Synthesis and properties of [A19-(p-fluorophenylalanine)] insulin |
| |
| Authors: | S Stoev S Zakhariev E Golovinsky H G Gattner V K Naithani A Wollmer D Brandenburg |
| |
| Institution: | Institute of Molecular Biology, Bulgarian Academy of Sciences, Sofia. |
| |
| Abstract: | The synthesis of Phe(F)A19]insulin (porcine) is described. First the protected Phe(F)19]A-chain was assembled by segment condensation of 1-12] and 13-21] using the dicyclohexyldiimide/1-hydroxybenzotriazole procedure. Phe(F)19]A-chain was purified by ion exchange chromatography after removal of all the protecting groups (Boc, But, OBut and S-Trt) and its conversion into the tetra-S-sulfonated derivative. Phe(F)A19]insulin was prepared by combination with porcine B-chain and purified by gel filtration and ion-exchange chromatography. The in vitro biological activity of this analogue was 60%. CD spectra in the near and far UV are qualitatively very similar to those of insulin. |
| |
| Keywords: | |
|
|
