NDLI: PA-457: a potent HIV inhibitor that disrupts core condensation by targeting a late step in Gag processing.

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PA-457: a potent HIV inhibitor that disrupts core condensation by targeting a late step in Gag processing.

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PA-457: a potent HIV inhibitor that disrupts core condensation by targeting a late step in Gag processing.

Content Provider	World Health Organization (WHO)-Global Index Medicus
Author	Freed, E. O. Goila-gaur, R. Salzwedel, K. Wild, C. T. Allaway, G. P. Reddick, M. Li, F. Castillo, A. Matallana, C. Orenstein, J. M. Martin, D. E. Kilgore, N. R. Zoumplis, D.
Description	Author Affiliation: Li F ( Panacos Pharmaceuticals Inc., 209 Perry Parkway, Gaithersburg, MD 20877, USA.);
Abstract	New HIV therapies are urgently needed to address the growing problem of drug resistance. In this article, we characterize the anti-HIV drug candidate 3-O-(3',3'-dimethylsuccinyl) betulinic acid (PA-457). We show 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. 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.
ISSN	00278424
e-ISSN	10916490
Journal	Proceedings of the National Academy of Sciences of the United States of America
Issue Number	23
Volume Number	100
Language	English
Publisher	National Academy of Sciences
Publisher Date	2003-11-01
Publisher Place	United States
Access Restriction	Open
Subject Keyword	Anti-HIV Agents Pharmacology Gene Products, Gag Chemistry Succinates Triterpenes Binding Sites Drug Design Antagonists & Inhibitors Genotype HIV Core Protein P24 Metabolism HeLa Cells Inhibitory Concentration 50 Microscopy, Electron Models, Chemical Models, Genetic Mutation Plasmids Precipitin Tests Gag Gene Products, Human Immunodeficiency Virus Research Support, U.S. Gov't, P.H.S. Multidisciplinary
Content Type	Text
Resource Type	Article
Subject	Multidisciplinary

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