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Review Article

Structure-based discovery of cyclin-dependent protein kinase inhibitors

Mathew P. Martin, Jane A. Endicott, Martin E.M. Noble
Essays In Biochemistry Nov 08, 2017, 61(5) 439-452; DOI: 10.1042/EBC20170040
Mathew P. Martin
Newcastle Cancer Centre, Northern Institute for Cancer Research, Paul O’Gorman Building, Medical School, Newcastle University, Framlington Place, Newcastle upon Tyne NE2 4HH, U.K.
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Jane A. Endicott
Newcastle Cancer Centre, Northern Institute for Cancer Research, Paul O’Gorman Building, Medical School, Newcastle University, Framlington Place, Newcastle upon Tyne NE2 4HH, U.K.
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Martin E.M. Noble
Newcastle Cancer Centre, Northern Institute for Cancer Research, Paul O’Gorman Building, Medical School, Newcastle University, Framlington Place, Newcastle upon Tyne NE2 4HH, U.K.
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  • For correspondence: martin.noble@ncl.ac.uk
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November 2017

Volume: 61 Issue: 5

Essays In Biochemistry: 61 (5)
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Structure-based discovery of cyclin-dependent protein kinase inhibitors
Mathew P. Martin, Jane A. Endicott, Martin E.M. Noble
Essays In Biochemistry Nov 2017, 61 (5) 439-452; DOI: 10.1042/EBC20170040
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Structure-based discovery of cyclin-dependent protein kinase inhibitors
Mathew P. Martin, Jane A. Endicott, Martin E.M. Noble
Essays In Biochemistry Nov 2017, 61 (5) 439-452; DOI: 10.1042/EBC20170040

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  • Article
    • Abstract
    • Introduction
    • CDK active and inactive states
    • The CDK ATP binding site
    • The selectivity surface
    • CDK4/6 lend themselves to selective inhibition and show clear disease linkage
    • The C-terminal tail
    • Targeting the monomeric enzyme
    • Conclusions
    • Summary
    • Funding
    • Competing Interests
    • Author Contribution
    • References
  • Figures
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Keywords

CDK
cell cycle
kinase
Structure-based drug design

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