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A simple set-and-mix assay for screening of protein kinase inhibitors in cell lysates |
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| Authors: | Asami Yoji Oishi Jun Kitazaki Hirotaro Kamimoto Jumpei Kang Jeong-Hun Niidome Takuro Mori Takeshi Katayama Yoshiki |
| Institution: | aGraduate School of Systems Life Sciences, Kyushu University, Nishi-ku, Fukuoka 819-0395, Japan;bDepartment of Applied Chemistry, Faculty of Engineering, Kyushu University, Nishi-ku, Fukuoka 819-0395, Japan;cCenter for Future Chemistry, Kyushu University, Nishi-ku, Fukuoka 819-0395, Japan;dCenter for Advanced Medical Innovation, Kyushu University, Higashi-ku, Fukuoka 812-8582, Japan |
| 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. |
| Keywords: | Protein kinase Cell-based drug screening Gold nanoparticles Colorimetry |
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