facilitate the incorporation of viral DNA into human DNA.
"Blocking the biochemical steps by which this enzyme works is the key
to thwarting its action and preventing the ultimate viral DNA invasion,"
Nair's co-workers on the discovery include UI chemistry department postdoctoral
associates M. Taktakishvili and S. Pal, and his collaborators in the Laboratory
of Pharmacology at the National Cancer Institute are Dr. Y. Pommier and Dr.
N. Neamati. In addition, he acknowledges his former graduate student, Tamera
Jahnke, currently professor and head of chemistry at Southwest Missouri State
University, for her contribution to the initial stages of the work.
Nair, internationally known for his work on antiviral compounds, was named
UI Foundation Distinguished Professor of Chemistry in 1993 and has received
various patents, research awards and grants. In 1998, he was elected a Fellow
of the American Association for the Advancement of Science (AAAS), "for
his contributions to the development of antiviral agents."
"This publication is just the tip of the iceberg. We may be able to
design molecules that may be even better in combating AIDS," he says.
"We need to be constantly finding new ways to fight HIV and other viruses."