Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:dateCreated
2004-2-9
pubmed:abstractText
Nucleoside-resistant isolates have been identified in patients receiving antiretroviral nucleoside drugs. The different resistance phenotypes seem to correlate with different sets of mutations in reverse transcriptase (RT), and the effect of individual set of mutations on resistance to a specific NRTI can only be presumed by kinetic studies and building up the enzyme active site by molecular modeling studies. However, the understanding how mutations affect RT structure and function, and the ensuing loss of potent antiviral activities of certain NRTIs have not been demonstrated in conjunction with their binding modes, which would provide invaluable insight into the design of more effective NRTIs active against the mutant RTs. This review discusses our recent efforts to assess the structural adjustment resulting from mutations and the accompanying energetic consequences based on the assumption that mutation may either deform the active site conformation through structural realignment or destabilize inhibitor binding.
pubmed:grant
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
Jan
pubmed:issn
1093-4715
pubmed:author
pubmed:issnType
Electronic
pubmed:day
1
pubmed:volume
9
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
164-86
pubmed:dateRevised
2007-11-15
pubmed:meshHeading
pubmed:year
2004
pubmed:articleTitle
Understanding the molecular mechanism of drug resistance of anti-HIV nucleosides by molecular modeling.
pubmed:affiliation
Department of Pharmaceutical and Biomedical Sciences, College of Pharmacy, The University of Georgia, Athens, GA 30602, USA.
pubmed:publicationType
Journal Article, Research Support, U.S. Gov't, P.H.S., Research Support, U.S. Gov't, Non-P.H.S.