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

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.

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