title: A simple set-and-mix assay for screening of protein kinase inhibitors in cell lysates.
abstract: Here we developed a simple set-and-mix assay to perform high-throughput screening of protein kinase A (PKA) inhibitors from the LOPAC 1280 compound library. This assay is based on the color change of gold nanoparticles on aggregation induced by a cationic substrate peptide as coagulant. In spite of the simplicity of this assay system, this assay can be applied to drug screening based on cellular kinases. We successfully found several highly active inhibitors, including compounds that have not been reported before.
authors.affiliation: Graduate School of Systems Life Sciences, Kyushu University, Nishi-ku, Fukuoka 819-0395, Japan.
authors.forename: Yoji
authors.initials: Y
authors.lastname: Asami
authors.forename: Jun
authors.initials: J
authors.lastname: Oishi
authors.forename: Hirotaro
authors.initials: H
authors.lastname: Kitazaki
authors.forename: Jumpei
authors.initials: J
authors.lastname: Kamimoto
authors.forename: Jeong-Hun
authors.initials: JH
authors.lastname: Kang
authors.forename: Takuro
authors.initials: T
authors.lastname: Niidome
authors.forename: Takeshi
authors.initials: T
authors.lastname: Mori
authors.forename: Yoshiki
authors.initials: Y
authors.lastname: Katayama
mesh_terms: D001665:Binding Sites; D001681:Biological Assay / Q000379:methods; D004353:Drug Evaluation, Preclinical / Q000379:methods; D006801:Humans; D053768:Metal Nanoparticles; D047428:Protein Kinase Inhibitors / Q000737:chemistry* / Q000494:pharmacology; D017346:Protein Serine-Threonine Kinases / Q000037:antagonists & inhibitors* / Q000378:metabolism; D014407:Tumor Cells, Cultured
chemical_list: D047428:Protein Kinase Inhibitors; D017346:Protein Serine-Threonine Kinases