Abstract
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
Mini-Reviews in Medicinal Chemistry
Title: New Lead Generation Strategies for Protein Kinase Inhibitors - Fragment Based Screening Approaches
Volume: 4 Issue: 3
Author(s): Adrian Gill
Affiliation:
Keywords: kinase inhibitors, x-ray crystallography, lead generation, structure-based drug design, virtual screening
Abstract: 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.
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Cite this article as:
Gill Adrian, New Lead Generation Strategies for Protein Kinase Inhibitors - Fragment Based Screening Approaches, Mini-Reviews in Medicinal Chemistry 2004; 4 (3) . https://dx.doi.org/10.2174/1389557043487385
DOI https://dx.doi.org/10.2174/1389557043487385 |
Print ISSN 1389-5575 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5607 |
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