大内皮素-1的C末端区域对磷酰胺敏感的内皮素转化酶进行特异性转化的重要性。

Importance of the C-terminal region of big endothelin-1 for specific conversion by phosphoramidon-sensitive endothelin converting enzyme.

作者信息

Okada K, Takada J, Arai Y, Matsuyama K, Yano M

机构信息

Central Research Laboratories, Banyu Pharmaceutical Co., Ltd., Tokyo, Japan.

出版信息

Biochem Biophys Res Commun. 1991 Oct 31;180(2):1019-23. doi: 10.1016/s0006-291x(05)81167-2.

DOI:10.1016/s0006-291x(05)81167-2

PMID:1953706

Abstract

Based on our previous findings that phosphoramidon-sensitive endothelin (ET) converting enzyme (ECE) converts human big ET-1 but does not big ET-3, we investigated structural requirement for substrate peptide. We prepared shorter peptides of big ET-1 and measured hydrolysis of the Trp-Val bond of these peptides. Relative hydrolysis ratios of big ET-1(1-38), (1-37), (16-37), (1-31) and (17-26) were 1, 1.15, 3.71, 0.01 and 0, respectively. In addition, big ET-2 and big ET-3 were not significantly converted by ECE. These results suggest that the carboxyl-terminal sequence at residues 32-37 of big ET-1 is important for conversion, whereas the amino-terminal disulfide loop structure appears to interfere with access of ECE to big ET-1.

摘要

基于我们之前的研究发现，即磷酰胺素敏感的内皮素（ET）转换酶（ECE）可转换人 big ET-1 但不能转换 big ET-3，我们研究了底物肽的结构要求。我们制备了 big ET-1 的较短肽段，并测量了这些肽段中 Trp-Val 键的水解情况。big ET-1(1-38)、(1-37)、(16-37)、(1-31) 和 (17-26) 的相对水解率分别为 1、1.15、3.71、0.01 和 0。此外，big ET-2 和 big ET-3 未被 ECE 显著转换。这些结果表明，big ET-1 第 32 - 37 位残基的羧基末端序列对于转换很重要，而氨基末端二硫键环结构似乎会干扰 ECE 接近 big ET-1。