Study of Inhibitors of Neu and Related Tyrosine-Specific Protein Kinases: Implications for the Treatment of Breast Cancer

摘要

Our objectives have been to develop synthetic modulators of tyrosine- specific protein kinases (TPKs) so that the biochemical consequences of their deregulation in breast cancer can be studied. These enzymes play a crucial, albeit still enigmatic role in the signal transduction pathways responsible for cell growth and differentiation. Upon the loss of key regulatory controls, either through the over-expression or mutation of specific PTKs, the oncogenic potential of these enzymes is unleashed. Regulatory agents, which disturb or otherwise alter the myriad of protein-protein recognition events that drive signal transduction pathways, will be extraordinarily useful in helping to decipher the role of specific enzymes in these pathways. In addition, these regulatory agents may ultimately provide the foundation upon which therapeutically useful compounds can be devised.