Protein kinase inhibitors highlight the complexities of drug-target non-covalen interactions

作者：Engh R^*

来源：Biotechnology & Biotechnological Equipment, 2008, 22(3): 772-777.

• protein kinase
• drug discovery
• cancer
• CML
• aurora kinase
• ABL kinase
• protein crystallography

Atomic resolution structures of drug targets enable drug disco vet:v. but generally riot by a simple programatic process. A popular expectation is that a simple target structure will reveal what is needed to block its pathogenic activity. In contrast, the practical experience of recent years shows how complexities at ever:v stage of drug discovery processes challenge predictivity. This is true riot only at the scale of the biological organism, but also at the atomic scale, with respect to the drug-target interactions. Fortunately, high throughput experimental methods and data mining techniques cued in combination continue to revolutionize pharmaceutical research. This article illustrates how "structure based drug design might rather he considered ".structure assisted drug discovery." with examples taken from the major- emerging class of anticancer drugs, protein kinase inhibitors.

• 出版日期2008-8