Receptor tyrosine kinases: role in cancer progression

The mutation and deregulation of rtks can lead to a wide variety of changes in cellular structure and function, all of which contribute to the malignant phenotype and pathologic behaviour of human cancer. The progress in recent years on the clinical validation of molecularly targeted drugs that inhibit rtks has demonstrated that, in appropriately selected patients, treatment can alter disease progression and survival. Rational drug design will benefit from computational biology and a detailed understanding at the structural level both of the kinase domains and of the ligand binding sites of these receptors. The large tissue and serum repositories from patients in clinical trials will also allow outcome to be linked to molecular changes observed in tumours.