Discovery of an Aurora kinase inhibitor through site-specific dynamic combinatorial chemistry

We demonstrate a fragment-based lead discovery method that combines site-directed ligand discovery with dynamic combinatorial chemistry to identify inhibitors of Aurora kinase A. We demonstrate a fragment-based lead discovery method that combines site-directed ligand discovery with dynamic combinato...

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Veröffentlicht in:	Bioorganic & medicinal chemistry 2008-07, Vol.18 (14), p.3978-3981
Hauptverfasser:	Cancilla, Mark T., He, Molly M., Viswanathan, Nina, Simmons, Robert L., Taylor, Meggin, Fung, Amy D., Cao, Kathy, Erlanson, Daniel A.
Format:	Artikel
Sprache:	eng
Schlagworte:	Aurora Aurora Kinases Binding Sites - drug effects Biological and medical sciences Chemistry, Pharmaceutical - methods Combinatorial Chemistry Techniques - methods Crystallography, X-Ray Cysteine DCC DFG-out Drug Design Dynamic combinatorial chemistry Enzyme Inhibitors - chemical synthesis Enzyme Inhibitors - chemistry FBLD Fragment-based Fragment-based lead discovery Kinase Ligands Mass Spectrometry - methods Mass-spectrometry Medical sciences Miscellaneous Models, Chemical Molecular Structure Pharmacology. Drug treatments Protein-Serine-Threonine Kinases - antagonists & inhibitors Purines - chemistry Site-directed Structure-Activity Relationship
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