Issue 5, 2013
From the journal:

Chemical Science

Selective affinity-based probe for oncogenic kinases suitable for live cell imaging†

Claudio Zambaldo,a   Kalyan K. Sadhu,a   Ganesan Karthikeyan,a   Sofia Barluenga,a   Jean-Pierre Daguera  and  Nicolas Winssinger*ab  

* Corresponding authors

a Institut de Science et Ingénierie Supramoléculaires (ISIS – UMR 7006), Université de Strasbourg – CNRS, 8 allée Gaspard Monge, F67000 Strasbourg, France

b Department of Organic Chemistry, University of Geneva, 30 quai Ernest Ansermet, CH-1211 Geneva 4, Switzerland
E-mail: Nicolas.Winssinger@unige.ch

Abstract

Cell permeable probes to image the presence and localization of kinases are important in studying their function and as diagnostic tools. Despite the central role of kinases as therapeutic targets, there are remarkably few probes available. Herein we report the discovery of a probe to image two therapeutically relevant kinases: EGFR and ERBB2. The probe was identified from a library based on a scaffold derived from the resorcyclic acid lactones that form a covalent adduct by reacting specifically with an unconserved cysteine in the nucleotide-binding site of the kinases. We demonstrated the utility of the newly discovered probe by imaging of EGFR localization and ERBB2 inhibition in live cells.

Graphical abstract: Selective affinity-based probe for oncogenic kinases suitable for live cell imaging

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Article information

DOI
https://doi.org/10.1039/C3SC21856B
Article type
Edge Article
Submitted
29 Oct 2012
Accepted
11 Mar 2013
First published
13 Mar 2013

Chem. Sci., 2013,4, 2088-2092

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Selective affinity-based probe for oncogenic kinases suitable for live cell imaging

C. Zambaldo, K. K. Sadhu, G. Karthikeyan, S. Barluenga, J. Daguer and N. Winssinger, Chem. Sci., 2013, 4, 2088 DOI: 10.1039/C3SC21856B

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