Biologics & Small Molecules Research
Biologics Research and Development
- Measure target binding affinity and kinetics of purified and non-purified biological molecules
- Rapidly perform DOEs to screen optimal assay conditions
The development of Biologics based drugs is an expensive and lengthy process. Early discovery requires researchers to select multiple lead candidates, confirm their mechanisms of action (MOA) against the target, and investigate optimal conditions for their production and functional activity before looking into their downstream critical quality attributes. The Octet® system provides unmatched ease-of-use and throughput capability in research and assay development for screening and characterization purposes.
Fc Receptor Binding Assays on the Octet® System
The selection of desired antibody-based therapeutics is often based on their binding properties, including binding to FcγRs. Antibodies are sometimes engineered to achieve desired FcγRs binding properties, as their binding can greatly impact their safety and efficacy to both the target and to FcγRs.
- Octet® systems offer a high-throughput and sensitive solution for Fc receptor binding analysis
- A variety of assay-ready biosensor surfaces are available and allow for flexibility and rapid optimization of assays
Small Molecule and Peptide Binding Kinetics
The discovery of small molecule and peptide lead molecules can stem from many sources including, fragment screening, high throughput screening and de novo structural design, amongst others. Determining and evaluating the affinity of small molecule binding to a therapeutic target is a significant component of the drug discovery process and lead optimization. The hit-to-lead and lead optimization processes are essential to accurately determine biological potency in vitro so that structure-activity relationships (SARs) can be used for efficient structural design. Learn how Octet® R Series of Systems, Octet® RH16, Octet® RH96 and Pioneer SPR platforms can be used to characterize small molecule and peptide binding.
High Throughput Phage Display Screening
Phage display is a technique to enable the study of protein, peptide, or DNA interactions with a target protein. This technology enables the discovery of high-affinity binders by using bacteriophages to present a target protein on the exterior of the viral coat, while containing the DNA encoding the target protein inside the viral coat. The resulting phages can be screened for binding against a library of peptides or proteins in a high throughput fashion.
Due to its high throughput design, the Octet® system is routinely used as a secondary screening platform for Fab fragments and non-antibody ligands derived from phage display libraries. An Octet® system screen can provide affinity ranking data and estimates of association and dissociation constants for primary hits.
Characterize Irreversible Inhibitors and Measure Commitment to Covalency
The majority of small molecule inhibitor assays tested with label-free, real-time biosensor technologies are reversible interactions, characterized by commonly used kinetic rate models. However, a significant fraction of therapeutic enzyme inhibitors on the market functions through covalent modification of the target.
The Pioneer FE system is a SPR platform that can be used with regenerable Streptavidin biosensors to reversibly capture protein targets and quantify the efficiency of covalent inhibitors binding to the target. The Pioneer FE system's irreversible inhibitor applications method can be used to determine inhibitor compound's commitment to covalency (Cc) as a metric for irreversible inhibitors.