Linked Life Data

8074936

Source:http://linkedlifedata.com/resource/pubmed/id/8074936

Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
6
pubmed:dateCreated
1994-10-5
pubmed:abstractText
A C2 symmetry-based HIV protease inhibitor, A77003, exerts potent antiviral activity against a wide spectrum of HIV isolates in vitro. In this study, we asked whether A77003 could cause irreversible conformational changes to HIV-1, whether the amounts of viral RNA and p24 capsid protein per virion were altered, and how the infectivity of the virus produced in the presence of the drug was affected. We found that the number of viral particles and per-virion viral RNA content of the virus produced in the presence of A77003 did not significantly differ from those of the virus produced in the absence of the drug, whereas significant morphological changes were observed as assessed by transmission electron microscopy. However, the virus produced in the presence of A77003 contained substantially less p24gag protein per virion particle as compared to those produced in the absence of the drug or in the presence of AZT. Virions produced in the presence of A77003 showed up to 50-fold less infectious capability in subsequent tissue culture than control virions produced in the absence of drug or in the presence of AZT. This reduction in infectivity was maintained for at least 10 days in culture. The present data suggest that A77003 impairs HIV-1 protease-mediated Gag processing, interferes with the assembly and maturation of the virus, and leads to an irreversible loss of the infectivity of the virus, although a low but positive level of reversion to infectivity during the 10-day assay occurs. These features of A77003 (and perhaps similar HIV protease inhibitors as well) anti-HIV activity should represent desirable properties for antiviral therapy of AIDS and related diseases.
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
Jun
pubmed:issn
0889-2229
pubmed:author
pubmed:issnType
Print
pubmed:volume
10
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
735-43
pubmed:dateRevised
2006-11-15
pubmed:meshHeading
pubmed:year
1994
pubmed:articleTitle
A C2 symmetry-based HIV protease inhibitor, A77003, irreversibly inhibits infectivity of HIV-1 in vitro.
pubmed:affiliation
Experimental Retrovirology Section, National Cancer Institute, Bethesda, Maryland.
pubmed:publicationType
Journal Article, Comparative Study