Rational design of potent GSK3beta inhibitors with selectivity for Cdk1 and Cdk2

From an HTS hit, a series of potent and selective inhibitors of GSK3beta have been designed based on a Cdk2-homology model and with the help of several crystal structures of the compounds within Cdk2.

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Bibliographische Detailangaben
Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2010-03, Vol.20 (6), p.1985-1989
Hauptverfasser:	Lesuisse, Dominique, Dutruc-Rosset, Gilles, Tiraboschi, Gilles, Dreyer, Matthias K, Maignan, Sébastien, Chevalier, Alain, Halley, Frank, Bertrand, Philippe, Burgevin, Marie-Claude, Quarteronet, Dominique, Rooney, Thomas
Format:	Artikel
Sprache:	eng
Schlagworte:	CDC2 Protein Kinase - antagonists & inhibitors Cyclin-Dependent Kinase 2 - antagonists & inhibitors Drug Design Glycogen Synthase Kinase 3 - antagonists & inhibitors Glycogen Synthase Kinase 3 beta Models, Molecular Protein Kinase Inhibitors - chemistry Protein Kinase Inhibitors - pharmacology Substrate Specificity
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Beschreibung
Zusammenfassung:	From an HTS hit, a series of potent and selective inhibitors of GSK3beta have been designed based on a Cdk2-homology model and with the help of several crystal structures of the compounds within Cdk2.
ISSN:	1464-3405
DOI:	10.1016/j.bmcl.2010.01.114