Issue 6, 2016

A tyrosine-reactive irreversible inhibitor for glutathione S-transferase Pi (GSTP1)

Abstract

Glutathione S-transferase Pi (GSTP1) mediates cellular defense against reactive electrophiles. Here, we report LAS17, a dichlorotriazine-containing compound that irreversibly inhibits GSTP1 and is selective for GSTP1 within cellular proteomes. Mass spectrometry and mutational studies identified Y108 as the site of modification, providing a unique mode of GSTP1 inhibition.

Graphical abstract: A tyrosine-reactive irreversible inhibitor for glutathione S-transferase Pi (GSTP1)

Supplementary files

Article information

Article type
Communication
Submitted
04 Apr. 2016
Accepted
21 Apr. 2016
First published
22 Apr. 2016

Mol. BioSyst., 2016,12, 1768-1771

A tyrosine-reactive irreversible inhibitor for glutathione S-transferase Pi (GSTP1)

L. A. Crawford and E. Weerapana, Mol. BioSyst., 2016, 12, 1768 DOI: 10.1039/C6MB00250A

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