Process for preparing esters of human insulin

Details Process for preparing esters of human insulin Process for preparing esters of human insulin

1981-02-10

1982-08-10

Rosen, Sam

Chemistry: molecular biology and microbiology

Micro-organism, tissue cell culture or enzyme using process...

Using a micro-organism to make a protein or polypeptide

435 70, C12P 2104

Patent

active

043438989

ABSTRACT:
A process for converting insulin compounds containing the human insulin moiety ##STR1## into h-In-Thr.sup.B30 esters through transpeptidation of such insulin compounds with a threonine ester in solution of water and a water miscible solvent in the presence of trypsin and optionally an acid.
Yields in excess of 60% are obtained by limiting water content to less than 50% v/v of the reaction mixture and controlling reaction temperature, with below ambient temperature and extended reaction times being preferred.
A preferred starting material is the crude porcine insulin recovered from insulin salt cake and contaminated by proinsulin and degradation products thereof which contaminants convert into the h-In-Thr.sup.B30 ester.

REFERENCES:
patent: 3276961 (1966-10-01), Bodanszky et al.
Morihara et al.-Nature, vol. 280, Aug. 1979, pp. 412 & 413.
Inouye et al.-J.A.C.S., vol. 101, Jan. 1979, pp. 751 & 752.
Morihara-Hakka to Kogyo (Fermentation and Industry), vol. 38, No. 11 (1980), pp. 1052-1055.

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