New method to test drug-membrane interactions

The development of new small molecule drugs could be accelerated using a new technique that examines how they interact on the surface of a cell.

Using light microscopy, researchers were able to detect deformations at a resolution of less than a nanometer and quantify the membrane binding kinetics for both small and large molecules.

The majority of drugs are small molecules that interact with membrane proteins on the surface of cells. Understanding the kinetics of these interactions is critical for drug development but current methods are not optimal for testing small molecules. 

Researchers report in Science Advances (online, 23 October 2015)[1]
on a new method that harnesses the fact that molecular interactions with membrane proteins cause deformations in the cell membrane. Using light microscopy, the team were able to detect these deformations at a resolution of less than a nanometer and quantify the membrane binding kinetics for both small and large molecules. 

The researchers say the technique could help improve accuracy, and reduce the time and costs, of drug candidate screening.

References

[1] Guan Y, Shan X, Zhang F et al. Kinetics of small molecule interactions with membrane proteins in single cells measured with mechanical amplification. Science Advances 2015;1:e1500633. doi:10.1126/sciadv.1500633

Last updated
Citation
The Pharmaceutical Journal, New method to test drug-membrane interactions;Online:DOI:10.1211/PJ.2015.20069641

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