A Structural Perspective of the Pseudokinome: Defining the Targetable Space

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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.

Original languageEnglish
Title of host publicationKinase Drug Discovery
Subtitle of host publicationModern Approaches
EditorsRichard A. Ward, Frederick W. Goldberg
Place of PublicationLondon UK
PublisherThe Royal Society of Chemistry
Number of pages22
ISBN (Electronic)9781788013093, 9781788015639
ISBN (Print)9781788010832
Publication statusPublished - 2019
Externally publishedYes

Publication series

NameDrug Discovery Series
PublisherRoyal Society of Chemistry
ISSN (Print)2041-3203
ISSN (Electronic)2041-3211

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