A tyrosine-reactive irreversible inhibitor for glutathione S-transferase Pi (GSTP1).
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.
Department of Chemistry, Merkert Chemistry Center, Boston College, 2609 Beacon Street, Chestnut Hill, MA 02467, USA. eranthie@bc.edu.
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Crawford
Department of Chemistry, Merkert Chemistry Center, Boston College, 2609 Beacon Street, Chestnut Hill, MA 02467, USA. eranthie@bc.edu.
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Weerapana
D004791:Enzyme Inhibitors / Q000737:chemistry* / Q000494:pharmacology; D051549:Glutathione S-Transferase pi / Q000037:antagonists & inhibitors / Q000737:chemistry*; D006801:Humans; D008958:Models, Molecular; D008968:Molecular Conformation; D015394:Molecular Structure; D011485:Protein Binding; D013329:Structure-Activity Relationship; D014443:Tyrosine / Q000737:chemistry*
D004791:Enzyme Inhibitors; D014443:Tyrosine; D051549:Glutathione S-Transferase pi