Applications in Protein Interactions

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"Quick Characterization of Binding onto Unpurified GPCRs"
 

In this TechNote, we show how the WAVEsystem can be used for the kinetic analysis of G-protein binding onto detergent-solubilized, unpurified GPCRs. By shortening a typical 10-step purification process, this method requires significantly less material (30mL of cell culture) and less time (less than 1 hour), thereby offering an alternative for screening purposes at an early stage of the drug discovery process involving membrane proteins.

   

FBDS & Small molecules 

Employing our proprietary Grating-Coupled Interferometry (GCI) technology to deliver superior sensitivity over traditional Surface Plasmon Resonance (SPR) technologies, the Creoptix™ WAVEsystem pushes the limits of what is possible to overcome mass-transport limitations. This is achievable within a broad range of immobilization levels, meaning that it is no longer necessary to saturate the surface with the drug target. With no-clog, robust microfluidics design, it is now possible to determine off-rates of up to 10s-1, starting with just a crude reaction mixture, making the WAVEsystem ideal for fragment-based screening.
 
  • Small molecule characterisation
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  • Fragment-Based Drug Discovery (FBDD)
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  • Spotting the weakest binders
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  • Low Signal Kinetics: going below Rmax 1
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  • Large Drug Targets
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Membrane Proteins 

With the sensitivity and versatility to measure analyte-membrane protein interactions in a wide variety of sample matrices, the Creoptix™ WAVEsystem enables more detailed investigation of membrane protein pharmacology, providing, for example, real-time drug binding affinities and label-free kinetics. Interactions between large binding partners and membrane proteins can now be studied while maintaining the latter in their cell membrane environment. This provides essential insights to the binding of antibodies, nanobodies, or sybodies with the membrane protein of interest (e.g., GPCRs, ion-channels), and also allows investigation of membrane protein binding to intracellular signaling partners.
 
  • Quick characterization of Binding onto unpurified GPCRs
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  • Kinetics of small molecules binding to solubilized GPCR
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Pharmacology & Biologics

The Creoptix™ WAVEsystem combines superior resolution in signal and time with a crude-sample robustness normally only possible with plate-based assays (ELISA). This provides dynamic, label free analysis of molecular interactions in a wide range of biofluids, providing full kinetic data that includes both affinity evaluation and highly accurate measurement of association and dissociation constants. Delivering a level of sensitivity superior to traditional Surface Plasmon Resonance (SPR) technologies, Creoptix™’ proprietary Grating-Coupled Interferometry (GCI) technology is driving a new era of pharmacokinetics.
 
 
  • Measurements in crude matrices
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  • Kinetics and affinity of antibodies in serum
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