Kinase Drug Discovery: Modern Approaches
CHAPTER 13: A Structural Perspective of the Pseudokinome: Defining the Targetable Space
Published:31 Oct 2018
Pseudokinases share many of the common structural features of kinases but lack specific motifs that are required for catalytic activity. Although drug discovery efforts towards this family has been far more measured than that against traditional protein and lipid kinases, in recent years there has been increasing interest in pseudokinases as a potential target class. Such efforts may be able to exploit this structural overlap with kinases, whilst exploiting key differences to generate selectivity. This chapter summarises the recent developments in structural and biology understanding within this class of proteins and considers the future landscape. As the understanding of the biology of these fascinating proteins evolve it will also direct our understanding of how chemical approaches can be utilised as potential therapeutics.