Design and synthesis of a heterocyclic compound collection for probing the spatial charactistics of ATP binding sites

Abstract

Recent years have brought about serious interest in the kinases as potential therapeutic targets in a variety of disease conditions. Much of this interest has centred around the preparation and utilisation of species which interact with the ATP binding site of the kinase under investigation. Contrary to what one would expect, there is substantial variation in the nature of the ATP binding sites of differing kinases - the implications of this being the potential for the generation of ATP site-specific inhibitors which interact with only a limited group of kinases. The preparation of a collection of small heterocyclic compounds to probe differences in the spatial characteristics of ATP binding sites across the kinome is described