Overview for Target ID & Validation
Identifying and characterizing promising therapeutic targets as an intervention to disease is the first step in the drug discovery process. Recognizing the correct targets from the discovery process is critical through validation before investing further time and resources. Label-free binding technologies such as Bio-Layer Interferometry (BLI) and Surface Plasmon Resonance (SPR) systems are indispensable tools in both discovery and validation processes where high throughput binding screens can be quickly established to identify binding targets and accurately characterize for rates of complex formation (ka), complex stability (kd, dissociation) and affinities (KD).
Large molecules kinetics characterization
The BLI Octet® family of instruments accurately measures kinetic constants by bringing the detection surface directly to the sample, eliminating the need for microfluidics. This unique approach utilizing label-free, real-time analysis streamlines laboratory workflow and expedites assay development. It allows direct measurement of crude samples while minimizing instrument maintenance.
Protein - Small molecules and peptide kinetics & affinity characterization
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 ForteBio BLI Octet RED96e, Octet RED384 , HTX and Pioneer SPR platforms can be used to characterize small molecule and peptide systems.
Resources of Target ID & Validation
Application Note Generating Reliable Kinetic Data for Protein-Ligand Interactions
The Community Structure Activity Resource (CSAR, www.csardock. org) group is developing a database of high quality protein-ligand structures and the corresponding binding affinities. The data will be provided from in-house experiments and community collaborations. The proteins are generally well-studied structures that have been targeted in drug discovery projects.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 Fragment Based Drug Discovery on Pioneer Systems Using Next Generation SPR Analysis
Fragment-based drug design (FBDD) has become an increasingly popular platform for the identification of lead candidates in drug discovery programs.Read more
Application Note OneStep Lead Characterization of High Affinity Biologic Interactions with Pioneer SPR Systems
Biopharmaceutical drug discovery and development have celebrated the approval of breakthrough treatments in diseases of inflammation, cancer and infectious disease in recent years.Read more
Application Note Analysis of FcRn-Antibody Interactions on the Octet Platform
The Fc region of human IgG contributes to a number of beneficial biological and pharmacological characteristics of therapeutic antibodies.Read more
Application Note Kinetic Analysis of Antibody Binding to an Expressed Membrane Protein on Captured Lipoparticles
Membrane proteins govern the majority of input and output signals of cells and represent the largest class of pharmaceutical drug targets, making the analysis of their molecular interactions critical to mapping the interactome as well as drug discovery efforts.Read more