How to spark a chemical chain reaction

March 9, 2018, Flinders University

Tailor-made protein drugs in the fight against cancer and other diseases are a step close, with the Centre for NanoScale Science and Technology at Flinders playing a part in one of the latest chemistry discoveries in effectively modifying therapeutic proteins.

Just published in the Journal of the American Chemical Society, a new paper titled "Chemo- and Regio-selective Lysine Modification on Native Proteins," describes a process which allows molecules, such as drugs, to be attached to antibodies and other proteins at precise locations.

"Most current methods for attaching drugs to proteins result in unwanted mixtures that can compromise function," says Flinders University Senior Lecturer in Synthetic Chemistry Dr. Justin Chalker, who is a collaborator on the research.

"In contrast, our is easy to do and highly precise," he says.

The international team of researchers, led by Gonçalo J. L. Bernardes from the University of Cambridge and the Institute of Molecular Medicine Lisbon and Gonzalo Jiménez-Osés of the University of Rioja in Spain, has discovered a sulfonyl acrylate reagent that should give researchers more options for modifying proteins.

The reagent selectively targets only the most reactive lysine in a protein, and not other lysines or buried cysteines.

Lysines are nucleophilic and much more abundant than cysteines, representing about 5.9% of the amino acids in human proteins, the paper says.

"Most excitingly, the chemistry can be applied directly to proteins in their native form," Dr. Chalker says.

"This means that off-the-shelf therapeutic antibodies can be modified directly, attaching drugs that the antibody directs to diseased tissue."

Explore further: Radical chemistry research makes waves

More information: Maria J. Matos et al. Chemo- and Regioselective Lysine Modification on Native Proteins, Journal of the American Chemical Society (2018). DOI: 10.1021/jacs.7b12874

Related Stories

Radical chemistry research makes waves

November 10, 2016

SA Young Tall Poppy of the Year, Flinders University's Dr Justin Chalker, has been part of an international research effort which opens the door to new drug development and a range of other applications in biochemistry.

The sugar-attaching enzyme that defines colon cancer

January 26, 2018

Researchers have identified an enzyme that is absent in healthy colon tissue but abundant in colon cancer cells, according to a report in the Jan. 26 issue of the Journal of Biological Chemistry. The enzyme appears to drive ...

Recommended for you

Seeing small-molecule interactions inside cells

December 12, 2018

Like people in a large company, proteins in cells constantly interact with each other to perform various jobs. To develop new disease therapies, researchers are trying to control these interactions with small-molecule drugs ...


Please sign in to add a comment. Registration is free, and takes less than a minute. Read more

Click here to reset your password.
Sign in to get notified via email when new comments are made.