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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
18
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pubmed:dateCreated |
2010-9-6
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pubmed:abstractText |
Structure-activity relationship studies were conducted on HIV integrase (IN) inhibitory peptides which were found by the screening of an overlapping peptide library derived from HIV-1 gene products. Since these peptides located in the second helix of Vpr are considered to have an alpha-helical conformation, Glu-Lys pairs were introduced into the i and i+4 positions to increase the helicity of the lead compound possessing an octa-arginyl group. Ala-scan was also performed on the lead compound for the identification of the amino acid residues responsible for the inhibitory activity. The results indicated the importance of an alpha-helical structure for the expression of inhibitory activity, and presented a binding model of integrase and the lead compound.
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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 |
Sep
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pubmed:issn |
1464-3391
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pubmed:author |
pubmed-author:AraiHiroshiH,
pubmed-author:HashimotoChieC,
pubmed-author:KomanoJun AJA,
pubmed-author:MaddaliKasthuraiahK,
pubmed-author:NarumiTetsuoT,
pubmed-author:NomuraWataruW,
pubmed-author:OhashiNamiN,
pubmed-author:OzakiTaroT,
pubmed-author:PommierYvesY,
pubmed-author:SuzukiShintaroS,
pubmed-author:TamamuraHirokazuH,
pubmed-author:TanakaTomohiroT,
pubmed-author:TsutsumiHiroshiH,
pubmed-author:UranoEmikoE,
pubmed-author:YamamotoNaokiN
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pubmed:copyrightInfo |
Copyright (c) 2010 Elsevier Ltd. All rights reserved.
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pubmed:issnType |
Electronic
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pubmed:day |
15
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pubmed:volume |
18
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
6771-5
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pubmed:meshHeading |
pubmed-meshheading:20708407-Amino Acid Sequence,
pubmed-meshheading:20708407-Cell Line,
pubmed-meshheading:20708407-Circular Dichroism,
pubmed-meshheading:20708407-Glutamic Acid,
pubmed-meshheading:20708407-HIV Integrase Inhibitors,
pubmed-meshheading:20708407-Humans,
pubmed-meshheading:20708407-Lysine,
pubmed-meshheading:20708407-Molecular Sequence Data,
pubmed-meshheading:20708407-Peptides,
pubmed-meshheading:20708407-Structure-Activity Relationship,
pubmed-meshheading:20708407-vpr Gene Products, Human Immunodeficiency Virus
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pubmed:year |
2010
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pubmed:articleTitle |
Peptidic HIV integrase inhibitors derived from HIV gene products: structure-activity relationship studies.
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pubmed:affiliation |
Institute of Biomaterials and Bioengineering, Tokyo Medical and Dental University, Chiyoda-ku, Tokyo 101-0062, Japan.
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't,
Research Support, N.I.H., Intramural
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