Light and peptides: New method diversifies natural building blocks of life

phys.org | 4/30/2018 | Staff
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Discovering new biological targets is a critical part of our ongoing battle against diseases. Over the years, scientists have made impressive progress towards the understanding of biological systems, constantly identifying novel targets. The structural diversity of these targets requires a broad range of different therapeutic agents.

"Small synthetic molecules are still key players, but biomolecules such as peptides, proteins and oligonucleotides have become an important area of research," says Professor Jérôme Waser, director of EPFL's Laboratory of Catalysis and Organic Synthesis. Peptides are particularly interesting, with about 140 evaluated in clinical trials in 2015. However, peptides often are not stable in the blood and cannot permeate cells well, both of which diminish their potential use as drugs.

Solution - Difficulties - Structure - Peptides - Process

One solution to overcome these difficulties is chemically modifying the natural structure of peptides, a process called "functionalization". In chemistry, a molecule is "functionalized" by adding chemical groups to it, thus endowing it with new functions, capabilities, or properties, such as enhanced stability in the human body. However, functionalization of peptides is difficult, due to their complex structure.

"The main reason is the lack of selectivity when you try to modify a peptide: it contains many positions that react with chemicals, resulting in useless mixtures," explains Waser. "Therefore, methods enabling selective functionalization of a single position in peptides are actively sought-after to access more efficient ant stable peptide-based drugs."

Waser - Lab - Reagents - Class - Compounds

This is what Waser's lab has now achieved, using "EBX reagents" – a class of very reactive organic compounds developed by the group and now commercially available. Using those reagents, the researchers converted the C-terminal carboxylic acid of peptides into a carbon-carbon triple bond – an alkyne (in chemical jargon a "decarboxylative...
(Excerpt) Read more at: phys.org
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