Journal
BIOTECHNOLOGY LETTERS
Volume 38, Issue 8, Pages 1375-1380Publisher
SPRINGER
DOI: 10.1007/s10529-016-2117-0
Keywords
ERK phosphorylation level; Fluorescence; hRKIP; Ligand binding pocket; Pranlukast; Phosphatidylethanolamine binding protein; Protein binding
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Funding
- Natural Science Foundation of China [31470034]
- Fundamental Research Funds for the Central Universities [20720160033]
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To study the binding of pranlukast to hRKIP and its regulatory role in the Raf1/MEK/ERK signal pathway. 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 mu M pranlukast could up-regulate the ERK phosphorylation by about 17 %. Pranlukast may be used as a potential drug precursor for treating hRKIP involved diseases.
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