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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.

SUBMITTER: Crawford LA 

PROVIDER: S-EPMC4879005 | biostudies-literature | 2016 May

REPOSITORIES: biostudies-literature

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

Crawford L A LA   Weerapana E E  

Molecular bioSystems 20160501 6

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. ...[more]

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