Synthesis of peptides related to corticotropin (ACTH). IX. Application of N-hydroxy-5-norbornene-2,3-dicarboximide active ester procedure to the synthesis of human adrenocorticotropic hormone (.ALPHA.h-ACTH).
作者:OSAMU NISHIMURA、CHITOSHI HATANAKA、MASAHIKO FUJINO
DOI:10.1248/cpb.23.1212
日期:——
Human adrenocorticotropic hormone (αh-ACTH), H-Ser-Tyr-Ser-Met-Glu-His-Phe-Arg-Trp-Gly-Lys-Pro-Val-Gly-Lys-Lys-Arg-Arg-Pro-Val-Lys-Val-Tyr-Pro-Asn-Gly-Ala-Glu-Asp-Glu-Ser-Ala-Glu-Ala-Phe-Pro-Leu-Glu-Phe-OH, was synthesized by using N-hydroxy-5-norbornene-2, 3-dicarboximide (HONB) with N, N'-dicyelohexylcarbodiimide (DCC) for the stepwise elongation and fragment condensation. The synthetic αh-ACTH, purified on a column of carboxymethylcellulose, Amberlite XAD-2 resin and Bio-Gel P-6, was found to be homogeneous by various criteria and exhibits full biological activity (ca. 145 units/mg) in in vitro steroidogenic assay.
人促肾上腺皮质激素 (αh-ACTH),H-Ser-Tyr-Ser-Met-Glu-His-Phe-Arg-Trp-Gly-Lys-Pro-Val-Gly-Lys-Lys-Arg-Arg-Pro-Val -Lys-Val-Tyr-Pro-Asn-Gly-Ala-Glu-Asp-Glu-Ser-Ala-Glu-Ala-Phe-Pro-Leu-Glu-Phe-OH,使用N-羟基-5合成-降冰片烯-2, 3-二甲酰亚胺 (HONB) 与 N,N'-二环己基碳二亚胺 (DCC) 进行逐步延伸和片段缩合。合成的 αh-ACTH 在羧甲基纤维素、Amberlite XAD-2 树脂和 Bio-Gel P-6 柱上纯化,根据各种标准发现是均质的,并且在体外表现出完整的生物活性(约 145 单位/毫克)类固醇生成测定。