Medication to deal with most cancers are sometimes very costly to supply, leading to excessive prices for the sufferers who want them. Because of pathbreaking analysis by UCLA chemists, led by natural chemistry professor Ohyun Kwon, the worth of drug therapies for most cancers and different critical diseases might quickly plummet.
One chemical utilized in some anti-cancer medicine, for instance, prices pharmaceutical corporations $3,200 per gram — 50 occasions greater than a gram of gold. The UCLA researchers devised a reasonable strategy to produce this drug molecule from a chemical costing simply $3 per gram. They have been additionally in a position to apply the method to supply many different chemical compounds utilized in drugs and agriculture for a fraction of the standard value.
This feat, printed within the journal Science, includes a course of often called “aminodealkenylation.” Utilizing oxygen as a reagent and copper as a catalyst to interrupt the carbon-carbon bonds of many alternative natural molecules, the researchers changed these bonds with carbon-nitrogen bonds, changing the molecules into derivatives of ammonia referred to as amines.
As a result of amines work together strongly with molecules in dwelling crops and animals, they’re broadly utilized in prescribed drugs, in addition to in agricultural chemical compounds. Acquainted amines embody nicotine, cocaine, morphine and amphetamine, and neurotransmitters like dopamine. Fertilizers, herbicides and pesticides additionally comprise amines.
Industrial manufacturing of amines is subsequently of nice curiosity, however the uncooked supplies and reagents are sometimes costly, and the processes can require many sophisticated steps to finish. Utilizing fewer steps and no costly components, the method developed at UCLA can produce beneficial chemical compounds at a a lot decrease value than present strategies.
“This has by no means been completed earlier than,” Kwon stated. “Conventional metallic catalysis makes use of costly metals corresponding to platinum, silver, gold and palladium, and different valuable metals corresponding to rhodium, ruthenium and iridium. However we’re utilizing oxygen and copper, one of many world’s most considerable base metals.”
The brand new technique makes use of a type of oxygen referred to as ozone, a potent oxidant, to interrupt the carbon-carbon bond in hydrocarbons referred to as alkenes, and a copper catalyst to couple the damaged bond with nitrogen, turning the molecule into an amine. In a single instance, the researchers produced a c-Jun N-terminal kinase inhibitor — an anti-cancer drug — in simply three chemical steps, as an alternative of the 12 or 13 steps beforehand wanted. The associated fee per gram can thus be decreased from hundreds of {dollars} to just some {dollars}.
In one other instance, the protocol took only one step to transform adenosine — a neurotransmitter and DNA constructing block that prices lower than 10 cents per gram — into the amine N6-methyladenosine. The amine performs essential roles in controlling gene expression in mobile, developmental and illness processes, and its manufacturing value has beforehand been $103 per gram.
Kwon’s analysis group was in a position to modify hormones, pharmaceutical reagents, peptides and nucleosides into different helpful amines, displaying the brand new technique’s potential to change into an ordinary manufacturing method in drug manufacturing and lots of different industries.
The analysis was funded by the Nationwide Institutes of Well being.
