title: Pranlukast, a novel binding ligand of human Raf1 kinase inhibitory protein.
abstract: OBJECTIVE
  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 %.
  
  
  CONCLUSIONS
  Pranlukast may be used as a potential drug precursor for treating hRKIP involved diseases.
authors.affiliation: Department of Chemical Biology, College of Chemistry and Chemical Engineering, Xiamen University, 422 Siming South Road, Xiamen, 361005, Fujian, China.
authors.forename: Tao
authors.initials: T
authors.lastname: Sun
authors.affiliation: Department of Chemical Biology, College of Chemistry and Chemical Engineering, Xiamen University, 422 Siming South Road, Xiamen, 361005, Fujian, China.
authors.forename: Zhihua
authors.initials: Z
authors.lastname: Wu
authors.affiliation: Department of Chemical Biology, College of Chemistry and Chemical Engineering, Xiamen University, 422 Siming South Road, Xiamen, 361005, Fujian, China.
authors.forename: Mengyao
authors.initials: M
authors.lastname: Luo
authors.affiliation: Department of Chemical Biology, College of Chemistry and Chemical Engineering, Xiamen University, 422 Siming South Road, Xiamen, 361005, Fujian, China.
authors.forename: Donghai
authors.initials: D
authors.lastname: Lin
authors.affiliation: Department of Chemical Biology, College of Chemistry and Chemical Engineering, Xiamen University, 422 Siming South Road, Xiamen, 361005, Fujian, China. guochy78@xmu.edu.cn.
authors.forename: Chenyun
authors.initials: C
authors.lastname: Guo
mesh_terms: D002867:Chromones / Q000378:metabolism; D006801:Humans; D020935:MAP Kinase Signaling System; D009682:Magnetic Resonance Spectroscopy; D049488:Phosphatidylethanolamine Binding Protein / Q000378:metabolism*; D011485:Protein Binding; D019908:Proto-Oncogene Proteins c-raf / Q000378:metabolism
chemical_list: D002867:Chromones; D049488:Phosphatidylethanolamine Binding Protein; D019908:Proto-Oncogene Proteins c-raf; C047681:pranlukast
keywords: ERK phosphorylation level; Fluorescence; Ligand binding pocket; Phosphatidylethanolamine binding protein; Pranlukast; Protein binding; hRKIP