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The Final Link: Tapping the Power of Chemical Genetics to Connect the Molecular and Biologic Functions of Mitotic Protein Kinases
Journal article   Open access   Peer reviewed

The Final Link: Tapping the Power of Chemical Genetics to Connect the Molecular and Biologic Functions of Mitotic Protein Kinases

Robert F. Lera and Mark E. Burkard
Molecules (Basel, Switzerland), Vol.17(10), pp.12172-12186
10/17/2012
DOI: 10.3390/molecules171012172
PMCID: PMC3620603
PMID: 23075814
url
https://doi.org/10.3390/molecules171012172View
Published (Version of record) Open Access

Abstract

During mitosis, protein kinases coordinate cellular reorganization and chromosome segregation to ensure accurate distribution of genetic information into daughter cells. Multiple protein kinases contribute to mitotic regulation, modulating molecular signaling more rapidly than possible with gene expression. However, a comprehensive understanding of how kinases regulate mitotic progression remains elusive. The challenge arises from multiple functions and substrates, a large number of "bystander" phosphorylation events, and the brief window in which all mitotic events transpire. Analog-sensitive alleles of protein kinases are powerful chemical genetic tools for rapid and specific interrogation of kinase function. Moreover, combining these tools with advanced proteomics and substrate labeling has identified phosphorylation sites on numerous protein targets. Here, we review the chemical genetic tools available to study kinase function and identify substrates. We describe how chemical genetics can also be used to link kinase function with cognate phosphorylation events to provide mechanistic detail. This can be accomplished by dissecting subsets of kinase functions and chemical genetic complementation. We believe a complete "chemical genetic toolbox" will ultimately allow a comprehensive understanding of how protein kinases regulate mitosis.
Biochemistry & Molecular Biology Chemistry Chemistry, Multidisciplinary Life Sciences & Biomedicine Physical Sciences Science & Technology

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