Publication: Novel inhibitor for fibroblast growth factor receptor tyrosine kinase
2
Issued Date
2007-09-01
Resource Type
ISSN
0960894X
Other identifier(s)
2-s2.0-34547498439
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Mahidol University
Rights Holder(s)
SCOPUS
Bibliographic Citation
Bioorganic and Medicinal Chemistry Letters. Vol.17, No.17 (2007), 4812-4818
Suggested Citation
Naparat Kammasud, Chantana Boonyarat, Satoshi Tsunoda, Hiroaki Sakurai, Ikuo Saiki, David S. Grierson, Opa Vajragupta Novel inhibitor for fibroblast growth factor receptor tyrosine kinase. Bioorganic and Medicinal Chemistry Letters. Vol.17, No.17 (2007), 4812-4818. doi:10.1016/j.bmcl.2007.06.058 Retrieved from: https://repository.li.mahidol.ac.th/handle/123456789/24136
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Title
Novel inhibitor for fibroblast growth factor receptor tyrosine kinase
Abstract
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 μM 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. © 2007 Elsevier Ltd. All rights reserved.