Caliper measures up kinase profiling
The new “RapidKinase” profiling and enzymatic “Mechanism of Action” services launched by Caliper’s Discovery Alliance and Services (CDAS) division, aim to provide pharmaceutical firms a way of screening drug candidates against a range of kinase targets and reap the organisational and cost benefits of outsourcing.
For those wishing to keep their kinase profiling programmes in-house, the company has also launched a series of more than 200 kinase assays for use with its LabChip EZ Reader platform.
There are over 500 human protein kinases, all of which are of interest as possible drug targets as they play a key role in regulating cell signalling pathways. The large number of possible targets often makes kinase profiling too expensive to conduct in house.
This has led to many contract research organisations (CROs) offering kinase profiling services and the new services from CDAS will compete against offerings from Millipore, BioFocus DPI, SignalChem and ProQinase to name just a few.
The high level of interest in offering kinase assays and services is not surprising as the kinase inhibitor market has been predicted by Pharmaprojects to reach $58.6bn by 2010, with drugs targeting indications in cancer, diabetes, arthritis and Alzheimer’s.
The RapidKinase profiling service uses Caliper’s LabChip EZ Reader technology and ProfilerPro reagents to provide kinase profiling data to researchers within one week.
The more detailed Mechanism of Action studies provide researchers with information about how their compounds interact with targets, the characterisation of allosteric inhibitors and the assessment of kinetic on-off rates.
Allosteric inhibitors interact with enzymes at locations other than the active site and are less likely to be covered by existing patents. Compounds with slower ‘off rates’ take longer to disassociate than those with faster ‘off rates’, allowing lower doses to be used for treatments which decreases the risk of side effects.
“The availability of these new services from CDAS reflects Caliper’s deep understanding of the scientific, clinical, and commercial advantage of rapid kinase profiling and mechanism-of-action studies,” said Dr David Manyak, executive vice president, Discovery Services, Caliper Life Sciences.
“For many therapeutic treatment groups within pharmaceutical and biotech companies, outsourcing labour-intensive screening is the best option. Through CDAS, our customers have access to Caliper’s proprietary LabChip platforms. As both a platform and service provider, Caliper remains committed to continually enhancing our offerings to facilitate the drug discovery process.”
The new assay kits enable researchers using Caliper’s LabChip EZ Reader platform to profile the activity of drug candidates against more than 200 kinases in a single day.
Each of the ProfilerPro Kinase Selectivity Assay Kits contain all the reagents and control needed for rapid profiling up to 12 different compounds against 24 protein kinases.
The reagents are pre-dispensed into reaction-ready 384 well microtiter plates to simplify laboratory workflow and accelerate time to results.
“Caliper’s unique same-day kinase profiling platform enables researchers to make better compounds by providing chemists faster access to more information about potential off target liabilities,” said Rick Bunch, business unit manager, LabChip Systems, Caliper Life Sciences.
“The combination of high quality data generated by LabChip microfluidic assays with workflow improvements inherent to ProfilerPro reagents means that overall drug discovery programs can be accelerated, enabling companies to bring drugs to market faster.”
