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Products and Contract Services

General Assay Development & Kinase Assay Development

Caliper Discovery Alliances & Services (CDAS) has assay development programs directed toward serving the science needs of our clients using the most appropriate detection methods for a given molecular target and screening objective. CDAS develops on average more than 100 new assays per year for its clients and its screening service business. Our broad instrumentation platforms also allow more flexibility to perform your assays here at CDAS on an exclusive, outsourced basis. Our core capabilities including experience in compound profiling and high throughput screening provide an expansive range of assay technologies to serve your assay development efforts. These programs focus on several major areas of interest.


General Assay Development


Protein-Ligand Interactions
Common targets for these types of assays include both GPCRs and other membrane bound receptors, nuclear receptors, DNA-transcription factors and  siRNA. Standard platforms include Radioligand Binding, Time Resolved Fluorescence (TRF), Fluorescence Polarization (FP), Fluorescence Resonance Energy Transfer (FRET), Alpha Screen, Luminescence/Absorbance, Scintillation Proximity Assays (SPA)* and Scintillating Microplates

Enzyme
A wide range of enzyme assays can be developed using either endogenous cellular enzymes or recombinant ones. The assays can be developed to simply measure compound inhibition or changes in kinetics or expression levels. Technologies employed for these types of assays include Caliper’s Microfluidic Platform, Radioactive and Fluorescent Label Substrate Microplate Conversion Measurements, HPLC and LC-MS.

Ion Channels
Both channel binding sites and ion fluxes can be tracked in custom in vitro systems to measure compound interactions with ion channels. Approaches range from an assessment of ligand interacts with these sites to actual ion flows using fluorescent dyes, radioactive ions, flame photometry and automated whole cell patch clamping.

Cellular Responses
Functional readouts from cellular responsive elements can be measured in a variety of formats including signal transduction through customized transfected reporter genes in a cell. These assays can be developed to provide High Content information using multiple readouts from a single screening. Cell readouts can typically determined with second messenger reporter systems, transport across membranes, ELISAs, RT PCR, Protein Arrays, and whole cell responses such as migration and proliferation.

Functional cellular response is a complex multi-step biological process that can be measured utilizing several techniques. Here at CDAS we are utilizing the latest, state of the art assay platforms such as Luminex, flowcytometry, planar protein and gene expression arrays, high throughput Western blotting, multiplex qRT-PCR and many others. Through successful implementation of these methods we are offering complete custom build solutions to measure cellular responses at each step of the cell activation cascade, such as:

  • - Intracellular protein phosphorylation
  • - Transcription factor activation (DNA binding activity and reporter assays)
  • - Gene expression, (qRT-PCR and gene expression arrays)
  • - Protein expression (including cytokines, chemokines and growth factors)
Each of these readouts can be evaluated individually or can be incorporated into multi parameter assay system thus increasing throughput and informational content of each assay run.

Toxicology
Compound effects on the function and viability of a wide array of tumor and primary human and rodent cell lines can be measured with a series of custom assays to measure the integrity of cells. These can range from multiple endpoints for cell viability to functional readouts from any set of chosen biomarkers.

Kinase Assay Development

Kinases are one of the most important classes of enyzmes and are involved in signal transduction and signaling networks within cells. These kinase signaling pathways play a fundamental role in regulating cell proliferation, cell metabolism and cell death. Research shows that changes in protein kinase activity within a cell can lead to several disease states, most notably cancer. With this knowledge base, scientists have been investigating the ability of drugs to block various protein kinases as a cancer therapy. This approach has proved successful with the discovery of several kinase inhibitor drugs for the treatment of various cancers such as Gleevec®, Iressa® and Tarceva®. In addition to their involvement in cancer, protein kinases are implicated in diabetes, inflammation and neurological development and degeneration.

Because protein kinases are involved in a wide variety of disease states, over 30% of all spending for drug development focuses on this area of research. Through the use of the Caliper’s LabChip® microfluidic platform, we can develop specialized kinase assays to assist you in accelerating and optimizing your lead identification efforts in this area.

Advantages of Kinase Assay Development using microfluidics

  • - Enzymology studies available with real time kinetics
  • - Direct measurement of both phosphorylated & unphosphorylated peptide
  • - Improved data quality and precision when compared to traditional methods
  • - High signal-to-noise ratio
  • - Identification of weak enzyme inhibitors
  • - Increased Z’ values (range of 0.8 - 0.9)
  • - Non-radioactive, antibody free format
  • - High throughput screening format