Biophysical methods for the detection and quantification of binding between small molecules or biologicals and their target are fundamental to chemical biology and pharmacological research. Target engagement assays can be utilized for target deconvolution and validation, establishing structure-activity relationships, probe discovery, and understanding the mode of action of prospective therapeutics.
Different biophysical methods such as isothermal titration calorimetry, differential scanning fluorimetry, surface plasmon resonance, biolayer interferometry and microscale thermophoresis have been established to measure target-ligand interactions using purified target molecules. Despite their various advantages each method also has different limitations, including high material consumption, sensitivity limits, low throughput or impacted performance when working with complex matrices or crude material. Moreover, the binding observed between a ligand and a target in a cell-free system does not always translate to a similar interaction within the intracellular environment. Therefore, new techniques have emerged in recent years to quantify the binding of small molecules and biologicals to targets within living cells.
The goal of the current Research Topic is to introduce novel approaches to monitor and measure target engagement, and present new technological and methodological advances to break through the limitations of established methods in cell free and living systems.
The scope of this Research Topic is to cover the application of well established, recent, and novel biophysical target engagement technologies in chemical biology and pharmacological research. We welcome all available article types, including original research articles, brief research reports, and reviews covering, but not limited to:
• Target engagement in cells
• Cell free assays
• Target deconvolution
• Mode of action studies
• Labelled chemical probes
Biophysical methods for the detection and quantification of binding between small molecules or biologicals and their target are fundamental to chemical biology and pharmacological research. Target engagement assays can be utilized for target deconvolution and validation, establishing structure-activity relationships, probe discovery, and understanding the mode of action of prospective therapeutics.
Different biophysical methods such as isothermal titration calorimetry, differential scanning fluorimetry, surface plasmon resonance, biolayer interferometry and microscale thermophoresis have been established to measure target-ligand interactions using purified target molecules. Despite their various advantages each method also has different limitations, including high material consumption, sensitivity limits, low throughput or impacted performance when working with complex matrices or crude material. Moreover, the binding observed between a ligand and a target in a cell-free system does not always translate to a similar interaction within the intracellular environment. Therefore, new techniques have emerged in recent years to quantify the binding of small molecules and biologicals to targets within living cells.
The goal of the current Research Topic is to introduce novel approaches to monitor and measure target engagement, and present new technological and methodological advances to break through the limitations of established methods in cell free and living systems.
The scope of this Research Topic is to cover the application of well established, recent, and novel biophysical target engagement technologies in chemical biology and pharmacological research. We welcome all available article types, including original research articles, brief research reports, and reviews covering, but not limited to:
• Target engagement in cells
• Cell free assays
• Target deconvolution
• Mode of action studies
• Labelled chemical probes
