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Mini Rev Med Chem. 2004 Mar;4(3):301-11.

New lead generation strategies for protein kinase inhibitors - fragment based screening approaches.

Author information

  • Astex Technology, 436 Cambridge Science Park, Milton Road, Cambridge, CB4 0QA, UK. a.gill@astex-technology.com


The protein kinase superfamily represents both an enormous opportunity and a unique challenge for drug discovery. Protein kinases play central roles in the cellular economy and it is well known that a large number of diseases involve aberrant protein kinase activity. This review discusses how fragment based screening strategies, such as virtual screening, NMR and high-throughput X-ray crystallography are being employed to identify new chemo-types to produce the next generation of protein kinase inhibitors.

[PubMed - indexed for MEDLINE]
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