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一种用于裂解含叔戊酸的头孢菌素前药酯的新型酯酶。

A new esterase for the cleavage of pivalic acid-containing prodrug esters of cephalosporins.

作者信息

Sauber K, Aretz W, Meiwes J, Wollmann T

机构信息

Hoechst AG, Pharma Research, Frankfurt, Germany.

出版信息

Enzyme Microb Technol. 1996 Jul;19(1):15-9. doi: 10.1016/0141-0229(95)00171-9.

Abstract

An extracellular esterase from the actinomycetes Amycolatopsis orientalis was found by screening. It is capable of splitting the isomeric mixture (K/J) of (I, Scheme 1) into 7-amino-3-methoxymethyl-3-cephem-4-carboxylic acid, pivalic acid, and acetaldehyde with a high yield. The purified enzyme of 55.4 Kd by SDS-PAGE shows an N-terminal sequence of VRTCADLVRTYDLPGAVTH. The isoelectric point is 8.9 +/- 0.1. It can be immobilized with good yield to VA-Epoxy Biosynth. Besides the above-mentioned reaction, the esterase cleaves many other esters such as methyl-2-chloropropionic acid.

摘要

通过筛选发现了一种来自东方拟无枝酸菌的细胞外酯酶。它能够以高产率将(I,方案1)的异构体混合物(K/J)裂解为7-氨基-3-甲氧基甲基-3-头孢烯-4-羧酸、新戊酸和乙醛。经SDS-PAGE测定,纯化后的酶分子量为55.4 Kd,其N端序列为VRTCADLVRTYDLPGAVTH。等电点为8.9±0.1。它可以高产率地固定在VA-环氧生物合成载体上。除上述反应外,该酯酶还能裂解许多其他酯类,如2-氯丙酸甲酯。

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