与水蛭素c相关的肽片段的合成及其对人白细胞弹性蛋白酶、组织蛋白酶G和α-糜蛋白酶抑制作用的研究
Synthesis of peptide fragments related to eglin c and examination of their inhibitory effect on human leukocyte elastase, cathepsin G and alpha-chymotrypsin.
作者信息
Okada Y, Tsuboi S, Tsuda Y, Nakabayashi K, Nagamatsu Y, Yamamoto J
机构信息
Faculty of Pharmaceutical Sciences, Kobe-Gakuin University, Japan.
出版信息
Biochem Biophys Res Commun. 1989 May 30;161(1):272-5. doi: 10.1016/0006-291x(89)91591-x.
Various kinds of peptide fragments related to eglin c were prepared by the conventional solution method and their inhibitory effects on human leukocyte elastase, cathepsin G and alpha-chymotrypsin were examined. Peptide (31-40) inhibited cathepsin G (Ki = 2.3 x 10(-4) M), peptide (41-49) potently inhibited cathepsin G and alpha-chymotrypsin (Ki = 4.2 x 10(-5) M and 2.0 x 10(-5) M, respectively), and peptide (60-63) inhibited leukocyte elastase (Ki = 1.6 x 10(-4) M), whereas, peptide (31-35) weakly inhibited both elastase and cathepsin G (Ki = 2.1 x 10(-3) M and 7.3 x 10(-4) M, respectively).
通过传统溶液法制备了各种与水蛭素c相关的肽片段，并检测了它们对人白细胞弹性蛋白酶、组织蛋白酶G和α-糜蛋白酶的抑制作用。肽（31-40）抑制组织蛋白酶G（Ki = 2.3×10⁻⁴ M），肽（41-49）有效抑制组织蛋白酶G和α-糜蛋白酶（Ki分别为4.2×10⁻⁵ M和2.0×10⁻⁵ M），肽（60-63）抑制白细胞弹性蛋白酶（Ki = 1.6×10⁻⁴ M），而肽（31-35）对弹性蛋白酶和组织蛋白酶G均有微弱抑制作用（Ki分别为2.1×10⁻³ M和7.3×10⁻⁴ M）。
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