Irvine protein kinases atp binding site gln 767 h2 oc

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Unformatted text preview: odify purine scaffold for kinase inhibitors 6nM Combichem: future prospects •  Combichem is important and an established part of the drug discovery process •  Emphasis is on making smaller, focused libraries •  Expedites target SAR and lead idenAficaAon Kinase Review Protein Kinases • Enzymes that catalyse phosphoryla>on reac>ons on protein substrates • 500- 2000 es>mated protein kinases in a cell • Protein kinases are present in the cytoplasm • Protein kinase receptors - dual role as receptor and enzyme • Overexpression can result in cancer • Tyrosine kinases, serine- threonine kinases and his>dine kinases • ATP used as enzyme cofactor - phosphoryla>ng agent H N N 1 6 N H H N O H H H OH H OH OP O O OP O N O OP N O N 6 H N O O 1 N O OP O H O OP O O H H OH H OH OP O N O O O Protein Kinases Tyrosine kinases Protein HH N O Protein Protein ATP OH HH N O Protein O ADP O P OH OH Protein Kinases Serine- threonine kinases HH N Protein O ATP Ser...
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