9 research outputs found
Biomimetic Synthesis of Insulin Enabled by Oxime Ligation and Traceless “C-Peptide” Chemical Excision
For decades, insulin
has represented a preeminent synthetic target.
Recently introduced “biomimetic” strategies based on
convertible single-chain precursors require incorporation of a chemical
linker or a unique proteolytic site, which limits their practicality.
In this approach the A- and B-chains are linked by two sequential
oxime ligations followed by disulfide bond formation under redox conditions
and linker excision by diketopiperazine (DKP) formation and ester
hydrolysis, yielding native two-chain insulin. The method is expected
to be applicable to any member of the insulin superfamily