Real is Native
Study binding kinetics onto membrane proteins and retain their conformation and activity for more successful drug discovery
Membrane proteins are prime drug targets due to their essential role in regulating physiological processes. Familiar examples include G-protein coupled receptors (GPCR), histidine and tyrosine kinases, and cytokine receptors, in addition to a vast range of ion channels, enzymes, and transporters. With more than half of all currently validated drugs on the market targeting membrane proteins, the importance of this protein family to drug development is well established. However, membrane proteins are notoriously difficult to study, mainly because their hydrophobicity makes them extremely unstable following their extraction from the cell membrane.
Discover new membrane proteins as therapeutic targets
Understanding the interaction between a membrane protein and a small molecule drug or monoclonal antibody therapeutic is fundamental to drug development since it provides valuable insight regarding drug potency and efficacy. Yet to fully understand such liaisons, it is vital that the measurement of binding kinetics between these molecules is reliable. 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.
Detergents and other additives can compromise membrane protein integrity
The study of analyte-membrane protein interactions often involves the use of detergents, lipids and other additives to solubilize and purify the protein of interest. These non-native conditions have significant potential to alter the structure and conformation of the membrane protein, as well as impacting analyte-membrane protein binding kinetics, leading to inaccurate interpretation of data.
More than buffer
Explore a greater range of solubilization and purification conditions with our patented no-clog microfluidics, accommodating detergents, less common solvents, and multiple additives.
Study membrane protein pharmacology using only partially solubilized, unpurified material thanks to our no-clog microfluidics.
Virus-like particles, liposomes, and nanodiscs present unique challenges
To avoid the lengthy solubilization and purification processes required to study membrane proteins, researchers often choose to incorporate these biomolecules into a membrane-like environment. This is typically provided by virus-like particles (VLPs), liposomes, or nanodiscs, all of which function to preserve membrane protein integrity and activity. A limitation of this approach is that the resultant size of these structures, combined with a tendency to aggregate, can cause microfluidics channels to clog. Impeded flow may lead to experimental delays and can also increase instrument maintenance costs, however the Creoptix® WAVEsystem overcomes this issue by incorporating a unique, no-clog microfluidic design.
No clogging, regardless of size
Take advantage of the Creoptix WAVEsystem’s valveless microfluidics to analyze and characterize larger molecules.
Push the limits and generate high-quality binding kinetics with our sensitive GCI technology and resolve data at very low responses
Studying interactions within a membrane context provides greater insight
While some membrane proteins retain their analyte binding activity following solubilization and purification, this is not always the case. It is therefore important to study analyte-membrane protein binding within a membrane context to generate meaningful data. The Creoptix WAVEsystem allows researchers to investigate interactions between large binding partners and membrane proteins while maintaining the latter in their cell membrane environment. This provides essential insights to the binding of antibodies, nanobodies, or Sybody® candidates with the membrane protein of interest, and also allows investigation of membrane protein binding to intracellular signaling partners.
Wide range of affinities
Characterize large binding partners and resolve a wide range of affinities and off-rates with our stable GCI technology.
Close to native conditions
Immobilize membrane proteins from crude extracts with our no-clog microfluidic technology, without compromising the native state.