Infrared sensor can help scientists to analyze easily and quickly which active agents affect the protein structure and how long that effect lasts which may help develop new drugs with little side effects in a quick and targeted manner, according to a new study led by biophysicists at Ruhr-Universität Bochum (RUB). The findings of the study are published in the journal Angewandte Chemie. Prof Dr. Klaus Gerwert and Dr. Jörn Güldenhaupt performed time-resolved measurements of the changes to the structure of protein scaffolds, which were triggered by the active agents. Their methods might one day help develop drugs with little side effects in a quick and targeted manner. The team published a report on their research, which was conducted under the umbrella of the EU-funded programme Innovative Medicines Initiative in the project Kinetics for drug discovery (K4DD).
‘Using infrared sensor, Scientists can easily analyze which active agents affect the structure of proteins and how long that effect lasts which may help develop new drugs with little side effects in a quick and targeted manner.’
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Active Agents can Alter the Structure of Target ProteinsThe efficacy of many drugs is based on the fact that they manipulate the metabolism of cells by inhibiting the activity of specific proteins. To this end, the drug molecule must bind to the respective target protein, while the active agent more often than not settles in the functional compartments of proteins, which are often hollow like a pouch.
In the case of some active agents, binding to the target protein additionally alters the structure of the protein surface. Following the so-called conformational change, new surface areas and binding pouches become accessible, and an active agent can be further adapted to match them. This process often results in a better selectivity of active agents, thus reducing side effects.
New Method Facilitates Rapid Measurements
"The way an active agent affects the structure of its target protein has so far been analyzed using time-consuming and material-intensive methods, which may provide extremely detailed spatial information, but which don't yield results until weeks or even months later," explains Jörn Güldenhaupt.
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Example: Heat Shock Protein
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Binding Period Determines How often a Drug has to be Taken
The rate at which a drug molecule disengages from the target protein corresponds with the efficacy period of the drug in the body. Active agents with a high complex lifespan are bound to the target protein for a long time, thus remaining effective for a long time. Tablets containing such active agents have to be taken only once a day, for example, and often have fewer side effects. "Since our sensor acts as a flow system, we can rinse the active agents off the target protein after binding and, consequently, measure how the efficacy changes over time," explains Klaus Gerwert.
Source-Eurekalert