ABSTRACT
This chapter looks at the design of inhibitors against a tyrosine kinase-linked receptor called the epidermal growth factor (EGF) receptor. Tyrosine kinase-linked receptors are important to cell growth and cell division. They have a dual action in that they act both as a receptor and as an enzyme. Kinase-linked receptors are found to be overexpressed in many cancers, so inhibitors may be potential anticancer agents. The overexpression of the receptors is caused by overexpression of the genes that code for them. Like other kinase linked receptors, the EGF receptor is located in the cell membrane and doubles up as a receptor and as an enzyme. Overexpression of EGF kinase has been observed in a variety of epithelial type cancers, such as squamous cell carcinoma, breast cancer, and ovarian cancer. Clearly, the active site of tyrosine kinase enzymes must contain two binding sites – one for the tyrosine residue and one for adenosine triphosphate.
