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Synthesis and properties of [A19-(p-fluorophenylalanine)] insulin.

作者信息

Stoev S, Zakhariev S, Golovinsky E, Gattner H G, Naithani V K, Wollmer A, Brandenburg D

机构信息

Institute of Molecular Biology, Bulgarian Academy of Sciences, Sofia.

出版信息

Biol Chem Hoppe Seyler. 1988 Dec;369(12):1307-15. doi: 10.1515/bchm3.1988.369.2.1307.

DOI:10.1515/bchm3.1988.369.2.1307
PMID:3072012
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.

摘要

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