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Surface Plasmon Resonance for Identifying and Characterising Small Molecule Ligands

From the book “Biophysical Techniques in Drug Discovery”, Chapter 7, Pages 170 – 207

Editor: Angeles Canales

S. J. Pollack

Abstract

Surface plasmon resonance (SPR) is a powerful technology that allows an information-rich assessment of the interactions of tethered protein molecular targets with their interacting ligands in real time. As such, SPR has proven useful at all stages of drug discovery, from initial hit finding (particularly the screening of fragment libraries) to mechanistic kinetic and thermodynamic profiling during hit validation and lead optimisation phases. Each of these stages of drug discovery involves somewhat different considerations in the optimal design and interpretation of SPR experiments. These factors will be discussed along with other relevant applications of SPR technology for drug discovery, such as in DMPK and toxicology assessments. Finally, the future developments in SPR for drug discovery will be considered.

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