title: Fluorescent monitoring of kinase activity in real time: development of a robust fluorescence-based assay for Abl tyrosine kinase activity.
abstract: Fluorescent biosensors hold great promise for drug discovery. Using a solid-phase version of protein semi-synthesis, we incorporated two fluorophores at specific sites within a truncated version of the c-Crk-II protein. The resulting fluorescent protein biosensor permits the real-time monitoring of Abl kinase activity and provides a robust and rapid method for assaying Abl kinase inhibitors.
authors.affiliation: Laboratory of Synthetic Protein Chemistry, The Rockefeller University, New York, NY 10021, USA.
authors.forename: R M
authors.initials: RM
authors.lastname: Hofmann
authors.forename: G J
authors.initials: GJ
authors.lastname: Cotton
authors.forename: E J
authors.initials: EJ
authors.lastname: Chang
authors.forename: E
authors.initials: E
authors.lastname: Vidal
authors.forename: D
authors.initials: D
authors.lastname: Veach
authors.forename: W
authors.initials: W
authors.lastname: Bornmann
authors.forename: T W
authors.initials: TW
authors.lastname: Muir
mesh_terms: D000595:Amino Acid Sequence; D015374:Biosensing Techniques; D004791:Enzyme Inhibitors / Q000494:pharmacology; D016315:Proto-Oncogene Proteins c-abl / Q000037:antagonists & inhibitors / Q000378:metabolism*; D013050:Spectrometry, Fluorescence
chemical_list: D004791:Enzyme Inhibitors; D016315:Proto-Oncogene Proteins c-abl