氨基酸与肽。二十八。谷氨酰胺 - 缬氨酸 - 缬氨酸 - 丙氨酸 - 甘氨酸类似物的聚乙二醇杂化物的制备及其对木瓜蛋白酶的抑制作用。

Amino acids and peptides. XXVIII. Preparation of poly(ethylene glycol) hybrids of Gln-Val-Val-Ala-Gly analogs and their inhibitory effect on papain.

作者信息

Kawasaki K, Inoue S, Okada Y, Iguchi S, Okamoto H

机构信息

Faculty of Pharmaceutical Sciences, Kobe Gakuin University, Japan.

出版信息

Biol Pharm Bull. 1996 Jun;19(6):890-2. doi: 10.1248/bpb.19.890.

DOI:10.1248/bpb.19.890

PMID:8799495

Abstract

Gln-Val-Val-Ala-Gly is a sequence which is common in cysteine protease inhibitors. Poly(ethylene glycol) hybrids of Gln-Val-Val-Ala-Gly analogs were prepared by the solid phase method by fluorenylmethyloxycarbonyl chemistry. The hybrid formation of Gln-Val-Val-Ala-Gly resulted in improvement of the solubility and also in enhancement of the inhibitory effect of the peptide on papain. In addition, the hybrid formation of Gln-Val-Val-Ala-Gly analogs resulted in the enhancement of the inhibitory effect of the peptide analogs.

摘要

谷氨酰胺-缬氨酸-缬氨酸-丙氨酸-甘氨酸是半胱氨酸蛋白酶抑制剂中常见的序列。通过芴甲氧羰基化学的固相方法制备了谷氨酰胺-缬氨酸-缬氨酸-丙氨酸-甘氨酸类似物的聚乙二醇杂化物。谷氨酰胺-缬氨酸-缬氨酸-丙氨酸-甘氨酸的杂化形成提高了溶解度，同时增强了该肽对木瓜蛋白酶的抑制作用。此外，谷氨酰胺-缬氨酸-缬氨酸-丙氨酸-甘氨酸类似物的杂化形成增强了肽类似物的抑制作用。