A comparison of protein kinases inhibitor screening methods using both enzymatic activity and binding affinity determination.

PubWeight™: 0.78‹?›

🔗 View Article (PMC 4051630)

Published in PLoS One on June 10, 2014

Authors

Amalie Frederikke Rudolf1, Tine Skovgaard1, Stefan Knapp2, Lars Juhl Jensen1, Jens Berthelsen3

Author Affiliations

1: Novo Nordisk Foundation Center for Protein Research, Faculty of Health Sciences, University of Copenhagen, Copenhagen, Denmark.
2: Structural Genomics Consortium, Nuffield Department of Clinical Medicine, University of Oxford, Oxford, United Kingdom.
3: Novo Nordisk Foundation Center for Protein Research, Faculty of Health Sciences, University of Copenhagen, Copenhagen, Denmark; Costerton Biofilm Center, Institute for International Health, Immunology and Microbiology, Faculty of Health Sciences, University of Copenhagen, Copenhagen, Denmark.

Articles cited by this

The protein kinase complement of the human genome. Science (2002) 35.36

A quantitative analysis of kinase inhibitor selectivity. Nat Biotechnol (2008) 14.74

A small molecule-kinase interaction map for clinical kinase inhibitors. Nat Biotechnol (2005) 12.22

The use of differential scanning fluorimetry to detect ligand interactions that promote protein stability. Nat Protoc (2007) 9.92

Comprehensive analysis of kinase inhibitor selectivity. Nat Biotechnol (2011) 5.65

Comprehensive assay of kinase catalytic activity reveals features of kinase inhibitor selectivity. Nat Biotechnol (2011) 3.72

A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. Proc Natl Acad Sci U S A (2007) 3.21

Structural coupling of SH2-kinase domains links Fes and Abl substrate recognition and kinase activation. Cell (2008) 2.46

High-throughput kinase profiling as a platform for drug discovery. Nat Rev Drug Discov (2008) 2.12

Navigating the kinome. Nat Chem Biol (2011) 1.88

The evolution of protein kinase inhibitors from antagonists to agonists of cellular signaling. Annu Rev Biochem (2011) 1.80

Assessment of chemical coverage of kinome space and its implications for kinase drug discovery. J Med Chem (2008) 1.74

Protein kinase inhibitors: contributions from structure to clinical compounds. Q Rev Biophys (2009) 1.72

SH2 domains: modulators of nonreceptor tyrosine kinase activity. Curr Opin Struct Biol (2009) 1.45

Kinase inhibitor selectivity profiling using differential scanning fluorimetry. Methods Mol Biol (2012) 1.35

A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. Biochem J (2013) 1.31

Targeting cancer with small-molecular-weight kinase inhibitors. Methods Mol Biol (2012) 1.29

Measuring and interpreting the selectivity of protein kinase inhibitors. J Chem Biol (2009) 1.24

Trends in kinase selectivity: insights for target class-focused library screening. J Med Chem (2010) 1.18

Therapeutic protein kinase inhibitors. Cell Mol Life Sci (2009) 1.16

The challenge of selecting protein kinase assays for lead discovery optimization. Expert Opin Drug Discov (2008) 1.16

Enzyme assay design for high-throughput screening. Methods Mol Biol (2009) 0.98

High-throughput biochemical kinase selectivity assays: panel development and screening applications. J Biomol Screen (2008) 0.93

Interrogating the kinome. Nat Biotechnol (2011) 0.86

What general conclusions can we draw from kinase profiling data sets? Biochim Biophys Acta (2013) 0.83

High-throughput screening of the cyclic AMP-dependent protein kinase (PKA) using the caliper microfluidic platform. Methods Mol Biol (2009) 0.79

Articles by these authors

KinomeXplorer: an integrated platform for kinome biology studies. Nat Methods (2014) 1.12