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An in situ combinatorial methodology to synthesize and screen chemical probes

Author:
van der ZouwenThese authors contributed equally., Antonie J., Lohse, Jonas, Wieske, Lianne H. E., Hohmann, Katharina F., van der Vlag, Ramon, Witte, Martin D.
Source:
Chemical communications 2019 v.55 no.14 pp. 2050-2053
ISSN:
1364-548X
Subject:
antibacterial properties, chemical bonding, chemical communication, chemical reactions, chloramphenicol acetyltransferase, imines, proteins, screening
Abstract:
Chemical probes that label proteins of interest in the context of complex biological samples are useful research tools. The reactive group that forms the covalent bond with the target protein has a large effect on the selectivity and selecting the appropriate group determines the success of a probe. We here report the development of a combinatorial methodology based on imine chemistry that enables straightforward in situ synthesis and screening of different reactive groups and thereby simplifies identification of probe leads. Using our methodology, we found chemical probes targeting BirA and chloramphenicol acetyl transferase, two proteins associated with antibacterial activity and resistance.
Agid:
6308036