AIDSWEEKLY Plus; Monday, December 29, 2003
Staff Medical Writers

In a recent study, F. Li and colleagues at Gaithersburg-based Panacos Pharmaceutical Inc. characterized "the anti-HIV drug candidate 3-0-(3',3'-dimethylsuccinyl) betulinic acid (PA-457)."

Published data revealed that "PA-457 potently inhibits replication of both WT and drug-resistant HIV-1 isolates," and "demonstrate that the compound acts by disrupting a late step in Gag processing involving conversion of the capsid precursor (p25) to mature capsid protein (p24)."

"We find that virions from PA-457-treated cultures are noninfectious and exhibit an aberrant particle morphology characterized by a spherical, acentric core and a crescent-shaped, electron-dense shell lying just inside the viral membrane," according to the report. "To identify the determinants of compound activity we selected for PA-457-resistant virus in vitro. Consistent with the effect on Gag processing, we found that mutations conferring resistance to PA-457 map to the p25 to p24 cleavage site."

"PA-457 represents a unique class of anti-HIV compounds termed maturation inhibitors that exploit a previously unidentified viral target, providing additional opportunities for HIV drug discovery," the investigators concluded.

Li and coauthors published the results of their research in the Proceedings of the National Academy of Sciences USA (PA-457: A potent HIV inhibitor that disrupts core condensation by targeting a late step in Gag processing. Proc Natl Acad Sci U S A. 2003 Nov 11;100(23):13555-60.

For additional information, contact C.T. Wild, Panacos Pharmaceutical Inc., 209 Perry Parkway, Gaithersburg, MD 20877, USA.

The publisher of the journal Proceedings of the National Academy of Sciences USA can be contacted at: National Academy of Sciences, 2101 Constitution Avenue NW, Washington, DC 20418, USA.

The information in this article comes under the major subject areas of AIDS & HIV, Pharmaceutical & Drug Development and Virology.

This article was prepared by AIDS Weekly editors from staff and other reports.

Reference

Li F, Goila-Gaur R, Salzwedel K, et al., "PA-457: a potent HIV inhibitor that disrupts core condensation by targeting a late step in Gag processing", Proc Natl Acad Sci U S A. 2003 Nov 11;100(23):13555-60

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