Reaction of COTC with Glutathione: Structure of the Putative Glyoxalase I Inhibitor

The structure of the active glyoxalase I inhibitor derived from the Streptomyces griseosporeus metabolite COTC 1 has been conclusively identified by means of total synthesis as 2c. Human glyoxalase I is competitively inhibited by 2c (K i = 183 ± 6 μM) but is not inhibited by 1 itself.

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Bibliographische Detailangaben
Veröffentlicht in:	Organic letters 2000-10, Vol.2 (20), p.3143-3144
Hauptverfasser:	Huntley, C. Frederick M, Hamilton, Diana S, Creighton, Donald J, Ganem, Bruce
Format:	Artikel
Sprache:	eng
Schlagworte:	Antibiotics, Antineoplastic - chemistry Cyclohexanones - chemistry Enzyme Inhibitors - chemical synthesis Enzyme Inhibitors - chemistry Glutathione - chemistry Humans Lactoylglutathione Lyase - antagonists & inhibitors Streptomyces - chemistry
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Beschreibung
Zusammenfassung:	The structure of the active glyoxalase I inhibitor derived from the Streptomyces griseosporeus metabolite COTC 1 has been conclusively identified by means of total synthesis as 2c. Human glyoxalase I is competitively inhibited by 2c (K i = 183 ± 6 μM) but is not inhibited by 1 itself.
ISSN:	1523-7060 1523-7052
DOI:	10.1021/ol006341z