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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
1
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pubmed:dateCreated |
2006-12-13
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pubmed:abstractText |
Pradimicin A (PRM-A), an antifungal nonpeptidic benzonaphtacenequinone antibiotic, is a low-molecular-weight (molecular weight, 838) carbohydrate binding agent (CBA) endowed with a selective inhibitory activity against human immunodeficiency virus (HIV). It invariably inhibits representative virus strains of a variety of HIV-1 clades with X4 and R5 tropisms at nontoxic concentrations. Time-of-addition studies revealed that PRM-A acts as a true virus entry inhibitor. PRM-A specifically interacts with HIV-1 gp120 and efficiently prevents virus transmission in cocultures of HUT-78/HIV-1 and Sup T1 cells. Upon prolonged exposure of HIV-1-infected CEM cell cultures, PRM-A drug pressure selects for mutant HIV-1 strains containing N-glycosylation site deletions in gp120 but not gp41. A relatively long exposure time to PRM-A is required before drug-resistant virus strains emerge. PRM-A has a high genetic barrier, since more than five N-glycosylation site deletions in gp120 are required to afford moderate drug resistance. Such mutated virus strains keep full sensitivity to the other known clinically used anti-HIV drugs. PRM-A represents the first prototype compound of a nonpeptidic CBA lead and, together with peptide-based lectins, belongs to a conceptually novel type of potential therapeutics for which drug pressure results in the selection of glycan deletions in the HIV gp120 envelope.
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pubmed:commentsCorrections |
http://linkedlifedata.com/resource/pubmed/commentcorrection/17050611-11040045,
http://linkedlifedata.com/resource/pubmed/commentcorrection/17050611-12072529,
http://linkedlifedata.com/resource/pubmed/commentcorrection/17050611-12829775,
http://linkedlifedata.com/resource/pubmed/commentcorrection/17050611-12921090,
http://linkedlifedata.com/resource/pubmed/commentcorrection/17050611-1332602,
http://linkedlifedata.com/resource/pubmed/commentcorrection/17050611-14714897,
http://linkedlifedata.com/resource/pubmed/commentcorrection/17050611-14747537,
http://linkedlifedata.com/resource/pubmed/commentcorrection/17050611-15251280,
http://linkedlifedata.com/resource/pubmed/commentcorrection/17050611-15367629,
http://linkedlifedata.com/resource/pubmed/commentcorrection/17050611-15388446,
http://linkedlifedata.com/resource/pubmed/commentcorrection/17050611-15572157,
http://linkedlifedata.com/resource/pubmed/commentcorrection/17050611-15582695,
http://linkedlifedata.com/resource/pubmed/commentcorrection/17050611-15665496,
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http://linkedlifedata.com/resource/pubmed/commentcorrection/17050611-16183648,
http://linkedlifedata.com/resource/pubmed/commentcorrection/17050611-16189008,
http://linkedlifedata.com/resource/pubmed/commentcorrection/17050611-16227301,
http://linkedlifedata.com/resource/pubmed/commentcorrection/17050611-16253890,
http://linkedlifedata.com/resource/pubmed/commentcorrection/17050611-16569440,
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http://linkedlifedata.com/resource/pubmed/commentcorrection/17050611-1710248,
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http://linkedlifedata.com/resource/pubmed/commentcorrection/17050611-3016298,
http://linkedlifedata.com/resource/pubmed/commentcorrection/17050611-3198502,
http://linkedlifedata.com/resource/pubmed/commentcorrection/17050611-3198504,
http://linkedlifedata.com/resource/pubmed/commentcorrection/17050611-7543588,
http://linkedlifedata.com/resource/pubmed/commentcorrection/17050611-8417177,
http://linkedlifedata.com/resource/pubmed/commentcorrection/17050611-8478264,
http://linkedlifedata.com/resource/pubmed/commentcorrection/17050611-8615015,
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http://linkedlifedata.com/resource/pubmed/commentcorrection/17050611-9526659,
http://linkedlifedata.com/resource/pubmed/commentcorrection/17050611-9623976,
http://linkedlifedata.com/resource/pubmed/commentcorrection/17050611-9641677,
http://linkedlifedata.com/resource/pubmed/commentcorrection/17050611-9671774,
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http://linkedlifedata.com/resource/pubmed/commentcorrection/17050611-9756780
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pubmed:language |
eng
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pubmed:journal |
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pubmed:citationSubset |
IM
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pubmed:chemical |
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pubmed:status |
MEDLINE
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pubmed:month |
Jan
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pubmed:issn |
0022-538X
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pubmed:author |
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pubmed:issnType |
Print
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pubmed:volume |
81
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
362-73
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pubmed:dateRevised |
2009-11-18
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pubmed:meshHeading |
pubmed-meshheading:17050611-Anthracyclines,
pubmed-meshheading:17050611-Anti-HIV Agents,
pubmed-meshheading:17050611-Antigens, CD4,
pubmed-meshheading:17050611-Carbohydrate Metabolism,
pubmed-meshheading:17050611-Cell Line,
pubmed-meshheading:17050611-Coculture Techniques,
pubmed-meshheading:17050611-Drug Resistance, Viral,
pubmed-meshheading:17050611-Genotype,
pubmed-meshheading:17050611-Glycosylation,
pubmed-meshheading:17050611-HIV Envelope Protein gp120,
pubmed-meshheading:17050611-HIV-1,
pubmed-meshheading:17050611-Humans,
pubmed-meshheading:17050611-Models, Molecular,
pubmed-meshheading:17050611-Mutation,
pubmed-meshheading:17050611-Receptors, CXCR4,
pubmed-meshheading:17050611-Viral Envelope Proteins
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pubmed:year |
2007
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pubmed:articleTitle |
Pradimicin A, a carbohydrate-binding nonpeptidic lead compound for treatment of infections with viruses with highly glycosylated envelopes, such as human immunodeficiency virus.
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pubmed:affiliation |
Rega Institute for Medical Research, Minderbroedersstraat 10, B-3000 Leuven, Belgium. jan.balzarini@rega.kuleuven.ac.be
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