INDEX
Introduction
Page
Tyrosine Kinase Receptors (RTKs) 1
The Epidermal Growth Factor Receptor EGFR 3
Growth Factor and Receptor Activation 6
EGFR Signalling Pathways 9
EGFR and Cancer 12
Gating EGFR 13
The Epidermal Growth Factor EGF Design of Tyrosine Kinase Inhibitors 14 17 EGFR inhibitors 20
News on the Clinical Use of EGFR inhibitors 26
Resistance to “EGFR-targeting” therapies 27
New Treatment Guidelines 28
Indirect and Direct Targeting of Angiogenesis Pathways 29
Vascular Endothelial Growth Factor and Receptors VEGF/VEGFR 29
VEGFR signalling 31
Anti-VEGFR Agents
Monoclonal Antibody
Small molecules TK Inhibitors
34 35 36
Introduction to Experimental Section
VEGFR-2 small molecules Inhibitors
Anthranilamides
Pyrimidine Derivatives
40 41 43 New Pyridothiopyrano Pyrimidines 49