Structural analysis of sulindac as an inhibitor of aldose reductase and AKR1B10

•The X-ray structure of AKR1B10 with NADP+ and the NSAID sulindac has been solved.•Sulindac and sulindac sulfone inhibit AR with increased selectivity over AKR1B10.•Sulindac and its sulfone might be leads for selective AR and AKR1B10 inhibitors.•Derivative K-80003 could be used both as an AKR inhibi...

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Veröffentlicht in:	Chemico-biological interactions 2015-06, Vol.234, p.290-296
Hauptverfasser:	Cousido-Siah, Alexandra, Ruiz, Francesc X., Crespo, Isidro, Porté, Sergio, Mitschler, André, Parés, Xavier, Podjarny, Alberto, Farrés, Jaume
Format:	Artikel
Sprache:	eng
Schlagworte:	Aldehyde Reductase - antagonists & inhibitors Aldehyde Reductase - metabolism Aldose reductase inhibitor Anti-Inflammatory Agents, Non-Steroidal - pharmacology Chemotherapy Colorectal cancer Humans Inhibition kinetics NADP - metabolism Non-steroidal anti-inflammatory drug Prostaglandin-Endoperoxide Synthases - metabolism Prostaglandins - metabolism Structure-Activity Relationship Sulindac - pharmacology Three-dimensional structure
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