Label Free Tools for Drug Discovery
Surface Plasmon Resonance (SPR) is a versatile technique for the label-free reporter free studies of bio-molecular interactions. Artifacts and interferences commonly observed in fluorescence-based assays are avoided.
NovAliX’ SPR instruments are highly sensitive. Both commercial and proprietary systems are available with complementary advantages in throughput, format, workflow and information delivered. The high level features of these formats are as follows:
Commercial channel-based Biacore™ systems
- Medium throughput ligand screening
- Hit confirmation
- Characterization of compound/protein binding
- Detailed analysis protein/ligand Interactions
Proprietary NovAliX chemical microarray SPR
- Higher throughput primary screening
- Fragment based drug discovery
- Affinity ligands for bio-separation (downstream processing)
- A technology platform for molecular recognition
In each format, one of the potential binding partners is immobilized on a sensor surface whist the other is in solution. Binding of the soluble analyte to the immobilized partner induces a change in refractive index close to the surface that can be read by SPR. The sensor surfaces are gold coated which permits functionalization in conventional systems this enables the coupling of the protein of interest to the sensor while in the microarray format thousands of small molecules are immobilized on a single chip.
SPR assays support many applications in research, development and manufacturing. NovAliX has considerable experience in the use of SPR for drug discovery and bio-separation. Measurements include binding affinity, binding kinetics and selectivity. Modern instruments are even sensitive enough to detect weak binding of low molecular weight analytes, a prerequisite for fragment based drug discovery.
NovAliX uses commercial channel-based GE BiacoreTM instruments but the array-based systems are exclusively designed & produced for in-house use. This combination creates more opportunities to address challenging issues.
T. Neumann et al. SPR Screening of Chemical Microarrays for Fragment-Based Discovery, in Label-Free Technologies for Drug Discovery, Ed. L Mayr, Wiley, 2011
A. HeimRiether, et.al. Improving potency and selectivity of a new class of non-Zn-chelating MMP-13 inhibitors , Bioorganic & Medicinal Chemistry Letters, 2009, 19(18), 5321-5324
T.Neumann et al. SPR Based Fragment Screening: Advantages and Applications, Current Topics in Medicinal Chemistry, 2007, 7, 1630-1642
T. Neumann, et al. Discovery of Thrombin Fragments from Chemical Microarray Screening, Letters in Drug Design & Discovery, 2005, 2, 563-566