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Protein Kinase Selectivity Profiling Using Microfluid Mobility Shift Assays.

Peter Drueckes1

  • 1CPC Screening Sciences, Novartis Pharma AG, Novartis Institutes for Biomedical Research, 4002, Basel, Switzerland. peter.drueckes@novartis.com.

Methods in Molecular Biology (Clifton, N.J.)
|June 19, 2016
PubMed
Summary
This summary is machine-generated.

Biochemical profiling identifies drug side effects early in development. This study details a microfluidic mobility shift assay workflow for efficient protein kinase selectivity testing.

Keywords:
Compound preparationKinaseMicrofluidic mobility shift assaySelectivity profiling

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Area of Science:

  • Drug Discovery and Development
  • Biochemistry
  • Molecular Biology

Background:

  • Biochemical selectivity profiling is crucial for early-stage drug development.
  • Testing compounds for off-target activities is a standard practice.
  • Protein kinases are a major target family in drug discovery.

Purpose of the Study:

  • To present a workflow for biochemical protein kinase profiling.
  • To highlight critical aspects of this profiling method.
  • To demonstrate the utility of microfluidic mobility shift assays.

Main Methods:

  • Utilized microfluidic mobility shift assays for biochemical profiling.
  • Developed a workflow for assessing compound selectivity across protein kinases.
  • Focused on compounds from the optimization phase of drug development.

Main Results:

  • Established a robust workflow for biochemical protein kinase profiling.
  • Demonstrated the effectiveness of microfluidic mobility shift assays for selectivity testing.
  • Identified key considerations for successful implementation of the assay.

Conclusions:

  • Microfluidic mobility shift assays provide an efficient method for protein kinase profiling.
  • The presented workflow aids in identifying potential off-target activities early in drug development.
  • This approach supports the optimization of drug candidates by assessing selectivity.