Source:http://linkedlifedata.com/resource/pubmed/id/21392990
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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
8
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pubmed:dateCreated |
2011-4-4
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pubmed:abstractText |
The human T cell leukemia/lymphotropic virus type 1 (HTLV-I) is clinically associated with adult T cell leukemia/lymphoma, HTLV-I associated myelopathy/tropical spastic paraparesis, and a number of other chronic inflammatory diseases. To stop the replication of the virus, we developed highly potent tetrapeptidic HTLV-I protease inhibitors. In a recent X-ray crystallography study, several of our inhibitors could not form co-crystal complexes with the protease due to their high hydrophobicity. In the current study, we designed, synthesized and evaluated the HTLV-I protease inhibition potency of compounds with hydrophilic end-capping moieties with the aim of improving pharmaceutic and pharmacokinetic properties.
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pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
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pubmed:chemical | |
pubmed:status |
MEDLINE
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pubmed:month |
Apr
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pubmed:issn |
1464-3405
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pubmed:author | |
pubmed:copyrightInfo |
Copyright © 2011 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 |
21
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
2425-9
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pubmed:meshHeading |
pubmed-meshheading:21392990-Binding Sites,
pubmed-meshheading:21392990-Catalytic Domain,
pubmed-meshheading:21392990-Computer-Aided Design,
pubmed-meshheading:21392990-Crystallography, X-Ray,
pubmed-meshheading:21392990-Drug Design,
pubmed-meshheading:21392990-HIV Protease,
pubmed-meshheading:21392990-Human T-lymphotropic virus 1,
pubmed-meshheading:21392990-Humans,
pubmed-meshheading:21392990-Hydrogen Bonding,
pubmed-meshheading:21392990-Hydrophobic and Hydrophilic Interactions,
pubmed-meshheading:21392990-Peptide Hydrolases,
pubmed-meshheading:21392990-Peptides,
pubmed-meshheading:21392990-Protease Inhibitors,
pubmed-meshheading:21392990-Structure-Activity Relationship
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pubmed:year |
2011
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pubmed:articleTitle |
Design and synthesis of several small-size HTLV-I protease inhibitors with different hydrophilicity profiles.
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pubmed:affiliation |
Department of Medicinal Chemistry, Center for Frontier Research in Medicinal Science, Kyoto Pharmaceutical University, Yamashina-ku, Kyoto 607-8412, Japan.
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
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