Overview for Biologics & Small Molecules Research
The discovery of lead candidates during Biologics drug molecules development can be an expensive and lengthy process. The early discovery process of these molecules require researchers to select multiple candidates, confirm their mechanisms of action (MOA) against target, and investigate optimal conditions for their production and activity before looking into their downstream critical quality attributes. The lifecycle of the drug product involves target molecule identification and validation, optimal cell line development, and process development before a molecule can be deemed fit for clinical testing and manufacturing. Among label-free molecular interactions platforms, the Octet system provides researchers with unmatched ease-of-use and throughput capability in research and assay development for screening and characterization purposes. The Pioneer FE SPR instrument expands capabilities in small molecules and protein interaction studies.
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. ForteBio's Pioneer FE 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.
ELISA conversion on the Octet system
ELISA has been a common practice in the biology research laboratory since the 1970's. Despite its widespread adoption, its variability in results, susceptibility to human error, labor-intensive workflow, and slow time-to-result remain as big hurdles for users looking to adopt ELISA in high throughput applications. Faster times-to-results, better consistency, and less human intervention are the prerequisites for next generation of high throughput laboratory operation.
- Transfer your ELISA assay onto the Octet system for real-time analysis
- Increase precision over manual ELISA in direct quantitation assays
- Amplify response signals in multistep quantitation assay to increase quantitation sensitivity
High throughput phage display screening
Phage display is a technique to enable the study of protein, peptide or DNA interaction with a target protein. This molecular tool 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 displaying 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. Using immobilized antigen, an Octet system screen can provide affinity ranking data and estimates of association and dissociation constants for each primary hit.
Virus and vaccine R&D on the Octet system
Small molecule and peptide therapeutic drugs are highly sought after in most areas of disease research due to their desirable pharmacological properties and low propensity for immunogenicity. In small molecule drug discovery, the path to lead molecules can stem from many sources or starting points including fragment screening, high throughput screening, de novo structural design, etc. The determination and evaluation of 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 process are essential to accurately determine biological potency in vitro so that structure-activity relationships (SAR) can be used for efficient structural design. Learn how Octet RED96e, Octet RED384, Octet HTX and Pioneer SPR platforms can be used to characterize small molecule and peptide systems.
- High throughput and rapid potency testing
- Quantitate or perform rapid virus affinity characterization
- Develop stability indicating methods
- Study and test intact virus samples
Resources of Biologics & Small Molecules Research
Application Note A Fast and High Precision Influenza Vaccine Potency Assay
Mall molecule and peptide therapeutic drugs are highly sought after in most areas of disease research due to their desirable pharmacological properties and low propensity for immunogenicity. In small molecule drug discovery, the path to lead molecules can stem from many sources or starting points including fragment screening, high throughput screening, de novo structural design, etc. The determination and evaluation of the affinity of small molecule binding to a therapeutic target is a significant component of the drug discovery process and lead optimization.Read more
Application Note Commitment to Covalency : Kinetics of Irreversible Inhibitors on the Pioneer FE System
The principal role of assay groups in drug discovery is to provide reliable methods, analysis, and data for confident decision-making about series progression. Particular assays are chosen to differentiate between affinity, specificity, cellular action, and most important mechanism of action.Read more
Application Note Octet Potency Assay: Development, Qualification and Validation Strategies
In this application note, we discuss the strategies for the development and validation of a potency assay using Octet® systems. We have highlighted the Octet system’s ease-ofuse and fast time to results by showcasing strategies for the development and validation of a method for evaluating the binding of an Fc gamma receptor III molecule to the widely characterized NISTmAb.Read more
Brochure Octet Systems
Your research should be guided by your imagination, not by the limitations of your label-free system. The Octet® platform’s flexible, open-format design and comprehensive menu of biosensors lets you attack research challenges in unique new ways. Perform truly comprehensive structure/function studies with large panels of structural variants.Read more
Technical Guide High Precision Streptavidin Biosensor (SAX) Quantitation and Kinetic Assays
Streptavidin-coated surfaces are widely used as a simple and straightforward method of molecular immobilization. Utilized with Bio-Layer Interferometry (BLI), Streptavidin biosensors enable quick and easy modification and customization of the biosensor with any biotintagged molecule for quantitative and kinetic measurements.Read more