423 / 1851
EGFR Mutation
Y1068
delE746-A750
delL747-T751
delL747-P753
G719C
L858R
L861Q
catalytic kinase
domain
transmembrane
domain
extracellular ligand
binding domain
specific mutations confer
sensitivity of EGFR-TK
activity to gefitinib/iressa
in NSCLC patients !
s
10
1
0.1
0.01
0.001
0
20
40
60
80
100
120
Gefitinib concentration (
µ
M)
Cell viability (% of control)
H3255 (L858R mutation)
H1781 (WT)
H1666 (WT)
H441 (WT)
EGFR Mutations (gain of function) are associated with Increased Sensitivity to Gefitinib