Iminoboronates as Dual-Purpose Linkers in Chemical Probe Development.
Chemistry
; 27(10): 3292-3296, 2021 Feb 15.
Article
em En
| MEDLINE
| ID: mdl-33259638
ABSTRACT
Chemical probes that covalently modify proteins of interest are powerful tools for the research of biological processes. Important in the design of a probe is the choice of reactive group that forms the covalent bond, as it decides the success of a probe. However, choosing the right reactive group is not a simple feat and methodologies for expedient screening of different groups are needed. We herein report a modular approach that allows easy coupling of a reactive group to a ligand. α-Nucleophile ligands are combined with 2-formylphenylboronic acid derived reactive groups to form iminoboronate probes that selectively label their target proteins. A transimination reaction on the labeled proteins with an α-amino hydrazide provides further modification, for example to introduce a fluorophore.
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MEDLINE
Idioma:
En
Ano de publicação:
2021
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Article