Kinase_Lecture_MedChem2

Hn 4 n ch3 6 small lipophilic group ome electron

Info iconThis preview shows page 1. Sign up to view the full content.

View Full Document Right Arrow Icon
This is the end of the preview. Sign up to access the rest of the document.

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://www.cdc.gov/cancer/lung/ 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...
View Full Document

This note was uploaded on 01/15/2014 for the course CHEM 167 taught by Professor Amaro during the Winter '13 term at UCSD.

Ask a homework question - tutors are online