Thermolysin-catalyzed synthesis of peptide amides.
作者:KIYOSHI SAKINA、KEIKO KAWAZURA、KAZUYUKI MORIHARA、HARUAKI YAJIMA
DOI:10.1248/cpb.36.4345
日期:——
Enzymatic condensation by thermolysin between various amino acid amides and Naprotected or unprotected peptides was examined.As models, three protected tetrapeptide amides, Boc-Trp-Met-Asp-X, Boc-Ser-Glu-Ala-X and Boc-Ser-Lys-Ala-X, and two unprotected tetrapeptide amides, H-Trp-Met-Asp-X and H-Phe-Met-Arg-X, were prepared [X=Phe-NH2, Leu-NH2, Phe-NHEt, Val-NH2, Ala-NH2, (p-fluoro) Phe-NH2], and the effects of various experimental conditions (pH, solvent and time) were examined.In addition, the C-terminal of oxidized insulin B-chain was elongated to an amide by addition of various amides mentioned above with the aid of thermolysin.
研究了热溶解酶在各种氨基酸酰胺和受保护或未受保护的肽之间的酶促缩合作用。作为模型,制备了三种受保护的四肽酰胺:Boc-Trp-Met-Asp-X、Boc-Ser-Glu-Ala-X 和 Boc-Ser-Lys-Ala-X,以及两种未受保护的四肽酰胺:H-Trp-Met-Asp-X 和 H-Phe-Met-Arg-X、X=Phe-NH2、Leu-NH2、Phe-NHEt、Val-NH2、Ala-NH2、(对氟)Phe-NH2],并考察了各种实验条件(pH 值、溶剂和时间)的影响。此外,在热溶解酶的帮助下,通过添加上述各种酰胺,将氧化胰岛素 B 链的 C 端拉长为酰胺。