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Kinetic controlled affinity labeling of target enzyme with thioester chemistry.

Abstract：

:High specificity has been an important feature in affinity labeling for target profiling. Especially, to label targets via rapidly progressing reactions with consumption of ligand (probe), high specificity of reaction with common functional groups of target protein should be achieved without reactions with similar groups of non-target proteins. Herein, we demonstrate the kinetic controlled affinity labeling of acyl CoA synthetase using a fatty acid analogue containing a phenylthioester linkage. High specificity was attained by accelerating the labeling rate in the binding pocket. This approach could be useful for profiling a series of target enzymes and transporters in signal transduction pathways.

journal_name

Bioorg Med Chem

journal_title

Bioorganic & medicinal chemistry

authors

Tomohiro T,Nakabayashi M,Sugita Y,Morimoto S

doi

10.1016/j.bmc.2016.05.059

subject

Has Abstract

pub_date

2016-08-01 00:00:00

pages

3336-41

issue

15

eissn

0968-0896

issn

1464-3391

pii

S0968-0896(16)30403-5

journal_volume

24

pub_type

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