Explore all resources related to
The Creoptix® WAVEsystem enables more detailed investigation of membrane protein pharmacology, providing, for example, real-time drug binding affinities and label-free kinetics.
Real is native
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.
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.
Binding kinetics of a GPCR
Membrane proteins are notoriously difficult to study due to the requirement for a membrane-mimicking environment and their instability once extracted from a cellular membrane. Here we show the capability of the WAVE to measure the interaction of a peptide ligand agonist (NTA11) with a thermostabilized variant of the neurotensin receptor 1 (NTSR1) at highest resolution.
Binding kinetics onto membrane proteins
- Analyze multiprotein complexes and even larger particles like VLPs and crude membranes.
- WAVE goodbye to lengthy and laborious receptor purification procedures.
- Welcome contaminants and work with crude samples.
Keeping kinetics real
PEGS Europe 2019
Kinetic characterization of analytes binding to membrane proteins (GPCRs) embedded in virus-like particles (VLPs) and captured from crude cell membrane extracts (centrifugation-sonication).
Transforming drug discovery on membrane proteins
Under the Microscope - Drug Target Review
In November 2017, leadXpro chose to strengthen its capabilities with the Creoptix® WAVEsystem. “We were looking for a label‑free, biophysical method to investigate binding affinity and kinetics of small molecules with challenging integral membrane proteins,” explained Michael Hennig, Chief Executive Officer of leadXpro...