An Inhibitor of Glutathione S-Transferase Omega 1 that Selectively Targets Apoptotic Cells

On (cell) suicide watch: The increased permeability of apoptotic cells was used to identify a peptide‐based, covalent inhibitor (NJP2) for glutathione S‐transferase omega (GSTO1) that is highly selective for apoptotic cells, with no inhibition of healthy cells (see scheme). This apoptosis‐specific p...

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Veröffentlicht in:	Angewandte Chemie International Edition 2012-08, Vol.51 (33), p.8365-8368
Hauptverfasser:	Pace, Nicholas J., Pimental, Daniel R., Weerapana, Eranthie
Format:	Artikel
Sprache:	eng
Schlagworte:	Antineoplastic Agents - chemical synthesis Antineoplastic Agents - chemistry Antineoplastic Agents - pharmacology apoptosis Apoptosis - drug effects Dose-Response Relationship, Drug Drug Screening Assays, Antitumor Enzyme Inhibitors - chemical synthesis Enzyme Inhibitors - chemistry Enzyme Inhibitors - pharmacology glutathione S-transferase omega Glutathione Transferase - antagonists & inhibitors Glutathione Transferase - metabolism HeLa Cells Humans inhibitors Microscopy, Fluorescence Molecular Structure Neoplasms - drug therapy Neoplasms - enzymology Neoplasms - pathology peptides Peptides - chemical synthesis Peptides - chemistry Peptides - pharmacology protein modifications Structure-Activity Relationship
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Beschreibung
Zusammenfassung:	On (cell) suicide watch: The increased permeability of apoptotic cells was used to identify a peptide‐based, covalent inhibitor (NJP2) for glutathione S‐transferase omega (GSTO1) that is highly selective for apoptotic cells, with no inhibition of healthy cells (see scheme). This apoptosis‐specific peptide could also be used for imaging programmed cell death.
ISSN:	1433-7851 1521-3773
DOI:	10.1002/anie.201203730