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Mini-Reviews in Medicinal Chemistry


ISSN (Print): 1389-5575
ISSN (Online): 1875-5607

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

Author(s): Adrian Gill

Volume 4, Issue 3, 2004

Page: [301 - 311] Pages: 11

DOI: 10.2174/1389557043487385

Price: $65


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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