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Drug discovery is a complex and multi-disciplinary field that aims to identify new therapeutic agents for the treatment of human diseases. This process starts with the identification of potential targets, followed by the screening of large libraries to find small molecules or biologics that interact with the target and show biological activity.
Hit-to-lead (HTL) is a critical stage in the drug discovery process, where a small number of compounds are selected from a large pool of hits, based on their activity and selectivity towards the target. One of the key challenges here is identifying high-value hits with a strong likelihood of success as a therapeutic.
However, the traditional approach of drug discovery often faces several challenges, such as high cost, time-consuming processes, limited success rates, and a lack of selectivity towards high-value drug candidates.
Label-free HTL technologies have emerged as a promising approach to address these challenges and improve the efficiency of drug discovery. Label-free approaches based on surface plasmon resonance (SPR) and bio-layer interferometry (BLI) allow efficient screening of large numbers of compounds, without the need for fluorescent labels or radiolabels. This not only reduces the overall complexity of screening, but also eliminates any potential artifacts that may arise from the labeling process. Furthermore, they offer several advantages over traditional methods, including higher sensitivity, better selectivity, and faster results.
High-throughput label-free technologies can significantly improve hit rates and increase the success of HTL programs. Researchers can screen large numbers of compounds, reducing the time and cost associated with traditional screening methods. Overall, this results in a larger pool of hits, from which high-quality leads can be selected. Additionally, label-free technologies provide full binding kinetics and valuable information about the mechanism of action of new leads, which are crucial for downstream steps, such as lead optimization and pre-clinical testing.
Both BLI and SPR are widely published with their own unique advantages, so the right choice depends on the application and the size range of molecules involved. SPR, for example, is a more sensitive technique for measuring interactions with small molecules and fragments. BLI on the other hand, is better suited for pharma-level high throughput analysis, with the added flexibility to perform assays in crude lysates during process optimization or bioprocess monitoring.
When used orthogonally, BLI and SPR are powerful, complementary tools for the characterization of biomolecules, such as antibodies, fragments or other biotherapeutic proteins in research and biopharma analysis workflows. Label-free approaches have been shown to significantly increase the hit rate in drug discovery, reduce time and costs, and provide valuable information about the properties and interactions of lead compounds with target molecules. As such, hit-to-lead label-free technologies have the potential to simplify the drug discovery process and lead to the development of new, effective, and more affordable drug treatments for patients resulting in better health for more people.