Why use single-molecule techniques for drug discovery?
Identification of the most potent drug candidates with single-molecule methods has enormous potential in the future of drug-discovery, offering major benefits over conventional assays used for screening. The ability of single-molecule tools to characterize new properties and specific transient steps in complex biochemical pathways, which are otherwise obscured in ensemble-average systems, allows you to look for inhibition of specific steps.
Given that most biochemical pathways usually consist of multiple steps, the total number of potential drug targets is considerably increased. Because of the C-Trap’s ability to directly visualize multi-step processes (even the most transient ones), it is extremely straightforward to observe at which step inhibition occurs and how it works. This, in turn, allows the development of more precise drugs while requiring significantly fewer secondary targets, and thus reducing the probability of side effects.
Common concerns such as long experimental time and high costs completely diminish when using the C-Trap. Bulk assays are often indirect methods of screening and require many experiments to reveal the molecular mechanism in question. Moreover, since only single molecules are required for the C-Trap experiments, the material consumption is several orders of magnitude lower. The intuitive software, the integrated microfluidics, and the automation capabilities guarantee an unprecedently quick workflow. The C-Trap gives access to novel information and ensures the precise screening of small molecules, quickly and effectively.
Visualization and characterization of small molecule-protein interactions.
In this example, optical tweezers are used to catch a DNA molecule tethered between two beads, while a motor protein and differently labeled small molecules are visualized by correlative fluorescence microscopy. The illustration shows how small molecules interact with the motor protein, thereby reducing or altering its activity. Alternatively, the small molecules can interact with the DNA template, resulting in barriers that restrict the movement of the proteins.
This is only one example of what can be investigated using this technology. Contact us to see how optical tweezers can benefit your research.