Protein Kinase Inhibitors for the Treatment of Inflammation - An Overview

Khusru      Asadullah; Matthias      Gaestel

Abstract

Protein kinases are key factors in signal transduction, playing a pivotal role in the initiation, propagation and regulation of immunologic responses. In contrast to protein- protein interaction they are considered to be “drugable” by small molecular weight inhibitors. Thus kinases moved into in the focus as promising drug targets for the therapy of inflammatory and autoimmune diseases. Whereas some kinase inhibitors are in clinical development already, most others are in early stages of research or still require validation. Recently, major progress has been made in elucidating the complete human kinome, in understanding molecular mechanisms of protein kinase action in inflammation as well as in regard to technologies suitable for in vitro and in vivo target validation, inhibitor screening and its structural refinement. Starting with some general points, this review summarise some recent findings and developments and prepare the stage for the subsequent review articles published in this hot topic issue. It is the purpose to highlight both the opportunities and the issues associated with kinases as drug targets and to enable the reader to keep up with this fast developing field, that is of substantial interest for basic and applied scientists.

Keywords: Drug targets, Inflammation, Immune regulation, Inhibitors, Kinases

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