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聚-L-组氨酰-L-天冬氨酰-L-丝氨酰-甘氨酸的合成与催化活性

Synthesis and catalytic activity of poly-L-histidyl-L-aspartyl-L-seryl-glycine.

作者信息

Sarwal A N, Adigun E O, Stephani R A, Kapoor A

出版信息

J Pharm Sci. 1982 Dec;71(12):1380-3. doi: 10.1002/jps.2600711217.

DOI:10.1002/jps.2600711217
PMID:7153887
Abstract

Poly(His-Asp-Ser-Gly) was synthesized from the fully protected tetrapeptide active ester hydrochloride, which was prepared by stepwise coupling, using pentachlorophenyl ester and mixed anhydride methods. Complete deprotection of the protected tetrapeptide polymer was achieved by using 90% trifluoroacetic acid. The free polymer was dialyzed for 24 hr using a membrane (which retains molecules with molecular weights greater than 5000). The catalytic activity was determined by studying the hydrolysis of p-nitrophenyl acetate in 0.2 M phosphate buffer (pH 7.4) at 37 degrees. The catalytic coefficient of the dialyzed polymer was found to be 138 liters/mole/min.

摘要

聚(组氨酸-天冬氨酸-丝氨酸-甘氨酸)由完全保护的四肽活性酯盐酸盐合成,该四肽活性酯盐酸盐通过逐步偶联,采用五氯苯基酯法和混合酸酐法制备。使用90%的三氟乙酸对受保护的四肽聚合物进行完全脱保护。游离聚合物使用截留分子量大于5000的膜透析24小时。通过研究对硝基苯乙酸在0.2M磷酸盐缓冲液(pH 7.4)中37℃下的水解来测定催化活性。发现透析后的聚合物的催化系数为138升/摩尔/分钟。

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