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The Creoptix® WAVEsystem improves fragment-based screening and kinetic analysis of small molecules to accelerate drug development.
Binding kinetics on fibrils with label-free, surface-based sensors
In collaboration with Istituto Mario Negri, Milano
Alzheimer’s disease (AD) is the most common form of dementia in older people. This neurodegenerative
disorder is characterized by the deposit of toxic b-amyloid plaques (amyloid fibrils) in the brain. b-Amyloid
can interact with many intracellular and extracellular molecules, hence the importance of characterizing both
binding affinity and kinetics of these interactions. With high sensitivity and the fastest off-rate resolution, the
Creoptix WAVEsystem enables kinetic studies of weak binding THT (with off-rates of 10 s-1) onto amyloid fibrils.
Small Molecule Development
Real is crude
The Creoptix WAVEsystem provides a reliable environment for fragment-based drug discovery and small molecule screening, allowing for accurate off-rate kinetic analysis of crude reaction mixtures. With exquisite sensitivity, the ability to resolve extremely rapid dissociating kinetics, and innate compatibility with the high molecular weight ratios characteristic of most drug discovery programs, the Creoptix WAVEsystem improves fragment-based screening and kinetic analysis of small molecules to accelerate drug development.
Highly sensitive analysis at low immobilization levels, without mass transport limitation
In this TechNote we show the remarkable sensitivity of the WAVEsystem. Thanks to the expanded sensing field over which the Grating-Coupled Interferometry (GCI) technology measures, high-resolution kinetic determination at even very low responses is possible, potentially reducing material costs significantly.
Scientific Reports, 2020
H. Jankovics, B. Kovacs, A. Saftics, T. Gerecsei, E. Tóth, I. Szekacs, F. Vonderviszt, R. Horvath. “Grating-coupled interferometry reveals binding kinetics and affinities of Ni ions to genetically engineered protein layers.”
Highly accurate resolution of fast off-rates to significantly reduce false-positives
In this TechNote we show how the WAVEsystem can be used to accurately measure fast off-rate kinetics of weakly binding molecules. Thanks to a cartridge design that enables ultra-fast transition times of 150 ms, low potency hits can now be easily spotted for more successful drug discovery.
Sensitive kinetic analysis of small molecules binding to large drug targets
In this TechNote we show how the WAVEsystem can be used to accurately monitor binding kinetics of large target-to-analyte molecular weight (MW) ratios (>300:1), thanks to the expanded sensing field over which the Grating-Coupled Interferometry (GCI) technology measures for high sensitivity.
Spotting the weakest binders
Reliably determine off-rates of up to 10s-1, starting with just a crude reaction mixture. Work with a wide variety of solvents - including acetonitrile and high concentrations of DMSO - and minimize the occurrence of false positives.
Small molecules: binding kinetics no matter the size
- Screen, rank and characterize weak binders with off-rates up to 10 s-1.
- Study binding kinetics even at large analyte:ligand MW ratios (up to 1:1000).
- Experiment with crude mixtures, detergents and other additives without clogging.
W. Pitsawong, V. Buosi, R. Otten, R.V. Agafonov, A. Zorba, N. Kern, S. Kutter, G. Kern, R.A.P. Pádua, X. Meniche, D. Kern. "Dynamics of human protein kinase Aurora A linked to drug selectivity."