Pranlukast, a novel binding ligand of human Raf1 kinase inhibitory protein
Objectives To study the binding of pranlukast to hRKIP and its regulatory role in the Raf1/MEK/ERK signal pathway. Results NMR and fluorescence experiments demonstrated hRKIP could bind pranlukast with a binding constant of 1016 $ mM^{−1} $. Residues (Y81, S109 and Y181) on the conserved ligand-binding pocket of hRKIP played a crucial role in binding pranlukast, and their mutations reduced the binding affinity more than 85 %. Furthermore, 25 μM pranlukast could up-regulate the ERK phosphorylation by about 17 %. Conclusion Pranlukast may be used as a potential drug precursor for treating hRKIP involved diseases..
| Medienart: |
Artikel |
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| Erscheinungsjahr: |
2016 |
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| Erschienen: |
2016 |
| Enthalten in: |
Zur Gesamtaufnahme - volume:38 |
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| Enthalten in: |
Biotechnology letters - 38(2016), 8 vom: 05. Mai, Seite 1375-1380 |
| Sprache: |
Englisch |
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| Beteiligte Personen: |
Sun, Tao [VerfasserIn] |
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| Links: |
Volltext [lizenzpflichtig] |
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| Themen: |
ERK phosphorylation level |
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| Anmerkungen: |
© Springer Science+Business Media Dordrecht 2016 |
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| doi: |
10.1007/s10529-016-2117-0 |
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| funding: |
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| Förderinstitution / Projekttitel: |
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OLC2050336640 |
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| 520 | |a Objectives To study the binding of pranlukast to hRKIP and its regulatory role in the Raf1/MEK/ERK signal pathway. Results NMR and fluorescence experiments demonstrated hRKIP could bind pranlukast with a binding constant of 1016 $ mM^{−1} $. Residues (Y81, S109 and Y181) on the conserved ligand-binding pocket of hRKIP played a crucial role in binding pranlukast, and their mutations reduced the binding affinity more than 85 %. Furthermore, 25 μM pranlukast could up-regulate the ERK phosphorylation by about 17 %. Conclusion Pranlukast may be used as a potential drug precursor for treating hRKIP involved diseases. | ||
| 650 | 4 | |a ERK phosphorylation level | |
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| 700 | 1 | |a Luo, Mengyao |4 aut | |
| 700 | 1 | |a Lin, Donghai |4 aut | |
| 700 | 1 | |a Guo, Chenyun |4 aut | |
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