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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
24
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pubmed:dateCreated |
1998-1-12
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pubmed:abstractText |
Using a combination of iterative structure-based design and an analysis of oral pharmacokinetics and antiviral activity, AG1343 (Viracept, nelfinavir mesylate), a nonpeptidic inhibitor of HIV-1 protease, was identified. AG1343 is a potent enzyme inhibitor (Ki = 2 nM) and antiviral agent (HIV-1 ED50 = 14 nM). An X-ray cocrystal structure of the enzyme-AG1343 complex reveals how the novel thiophenyl ether and phenol-amide substituents of the inhibitor interact with the S1 and S2 subsites of HIV-1 protease, respectively. In vivo studies indicate that AG1343 is well absorbed orally in a variety of species and possesses favorable pharmacokinetic properties in humans. AG1343 (Viracept) has recently been approved for marketing for the treatment of AIDS.
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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 |
Nov
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pubmed:issn |
0022-2623
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pubmed:author |
pubmed-author:AppeltKK,
pubmed-author:BurgessJ AJA,
pubmed-author:CampanaleK MKM,
pubmed-author:ChirgadzeN YNY,
pubmed-author:ClawsonD KDK,
pubmed-author:DaviesJ FJF2nd,
pubmed-author:DressmanB ABA,
pubmed-author:FritzJ EJE,
pubmed-author:HatchS DSD,
pubmed-author:KaldorS WSW,
pubmed-author:KalishV JVJ,
pubmed-author:KhalilD ADA,
pubmed-author:KosaM BMB,
pubmed-author:LubbehusenP PPP,
pubmed-author:MuesingM AMA,
pubmed-author:PatickA KAK,
pubmed-author:ReichS HSH,
pubmed-author:ShettyB VBV,
pubmed-author:SuK SKS,
pubmed-author:TatlockJ HJH
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pubmed:issnType |
Print
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pubmed:day |
21
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pubmed:volume |
40
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
3979-85
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pubmed:dateRevised |
2003-11-14
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pubmed:meshHeading |
pubmed-meshheading:9397180-Administration, Oral,
pubmed-meshheading:9397180-Animals,
pubmed-meshheading:9397180-Anti-HIV Agents,
pubmed-meshheading:9397180-Biological Availability,
pubmed-meshheading:9397180-Callithrix,
pubmed-meshheading:9397180-Dogs,
pubmed-meshheading:9397180-Dose-Response Relationship, Drug,
pubmed-meshheading:9397180-Female,
pubmed-meshheading:9397180-HIV Protease Inhibitors,
pubmed-meshheading:9397180-HIV-1,
pubmed-meshheading:9397180-Macaca fascicularis,
pubmed-meshheading:9397180-Male,
pubmed-meshheading:9397180-Nelfinavir,
pubmed-meshheading:9397180-Rats,
pubmed-meshheading:9397180-Rats, Sprague-Dawley,
pubmed-meshheading:9397180-Structure-Activity Relationship
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pubmed:year |
1997
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pubmed:articleTitle |
Viracept (nelfinavir mesylate, AG1343): a potent, orally bioavailable inhibitor of HIV-1 protease.
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pubmed:affiliation |
Agouron Pharmaceuticals, Inc., San Diego, California 92121, USA.
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pubmed:publicationType |
Journal Article
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