Next Article in Journal
Synthesis and Herbicidal Activity of Substituted Pyrazole Isothiocyanates
Next Article in Special Issue
Discovery and Validation of SIRT2 Inhibitors Based on Tenovin-6: Use of a 1H-NMR Method to Assess Deacetylase Activity
Previous Article in Journal
Synthesis and Characterization of New Thieno[3,2-b]thiophene Derivatives
Previous Article in Special Issue
Chemical Genetics — A Versatile Method to Combine Science and Higher Level Teaching in Molecular Genetics
Open AccessReview

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

1
Graduate Program in Cellular and Molecular Biology, University of Wisconsin, Madison, WI 53705, USA
2
Department of Medicine and UW Carbone Cancer Center, University of Wisconsin, Madison, WI 53705, USA
*
Author to whom correspondence should be addressed.
Molecules 2012, 17(10), 12172-12186; https://doi.org/10.3390/molecules171012172
Received: 17 September 2012 / Revised: 26 September 2012 / Accepted: 12 October 2012 / Published: 17 October 2012
(This article belongs to the Special Issue Chemical Genetics)
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. View Full-Text
Keywords: chemical biology; protein kinases; separation of function; mitosis; cell division chemical biology; protein kinases; separation of function; mitosis; cell division
Show Figures

Figure 1

MDPI and ACS Style

Lera, R.F.; Burkard, M.E. The Final Link: Tapping the Power of Chemical Genetics to Connect the Molecular and Biologic Functions of Mitotic Protein Kinases. Molecules 2012, 17, 12172-12186.

Show more citation formats Show less citations formats

Article Access Map by Country/Region

1
Only visits after 24 November 2015 are recorded.
Search more from Scilit
 
Search
Back to TopTop