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

  • Mol Biosyst. 2016 May 24;12(6):1768-71. doi: 10.1039/c6mb00250a.
L A Crawford  1 ,  E Weerapana  1
Affiliations
  • 1. Department of Chemistry, Merkert Chemistry Center, Boston College, 2609 Beacon Street, Chestnut Hill, MA 02467, USA. [email protected].
PMID: 27113843 DOI: 10.1039/c6mb00250a
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.

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