Hn 4 n ch3 6 small lipophilic group ome electron

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Unformatted text preview: ophobic pocket • The size of the gatekeeper residue is important in drug design • The nature of amino acids in the binding pockets is important to drug design O Protein Kinases Ac4ve Site • Contains the binding site for the protein substrate • Contains the binding site for the ATP cofactor • Clinically useful inhibitors target the ATP binding site • ATP binding site is similar but not iden4cal for all protein kinases • Allows selec4vity of inhibitor ac4on? EGFR kinase inhibitors •  Disease Target: Lung cancer –  More people die from lung cancer than any other cancer –  Over 158,000 deaths from lung cancer in 2009 (CDC) hOp:// Gefi4nib (Iressa): an EGFR- R kinase inhibitor F Aniline HN Cl 4 6 O 7 OMe N3 N Morpholine 1 N O Quinazoline Notes • Developed by Astra Zeneca • Inhibits the kinase ac4ve site of the epidermal growth factor receptor • The EGF- receptor is a tyrosine kinase receptor • Gefi4nib is a 4- anilinoquinazoline structure • Older inhibitor, typically only indicated in advanced cases of non- small cell lung cancer with EGFR muta4ons EGF- R kinase inhibitors ge...
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This note was uploaded on 01/15/2014 for the course CHEM 167 taught by Professor Amaro during the Winter '13 term at UCSD.

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