A new dimension to your kinase inhibitor screening

Are you interested in gaining valuable insights for your lead kinase inhibitor? Measuring kinase activity provides mechanistic insights into target interaction and the causes of different phenotypes in your disease model.

A new dimension to your kinase inhibitor screening

PamGene is operating on the cutting edge of next generation kinase science and high-tech to support scientists and companies in discovering, studying and optimizing kinase inhibitors. Measuring kinase activity provides mechanistic insights into target interaction and the causes of different phenotypes in your disease model.

Building on over 15 years of experience and a unique technology, we are able to go beyond recombinant kinase screening to provide you with a complete picture and better understanding of your compound’s:

Kinetic profile
Selectivity
Binding against 300+ kinases in a cellular context

Kinetic profile
Selectivity
Binding against 300+ kinases in a cellular context

“While quantitative measurements of transcripts and proteins are key to investigate the state of a biological system, they do not inform the “active” state of regulatory networks.” “Recent advancements of high-throughput protein kinase activity profiling platforms allow for a broad assessment of protein kinase networks in complex biological systems. In conjuncation with sophisticated computational modeling techniques, these profiling platforms provide datasets that inform the active state of regulatory systems in disease models and highlight potential drug targets.”

Learn more about this recently published review paper in ‘The current opinion in pharmacology’

Read further

Applications

Thanks to our unique and proven technology we will provide you with robust measurements, which can be applied in numerous of applications bringing your insights and research to the next level.

Compound screening
Compount off/on target investigation.
Compount toxicity
Compound re-positioning
Compound patient stratification

Our workflow

Intake meeting – with our scientists to define your research goals
Experimental design development – based on our extensive experience and fitted for your goals
Collecting samples – by the client following our easy-to-use sample preparation protocols
Process and analysis – using our unique and proven PamStation12 technique
Results meeting – data will be shared and discussed with you by our scientists

Applications

Thanks to our unique and proven technology we will provide you with robust measurements, which can be applied in numerous of applications bringing your insights and research to the next level.

Compound screening
Compount off/on target investigation.
Compount toxicity
Compound re-positioning
Compound patient stratification

Our workflow

Intake meeting – with our scientists to define your research goals
Experimental design development – based on our extensive experience and fitted for your goals
Collecting samples – by the client following our easy-to-use sample preparation protocols
Process and analysis – using our unique and proven PamStation12 technique
Results meeting – data will be shared and discussed with you by our scientists

Kinase inhibitor screening cases

We have over 15 years of experience in the field of kinase science and contributed to over 100+ publications with top European, North American and Japanese Institutes. For a selection visit the publications section.

To learn how our services contributed to different studies, request access to our whitepaper on two published cases we’ve worked on.

Case report

Kinase activity profiling cases we’ve worked on

To learn how our services contributed to different studies, request access to our whitepaper on two published cases we’ve worked on.

Case report

The benefits our Kinase Inhibitor Screening technology is bringing to your study

Kinase activity-based: Differentiate the primary and secondary effects of a kinase inhibitors.
Comprehensive: Broadly interrogate the full range of kinases (300+) and screen for selectivity and specificity of inhibitors across a wide range of conditions and concentrations
Distinctive: Distinguish primary and secondary effects of a kinase inhibitor for on/off target effects
Quantification: We bring the ability to quantify the inhibitory effect on the activity of fully decorated kinases

Technology

Kinases are the most intensively studied protein targets. We have developed a unique method to understand them. Our sensitive platform uses lysates obtained from only a few thousand cells or small amounts (2ug) of animal, xenografts or human tissues and cells to simultaneously determine the activity of all kinases present in these lysates.

This is accomplished by incubating the lysates across 196 to 144 tyrosine or serine/threonine kinase peptide substrates immobilized on the PamChip® microarray platform. Our 3D microarrays are spotted with peptides (i.e. phosphosites) that represent kinase targets. Kinases present in the lysates will phosphorylate the peptide substrates which are detected using fluorescently labelled antibodies. The phosphosites on the PamChips are human-derived and there is significant overlap with other organisms.

Based on current online knowledge, we compiled a comprehensive, integrated database (DB) of potential kinases that are linked to the peptides on the PamChips. This corresponds to ~350 unique kinases in literature, covering the majority of the kinome.