Autor: |
Aronov, A. M., Murcko, M. A. |
Zdroj: |
Journal of Medicinal Chemistry; November 2004, Vol. 47 Issue: 23 p5616-5619, 4p |
Abstrakt: |
Small molecule protein kinase inhibitors are widely employed as biological reagents and as leads in the design of drugs for a variety of diseases. One of the hardest challenges in kinase inhibitor design is achieving target selectivity. By utilizing X-ray structural information for four promiscuous inhibitors, we propose a five-point pharmacophore for kinase frequent hitters, demonstrate its ability to discriminate between frequent hitters and selective ligands, and suggest a strategy for selective inhibitor design. |
Databáze: |
Supplemental Index |
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