A new study carried out by the Swiss Federal Institute of Technology in Zurich (ETH) has facilitated an improved understanding among scientists as to how cyclic peptides are able to penetrate cell membranes. This is of interest due to the fact that these relatively large molecules are suitable to being used as potential drugs.
According to a press release issued by ETH Zurich, researchers are feverishly trying to find new active substances that can penetrate cell membranes. After all, only drugs of this kind can be administered orally, with all others needing to be injected directly into the blood. This is particularly urgent in the context of the declining efficacy of known antibiotics.
“The more we know about this mechanism and the properties a molecule must have, the earlier and more effectively researchers can take this into account when developing new drugs”, comments study leader Sereina Riniker, a professor in the Department of Chemistry and Applied Biosciences. With the help of computationally intensive computer modelling, she revealed how the molecule anchors itself onto the membrane surface and how it changes its three-dimensional shape on its way through the membrane, before re-assuming it when it exits on the other side. All of this helps drug researchers to improve the design of new active substances.
“Only modelling allows us such detailed, high-resolution insights, as there are no experiments that would let us observe an individual molecule crossing a membrane”, Riniker adds. The model peptides were developed by researchers from the pharma firm Novartis for basic research. As such, Riniker also collaborated with Novartis researchers as part of this study. mm
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