牛凝血酶原片段1，1-10片段。合成与免疫学研究。

Bovine prothrombin fragment 1, segment 1-10. Synthesis and immunological investigation.

作者信息

Ten Kortenaar P B, Wilkerson W W, Boggs N T, Madar D A, Koehler K A, Hiskey R G

出版信息

Int J Pept Protein Res. 1980 Nov;16(5):440-9. doi: 10.1111/j.1399-3011.1980.tb02968.x.

DOI:10.1111/j.1399-3011.1980.tb02968.x

Abstract

The N-terminal decapeptide methyl ester, H-Ala-Asn-Lys-Gly-Phe-Leu-Gla-Gla-Val-Arg-OCH3 (16) of bovine prothrombin fragment 1 has been prepared by standard solution techniques, via a fragment coupling strategy. Hexapeptide Boc-Ala-Asn-Lys epsilon (Boc)-Gly-Phe-Leu-OBzl (9) was obtained by coupling Boc-Ala-Asn-Lys epsilon (Boc)Gly-OH (6) to the trifluoroacetate salt of H-Phe-Leu-OBzl (8). Hydrogenolysis of (9) followed by coupling to HCl. H-Gla gamma (OtBu)2-Gla gamma (OtBu)2-Val-Arg(HCl)-OCH3 (14) gave the fully protected decapeptide (15). Treatment of 15 with 90% trifluoroacetic acid followed by ion exchange chromatography of 15 yielded the methyl ester (16). The decapeptide 16 labeled with 125I using the Bolton-Hunter reagent, did not bind to antibodies specific for the calcium ion-induced conformation of bovine fragment 1.

摘要

通过片段偶联策略，利用标准溶液技术制备了牛凝血酶原片段1的N端十肽甲酯，即H-Ala-Asn-Lys-Gly-Phe-Leu-Gla-Gla-Val-Arg-OCH3 (16)。六肽Boc-Ala-Asn-Lys ε(Boc)-Gly-Phe-Leu-OBzl (9)是通过将Boc-Ala-Asn-Lys ε(Boc)Gly-OH (6)与H-Phe-Leu-OBzl (8)的三氟乙酸盐偶联得到的。(9)进行氢解，然后与HCl偶联。H-Glaγ(OtBu)2-Glaγ(OtBu)2-Val-Arg(HCl)-OCH3 (14)反应得到完全保护的十肽(15)。用90%的三氟乙酸处理15，然后对15进行离子交换色谱，得到甲酯(16)。使用博尔顿-亨特试剂用125I标记的十肽16，不与针对钙离子诱导的牛片段1构象的抗体结合。