ATP site-directed kinase inhibitors

This symposium was organised by Dr Michael South (Monsanto/Searle Discovery Research, USA), and Dr Alex Bridges (Parke-Davis, MI USA), as a half-day symposium within the Medicinal Chemistry Division of the ACS. It was intended to provide an update to the chemical community of recent develop-ments in signal transduction enzymes, especially the progress towards clinical evaluation of a number of classes of ATP site-directed inhibitors. This is a rapidly expanding field, as judged by both the near capacity attendance and the number of additional posters on this subject at the meeting. Michael South opened the symposium with the comment that there were a large number of kinase enzymes now known. These show considerable homology at the ATP site, and it was thus originally expected that inhibitors targeting this site were unlikely to be selective. However, the discovery of potent and selective ATP site inhibitors has been a major step forward in the development of clinical agents.