Benjamin Rotstein, Ph.D., and collaborators have demonstrated an operationally simple method for preparing carbon-isotope-labeled versions of pharmaceuticals and diagnostics.
New drug development relies on the ability of scientists to design sophisticated, specific drugs for targeted clinical trials. And isotopic labeling of new drug candidates in research labs is critical in this overall effort.
In a new study, Dr. Benjamin Rotstein’s lab at the uOttawa School of Medicine, in collaboration with colleagues, has revealed an operationally simple method for preparing carbon isotope-labeled versions of drugs and diagnostics.they developed a way to exchange single atom of amino acid—As for isotopes, they are the building blocks of proteins that are also used to prepare molecules.
“This is really important drug development Because we want to know where drugs go in the body and how they are metabolized and excreted, so we can plan appropriate dosing and toxicity studies.”
This work, natural chemistry.
Dr. Rotstein’s lab originally designed the experiment to act like the catalyst our bodies use. carboxylic acid Derived from an amino acid, it is the active form of vitamin B-6. However, when he wanted to run in the opposite direction, it turned out that the mechanism was slightly different from what he had originally expected.
“Actually adding carbon dioxideRemoves acid. So it’s another mechanism that allows us to look at better catalysts and extend the scope even further beyond amino acids,” he says.
The study was conducted in collaboration with colleagues at the University of Alberta and chemists at French pharmaceutical company Sanofi. Dr. Rotstein’s lab has studied carbon-11 and worked with these collaborators to elucidate the mechanism of the reaction. His lab uses carbon-11 because it is radioactive in a way that makes it suitable for medical imaging.
Dr. Rotstein and his team are now studying how reactions can produce only one ‘mirror-image’ version of an amino acid so that researchers don’t have to separate them after the fact.
He says he’s particularly excited about using carbon-11 amino acids to measure the rate at which our bodies make proteins, as this could be an indicator of disease.
Dr. Rotstein, who is also director of the Molecular Imaging Probes and Radiochemistry Laboratory at the University of Ottawa Heart Institute, said:
For more information:
Odey Bsharat et al, Aldehyde-catalyzed carboxylate exchange of α-amino acids with isotope-labeled CO2, natural chemistry (2022). DOI: 10.1038/s41557-022-01074-0
University of Ottawa
Quote: Study reveals new method of preparing contrast agents (22 November 2022), available on 22 November 2022 at https://phys.org/news/2022-11-reveals-method-imaging Taken from -agents.html
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