Pseudokinases: update on their functions and evaluation as new drug targets

This review, brought to MedChemNet users by Future Medicinal Chemistry, highlights how and why members of the 'pseudokinome' are important new drug targets.

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The pseudokinase complement of the human kinase superfamily consists of approximately 60 signaling proteins, which lacks one or more of the amino acids typically required to correctly align ATP and metal ions, and phosphorylate protein substrates. Recent studies in the pseudokinase field have begun to expose the biological relevance of pseudokinases, which are now thought to perform a diverse range of physiological roles and are connected to a multitude of human diseases, including cancer. In this review, we discuss how and why members of the ‘pseudokinome’ represent important new targets for drug discovery, and describe how knowledge of protein structure and function provides informative clues to help guide the rational chemical design or repurposing of inhibitors to target pseudokinases.

Keywords: cancercysteinecysteinomediseaseenzymeinhibitorkinasekinome
pseudoenzymepseudokinasesignaling


Byrne DP, Foulkes DM and Eyers PA. Pseudokinases: update on their functions and evaluation as new drug targetsFuture Med Chem (2017) doi: 10.4155/fmc-2016-0207

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Future Medicinal Chemistry

Journal, Future Science Group

Future Medicinal Chemistry provides a monthly point of access to commentary and debate for this ever-expanding and diversifying community. The journal showcases milestones in pharmaceutical R&D and features expert analysis of emerging research – from the identification of targets, through to the discovery, design, synthesis and evaluation of bioactive agents.

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