INDEX
Introduction
Page
Tyrosine Kinase Receptors (RTKs) 1
The Epidermal Growth Factor Receptor EGFR 4
Growth Factor and Receptor Activation 7
EGFR Signalling Pathways 9
EGFR and Cancer 12
Gating EGFR 14
The Epidermal Growth Factor EGF 15
EGFR inhibitors 18
News on the Clinical Use of EGFR inhibitors 21
Resistance to “EGFR-targeting” therapies 22
New Treatment Guidelines 24
Direct and Indirect Targeting of Angiogenesis Pathways 24
Vascular Endothelial Growth Factor and Receptors VEGF/VEGFR 25
VEGFR signalling 27
Relationship Between EGFR and VEGF Signalling Pathways 29 VEGFR and Dual VEGFR/EGFR Targeted Therapies 29
Introduction to Experimental Section
Design of Tyrosine Kinase Inhibitors 32
New Pyrazolo[3,4-d]pyrimidines 47
Chemical Synthesis 50
