Linked Life Data

16611063

Source:http://linkedlifedata.com/resource/pubmed/id/16611063

Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
7
pubmed:dateCreated
2006-4-13
pubmed:abstractText
Recent advances in our understanding of cellular and molecular mechanisms of viral penetration of the target cell have provided the basis for novel chemotherapy and prophylaxis of HIV-1 infections. This knowledge has been successfully applied to the development of inhibitors that target discrete steps of the entry process. Interesting approaches for prevention of HIV-1 entry include the use of small-molecule inhibitors, natural ligands and/or monoclonal antibodies that interfere with gp120/CD4 interaction. Other compounds acting by novel mechanisms have recently been identified as anti-HIV agents and seem worthy of further preclinical development. Of particular interest in this regard are cyclotriazadisulfonamide (CADA) compounds, which down-modulate the cellular receptor, CD4. A series of analogues of 9-benzyl-3-methylene-1,5-di-p-toluenesulfonyl-1,5,9-triazacyclododecane (CADA) has been synthesized and tested for CD4 down-modulation and anti-HIV activity. Some derivatives proved to be highly effective in decreasing cellular CD4 and in acting as HIV entry inhibitors. Three-dimensional quantitative structure-activity relationship (3D-QSAR) studies correlating molecular features with potency have been used to produce a computational model. This model can be used to design more potent CD4 down-modulating drugs for HIV therapy and prophylaxis. This review summarizes the results of recent studies relating to inhibitors of HIV infection via CD4 and discusses the therapeutic potential of targeting this cellular receptor. Special attention is given to our own work on small-molecule HIV entry inhibitors endowed with CD4 down-modulating properties.
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:issn
0929-8673
pubmed:author
pubmed:issnType
Print
pubmed:volume
13
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
731-43
pubmed:dateRevised
2007-2-12
pubmed:meshHeading
pubmed:year
2006
pubmed:articleTitle
Inhibitors of HIV infection via the cellular CD4 receptor.
pubmed:affiliation
Rega Institute for Medical Research, Katholieke Universiteit Leuven, B-3000 Leuven, Belgium. kurt.vermeire@rega.kuleuven.be
pubmed:publicationType
Journal Article, Review