Drug Discovery and Development: Protein - Small Molecule Interactions

The unique combination of quantitative structural and functional measurements provided by AnaLight® instruments allow the researcher to understand the conformational and other structural changes taking place in target proteins whilst they are interacting with small molecule candidates. The affinity and kinetics of interactions can be followed through measurement of mass changes with class-leading sensitivity to small mass binders. Additionally, the mass measured by AnaLight® is quantitative so can also reveal the stoichiometry of interactions. The structural changes taking place during these interactions can be measured simultaneously in terms of molecular dimensions and molecular fold density, showing dynamic conformational changes and differentiating between specific and non-specific binding events. Candidate compounds can be ranked not only by affinity, but also assessed in terms of the structural changes they instigate on binding to the target protein. AnaLight® provides the first real-time measurements for compound libraries to be screened for the structural relevance of their binding, potentially removing a significant bottleneck in drug discovery and development.

Application notes are available as PDF documents that can be either downloaded or viewed online:

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Measurement of Structural Change in Antitrypsin on Small Molecule Binding (206 Kb)
Measurement of Conformational Change in MAP Kinase on Small Molecule Binding (149 Kb)
Biotin - Streptavidin Interactions: Measuring Conformational Change and Differentiating between Specific and Non-Specific Binding (188 Kb)
The Molecular Basis of Action for an Inhibitor of ß-Amyloid Aggregation (73 Kb)
Dynamic Measurements of Small Molecule Partitioning into a C18 Membrane Mimic using Dual Polarisation Interferometry (79 Kb)
High Resolution Structural Studies of Isoform-Specific Apolipoprotein E Interactions with Tissue Plasminogen Activator (89 Kb)
Measurement of Conformational Change in P38a/SAPK2a Kinase on Specific Binding of Small Molecules (450 Kb)
Quantifying the Effects of Dimethyl Sulphoxide (DMSO) on Protein Structure using DPI, Real Time Studies of the Adsorption Behaviour of C12E4 Surfactant (90 Kb)