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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
10
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pubmed:dateCreated |
2000-12-1
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pubmed:databankReference |
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pubmed:abstractText |
Efavirenz is a second-generation non-nucleoside inhibitor of HIV-1 reverse transcriptase (RT) that has recently been approved for use against HIV-1 infection. Compared with first-generation drugs such as nevirapine, efavirenz shows greater resilience to drug resistance mutations within HIV-1 RT. In order to understand the basis for this resilience at the molecular level and to help the design of further-improved anti-AIDS drugs, we have determined crystal structures of efavirenz and nevirapine with wild-type RT and the clinically important K103N mutant.
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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 |
Oct
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pubmed:issn |
0969-2126
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pubmed:author |
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pubmed:issnType |
Print
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pubmed:day |
15
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pubmed:volume |
8
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
1089-94
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pubmed:dateRevised |
2007-11-15
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pubmed:meshHeading |
pubmed-meshheading:11080630-Amino Acid Substitution,
pubmed-meshheading:11080630-Anti-HIV Agents,
pubmed-meshheading:11080630-Benzoxazines,
pubmed-meshheading:11080630-Binding Sites,
pubmed-meshheading:11080630-Crystallography, X-Ray,
pubmed-meshheading:11080630-Drug Resistance, Microbial,
pubmed-meshheading:11080630-HIV Reverse Transcriptase,
pubmed-meshheading:11080630-HIV-1,
pubmed-meshheading:11080630-Humans,
pubmed-meshheading:11080630-Models, Molecular,
pubmed-meshheading:11080630-Mutation,
pubmed-meshheading:11080630-Nevirapine,
pubmed-meshheading:11080630-Oxazines,
pubmed-meshheading:11080630-Protein Binding,
pubmed-meshheading:11080630-Protein Conformation,
pubmed-meshheading:11080630-Reverse Transcriptase Inhibitors,
pubmed-meshheading:11080630-Structure-Activity Relationship
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pubmed:year |
2000
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pubmed:articleTitle |
Structural basis for the resilience of efavirenz (DMP-266) to drug resistance mutations in HIV-1 reverse transcriptase.
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pubmed:affiliation |
Structural Biology Division The Wellcome Trust Centre for Human Genetics University of Oxford OX3 7BN, Oxford, United Kingdom.
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
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