New Lead Generation Strategies for Protein Kinase Inhibitors - Fragment Based Screening Approaches

Author(s): Adrian Gill

Journal Name: Mini-Reviews in Medicinal Chemistry

Volume 4 , Issue 3 , 2004

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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.

Keywords: kinase inhibitors, x-ray crystallography, lead generation, structure-based drug design, virtual screening

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Article Details

Year: 2004
Page: [301 - 311]
Pages: 11
DOI: 10.2174/1389557043487385
Price: $65

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PDF: 11