rdf:type |
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lifeskim:mentions |
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pubmed:issue |
17
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pubmed:dateCreated |
2007-8-7
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pubmed:abstractText |
NP603, the 6-dimethoxy phenyl indolin-2-one, was designed as FGF receptor 1 inhibitor by computational study. NP603 was synthesized and found to be more active against endothelial proliferation of HUVEC after the rhFGF-2 stimulation than SU6668 with minimum effective dose of 0.4 microM but with similar potency as SU16g. NP603 inhibited the tyrosine phosphorylation in FGF receptor and the activation of extracellular signal-regulated kinase and c-Jun-N-terminal-kinase after the rhFGF-2 stimulation. The increase in activity of NP603 supports the role of Lys514 movement in ligand-receptor binding in modeling study as the movement accommodates the hydrophobic interaction at the receptor pocket leading to the enhancement of binding capacity.
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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 |
http://linkedlifedata.com/resource/pubmed/chemical/Enzyme Inhibitors,
http://linkedlifedata.com/resource/pubmed/chemical/Fibroblast Growth Factor 1,
http://linkedlifedata.com/resource/pubmed/chemical/Indoles,
http://linkedlifedata.com/resource/pubmed/chemical/JNK Mitogen-Activated Protein...,
http://linkedlifedata.com/resource/pubmed/chemical/Lysine,
http://linkedlifedata.com/resource/pubmed/chemical/PD 173074,
http://linkedlifedata.com/resource/pubmed/chemical/Pyrimidines,
http://linkedlifedata.com/resource/pubmed/chemical/Pyrroles,
http://linkedlifedata.com/resource/pubmed/chemical/Receptor, Fibroblast Growth...,
http://linkedlifedata.com/resource/pubmed/chemical/SU 6668
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pubmed:status |
MEDLINE
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pubmed:month |
Sep
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pubmed:issn |
0960-894X
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pubmed:author |
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pubmed:issnType |
Print
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pubmed:day |
1
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pubmed:volume |
17
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
4812-8
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pubmed:dateRevised |
2009-11-19
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pubmed:meshHeading |
pubmed-meshheading:17618113-Chemistry, Pharmaceutical,
pubmed-meshheading:17618113-Crystallography, X-Ray,
pubmed-meshheading:17618113-Dose-Response Relationship, Drug,
pubmed-meshheading:17618113-Drug Design,
pubmed-meshheading:17618113-Enzyme Inhibitors,
pubmed-meshheading:17618113-Fibroblast Growth Factor 1,
pubmed-meshheading:17618113-Humans,
pubmed-meshheading:17618113-Hydrogen Bonding,
pubmed-meshheading:17618113-Indoles,
pubmed-meshheading:17618113-JNK Mitogen-Activated Protein Kinases,
pubmed-meshheading:17618113-Lysine,
pubmed-meshheading:17618113-Models, Chemical,
pubmed-meshheading:17618113-Molecular Conformation,
pubmed-meshheading:17618113-Pyrimidines,
pubmed-meshheading:17618113-Pyrroles,
pubmed-meshheading:17618113-Receptor, Fibroblast Growth Factor, Type 1
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pubmed:year |
2007
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pubmed:articleTitle |
Novel inhibitor for fibroblast growth factor receptor tyrosine kinase.
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pubmed:affiliation |
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Mahidol University, Bangkok, Thailand.
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
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