Fluorescent monitoring of kinase activity in real time: Development of a robust fluorescence-based assay for Abl tyrosine kinase activity

Roseanne M. Hofmann; Graham J. Cotton; Emmanuel J. Chang; Ephraim Vidal; Darren Veach; William Bornmann; Tom W. Muir

doi:10.1016/S0960-894X(01)00650-3

Fluorescent monitoring of kinase activity in real time: Development of a robust fluorescence-based assay for Abl tyrosine kinase activity

Roseanne M. Hofmann, Graham J. Cotton, Emmanuel J. Chang, Ephraim Vidal, Darren Veach, William Bornmann, Tom W. Muir

Research output: Contribution to journal › Article › peer-review

26 Scopus citations

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.

Original language	English (US)
Pages (from-to)	3091-3094
Number of pages	4
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	11
Issue number	24
DOIs	https://doi.org/10.1016/S0960-894X(01)00650-3
State	Published - Dec 17 2001
Externally published	Yes

All Science Journal Classification (ASJC) codes

Drug Discovery
Molecular Medicine
Molecular Biology
Biochemistry
Clinical Biochemistry
Pharmaceutical Science
Organic Chemistry

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10.1016/S0960-894X(01)00650-3

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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.",

author = "Hofmann, {Roseanne M.} and Cotton, {Graham J.} and Chang, {Emmanuel J.} and Ephraim Vidal and Darren Veach and William Bornmann and Muir, {Tom W.}",

note = "Funding Information: We thank T. Schindler and J. Kuriyan (Rockefeller University) for recombinant c-Abl protein. We thank Mike Goger for assistance with the microtiter plate reader. Supported by the Pew Charitable Trust, the Rockefeller University Presidential Fellowship (R.M.H.) and the Burroughs Wellcome Fund (G.C., E.C.).",

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doi = "10.1016/S0960-894X(01)00650-3",

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T1 - Fluorescent monitoring of kinase activity in real time

T2 - Development of a robust fluorescence-based assay for Abl tyrosine kinase activity

AU - Hofmann, Roseanne M.

AU - Cotton, Graham J.

AU - Chang, Emmanuel J.

AU - Vidal, Ephraim

AU - Veach, Darren

AU - Bornmann, William

AU - Muir, Tom W.

N1 - Funding Information: We thank T. Schindler and J. Kuriyan (Rockefeller University) for recombinant c-Abl protein. We thank Mike Goger for assistance with the microtiter plate reader. Supported by the Pew Charitable Trust, the Rockefeller University Presidential Fellowship (R.M.H.) and the Burroughs Wellcome Fund (G.C., E.C.).

PY - 2001/12/17

Y1 - 2001/12/17

N2 - 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.

AB - 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.

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Fluorescent monitoring of kinase activity in real time: Development of a robust fluorescence-based assay for Abl tyrosine kinase activity

Abstract

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