Generic placeholder image

Combinatorial Chemistry & High Throughput Screening


ISSN (Print): 1386-2073
ISSN (Online): 1875-5402

Chemical Libraries Towards Protein Kinase Inhibitors

Author(s): R. D.A. Kimmich and W. K. -C. Park

Volume 6, Issue 7, 2003

Page: [661 - 672] Pages: 12

DOI: 10.2174/138620703771981223

Price: $65


Over 500 human protein kinases identified to date are susceptible to play crucial roles in the regulation of many signal transduction pathways, making them significant drug discovery targets. However, their active sites share a high level of similarity, which constitutes a major challenge in the finding of selective and safe inhibitors. In order to meet this challenge, whether via traditional or alternative approaches, the use of chemical libraries to find either unknown natural ligands or specific inhibitors of particular kinases is more important than ever. This review briefly summarizes the recent literature on such libraries of peptides, natural product analogues, and small molecules. Significant chemical scaffolds, some synthetic routes particularly on solid-phase support, and computational tools employed for the efficient design of both selective and bioavailable inhibitors are highlighted.

Keywords: chemical libraries, protein kinase inhibitors, signal transduction pathways, chemical scaffolds, solid-phase support

Rights & Permissions Print Export Cite as
© 2023 Bentham Science Publishers | Privacy Policy