Development of a novel fluorescent probe for fluorescence correlation spectroscopic detection of kinase inhibitors.
We have developed a fluorescently labeled probe for high-throughput screening of kinase inhibitors using fluorescence correlation spectroscopy. With this probe, we have successfully evaluated the inhibitory activities of known inhibitors of a model kinase, ASK1. Because the probe contains a general kinase inhibitor, staurosporine, we believe that this homogeneous, high-throughput, and simple method can be applied to the inhibitor screening of other kinases as well.
Graduate School of Pharmaceutical Sciences, The University of Tokyo, 7-3-1 Hongo, Bunkyo-ku, Tokyo 113-0033, Japan.
Mitsuyasu
M
Kawaguchi
Takuya
T
Terai
Rei
R
Utata
Miki
M
Kato
Keiko
K
Tsuganezawa
Akiko
A
Tanaka
Hirotatsu
H
Kojima
Takayoshi
T
Okabe
Tetsuo
T
Nagano
D002626:Chemistry, Pharmaceutical / Q000379:methods; D018360:Crystallography, X-Ray / Q000379:methods; D004353:Drug Evaluation, Preclinical; D005454:Fluorescence Polarization; D005456:Fluorescent Dyes / Q000494:pharmacology*; D006801:Humans; D020128:Inhibitory Concentration 50; D007700:Kinetics; D048848:MAP Kinase Kinase Kinase 5 / Q000378:metabolism; D008956:Models, Chemical; D008968:Molecular Conformation; D011485:Protein Binding; D047428:Protein Kinase Inhibitors / Q000737:chemistry / Q000494:pharmacology*; D013050:Spectrometry, Fluorescence / Q000295:instrumentation* / Q000379:methods*; D019311:Staurosporine / Q000737:chemistry / Q000494:pharmacology
D005456:Fluorescent Dyes; D047428:Protein Kinase Inhibitors; D048848:MAP Kinase Kinase Kinase 5; D019311:Staurosporine