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Developments of bioorthogonal handle-containing photo-crosslinkers for photoaffinity labeling

Abstract

Photoaffinity labeling (PAL) has been widely applied in various research areas such as medicinal chemistry, chemical biology and structural biology, owing to its capability of interrogating non-covalent ligand-protein interactions under native environments and elucidating protein structures and functions etc. One important application of this technique is that using affinity-based proteome profiling (AfBP) coupled with bioimaging to profile drug-target interactions in situ. In order to accurately report drug-target interactions via these approaches, following considerations need to be made: (1) maximumly reserving bioactivities of photoprobes upon functionalizing with a photoreactive group and a reporter tag from a parental compound; (2) performing proteome profiling and imaging in situ simultaneously, so as to monitor drug-target interations in different manners; (3) developing excellent photo-crosslinkers capable of photo-crosslinking and fluorescence Turn-On at the same time. With these considerations in mind, we have developed three versions of “minimalist” bioorthogonal handle-containing photo-crosslinkers (L3-L6) during these years, and successfully applied them in all kinds of small bioactive molecules for protein labeling and cellular imaging studies. In this mini-review, the features and functions of these linkers are highlighted.

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Publication details

The article was received on 30 Apr 2017, accepted on 14 Jun 2017 and first published on 14 Jun 2017


Article type: Review Article
DOI: 10.1039/C7MD00217C
Citation: Med. Chem. Commun., 2017, Accepted Manuscript
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    Developments of bioorthogonal handle-containing photo-crosslinkers for photoaffinity labeling

    Z. Li and H. Guo, Med. Chem. Commun., 2017, Accepted Manuscript , DOI: 10.1039/C7MD00217C

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