Journal
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION
Volume 58, Issue 42, Pages 15000-15004Publisher
WILEY-V C H VERLAG GMBH
DOI: 10.1002/anie.201909536
Keywords
fluorescence; inhibitors; kinase; solvatochromism
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Funding
- European Union's Horizon 2020 programme [745626]
- Swedish Research Council [2016-03601, 2015-05268]
- Olle Engkvist Byggmastare Foundation
- Swedish Research Council [2016-03601, 2015-05268] Funding Source: Swedish Research Council
- Marie Curie Actions (MSCA) [745626] Funding Source: Marie Curie Actions (MSCA)
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The development of a fluorescent LCK inhibitor that exhibits favourable solvatochromic properties upon binding the kinase is described. Fluorescent properties were realised through the inclusion of a prodan-derived fluorophore into the pharmacophore of an ATP-competitive kinase inhibitor. Fluorescence titration experiments demonstrate the solvatochromic properties of the inhibitor, in which dramatic increase in emission intensity and hypsochromic shift in emission maxima are clearly observed upon binding LCK. Microscopy experiments in cellular contexts together with flow cytometry show that the fluorescence intensity of the inhibitor correlates with the LCK concentration. Furthermore, multiphoton microscopy experiments demonstrate both the rapid cellular uptake of the inhibitor and that the two-photon cross section of the inhibitor is amenable for excitation at 700 nm.
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