pubmed-article:10579814 | rdf:type | pubmed:Citation | lld:pubmed |
pubmed-article:10579814 | lifeskim:mentions | umls-concept:C0019682 | lld:lifeskim |
pubmed-article:10579814 | lifeskim:mentions | umls-concept:C0019699 | lld:lifeskim |
pubmed-article:10579814 | lifeskim:mentions | umls-concept:C0184511 | lld:lifeskim |
pubmed-article:10579814 | lifeskim:mentions | umls-concept:C0441655 | lld:lifeskim |
pubmed-article:10579814 | lifeskim:mentions | umls-concept:C0596988 | lld:lifeskim |
pubmed-article:10579814 | lifeskim:mentions | umls-concept:C0243071 | lld:lifeskim |
pubmed-article:10579814 | lifeskim:mentions | umls-concept:C1707689 | lld:lifeskim |
pubmed-article:10579814 | lifeskim:mentions | umls-concept:C0248121 | lld:lifeskim |
pubmed-article:10579814 | lifeskim:mentions | umls-concept:C0248122 | lld:lifeskim |
pubmed-article:10579814 | pubmed:issue | 22 | lld:pubmed |
pubmed-article:10579814 | pubmed:dateCreated | 1999-12-17 | lld:pubmed |
pubmed-article:10579814 | pubmed:abstractText | Two analogues of the nonnucleoside inhibitor of HIV-1 RT, MKC-442 (emivirine), containing different C6 substituents have been designed to be less susceptible to the commonly found drug-resistance mutation of Tyr181Cys. Compound TNK-6123 had a C6 thiocyclohexyl group designed to have more flexibility in adapting to the mutated drug-binding site. GCA-186 had additional 3',5'-dimethyl substituents aimed at forming close contacts with the conserved residue Trp229. Both compounds showed approximately 30-fold greater inhibitory effect than MKC-442 to the Tyr181Cys mutant virus as well as to the clinically important Lys103Asn virus. X-ray crystallographic structure determination of complexes with HIV-1 RT confirmed the predicted binding modes. These strategies might be used to improve the resilience of other NNRTI series against common drug-resistance mutations. | lld:pubmed |
pubmed-article:10579814 | pubmed:language | eng | lld:pubmed |
pubmed-article:10579814 | pubmed:journal | http://linkedlifedata.com/r... | lld:pubmed |
pubmed-article:10579814 | pubmed:citationSubset | IM | lld:pubmed |
pubmed-article:10579814 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
pubmed-article:10579814 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
pubmed-article:10579814 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
pubmed-article:10579814 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
pubmed-article:10579814 | pubmed:status | MEDLINE | lld:pubmed |
pubmed-article:10579814 | pubmed:month | Nov | lld:pubmed |
pubmed-article:10579814 | pubmed:issn | 0022-2623 | lld:pubmed |
pubmed-article:10579814 | pubmed:author | pubmed-author:TanakaHH | lld:pubmed |
pubmed-article:10579814 | pubmed:author | pubmed-author:BabbLL | lld:pubmed |
pubmed-article:10579814 | pubmed:author | pubmed-author:StammersD KDK | lld:pubmed |
pubmed-article:10579814 | pubmed:author | pubmed-author:StuartD IDI | lld:pubmed |
pubmed-article:10579814 | pubmed:author | pubmed-author:RecAA | lld:pubmed |
pubmed-article:10579814 | pubmed:author | pubmed-author:HopkinsA LAL | lld:pubmed |
pubmed-article:10579814 | pubmed:author | pubmed-author:OkamatoMM | lld:pubmed |
pubmed-article:10579814 | pubmed:issnType | Print | lld:pubmed |
pubmed-article:10579814 | pubmed:day | 4 | lld:pubmed |
pubmed-article:10579814 | pubmed:volume | 42 | lld:pubmed |
pubmed-article:10579814 | pubmed:owner | NLM | lld:pubmed |
pubmed-article:10579814 | pubmed:authorsComplete | Y | lld:pubmed |
pubmed-article:10579814 | pubmed:pagination | 4500-5 | lld:pubmed |
pubmed-article:10579814 | pubmed:dateRevised | 2009-8-19 | lld:pubmed |
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pubmed-article:10579814 | pubmed:meshHeading | pubmed-meshheading:10579814... | lld:pubmed |
pubmed-article:10579814 | pubmed:year | 1999 | lld:pubmed |
pubmed-article:10579814 | pubmed:articleTitle | Design of MKC-442 (emivirine) analogues with improved activity against drug-resistant HIV mutants. | lld:pubmed |
pubmed-article:10579814 | pubmed:affiliation | Laboratory of Molecular Biophysics, Rex Richards Building, South Parks Road, Oxford OX1 3QU, U.K. | lld:pubmed |
pubmed-article:10579814 | pubmed:publicationType | Journal Article | lld:pubmed |
pubmed-article:10579814 | pubmed:publicationType | Research Support, U.S. Gov't, P.H.S. | lld:pubmed |
pubmed-article:10579814 | pubmed:publicationType | Research Support, Non-U.S. Gov't | lld:pubmed |
http://linkedlifedata.com/r... | http://linkedlifedata.com/r... | pubmed-article:10579814 | lld:chembl |
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