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    • 81. 发明授权
    • Solid phase process for synthesizing peptides
    • 用于合成肽的固相方法
    • US4855407A
    • 1989-08-08
    • US849835
    • 1986-04-09
    • Su S. Wang
    • Su S. Wang
    • C07K1/04C07K1/08C07K1/113C07K7/23C07K14/00C07K14/575
    • C07K14/57581C07K1/04Y02P20/55Y10S930/18
    • Thymosin .alpha.1 and other peptide amides are synthesized in the solid phase using methylbenzhydrylamine resin as the support and hydrogen bromide as the deprotecting and cleaving agents. The N-terminal 14 amino acid partial sequence of thymosin .alpha.1, Ac-Ser-Asp-Ala-Ala-Val-Asp-Thr-Ser-Ser-Glu-Ile-Thr-Thr-Lys-OH is synthesized on benzyl ester resin. Using a mixture of hydrogen bromide, anisole and thioanisole as the cleavage and deprotection composition, the yields of the cleaved peptide and the selectivity of the deprotection is highly improved. For example, yields of thymosin .alpha.1 have been increased by about 90% as compared to the use of hydrogen bromide alone. By using hydrogen bromide rather than hydrogen fluoride, the synthesis can use conventional laboratory glassware and the synthesis can be easily scaled up to commercial production.
    • 使用甲基二苯甲基胺树脂作为载体和溴化氢作为脱保护和切割剂,在固相中合成了胸腺素α1和其他肽酰胺。 在苄酯上合成胸腺素α1,Ac-Ser-Asp-Ala-Ala-Val-Asp-Thr-Ser-Ser-Glu-Ile-Thr-Thr-Lys-OH的N-末端14个氨基酸部分序列 树脂。 使用溴化氢,苯甲醚和硫代苯甲醚的混合物作为切割和去保护组合物,裂解肽的产率和脱保护的选择性得到很大改善。 例如,与单独使用溴化氢相比,胸腺素α1的产量已增加约90%。 通过使用溴化氢而不是氟化氢,该合成可以使用常规的实验室玻璃器皿,并且可以将合成容易地扩大到商业生产。
    • 82. 发明授权
    • Prothymosin alpha
    • 孕激素α
    • US4659694A
    • 1987-04-21
    • US639757
    • 1984-08-13
    • Bernard L. Horecker
    • Bernard L. Horecker
    • A61K38/00C07K14/575C07K7/48C07K13/00
    • C07K14/57581A61K38/00Y10S930/18
    • A new biological polypeptide hormone has been isolated from mammalian thymus and has been given the designation prothymosin alpha. This peptide contains approximately 107 to 113 amino acid residues depending on species and is distinguished by having the thymosin alpha.sub.1 sequence at its amino-terminus. Prothymosin alpha appears to represent the native polypeptide from which thymosin alpha.sub.1, thymosin alpha.sub.11 and other fragments are generated during the isolation of thymosin fraction 5. Prothymosin alpha is one of several peptides isolated from thymic tissue which participate in the regulation, differentiation and function of thymic dependent lymphocytes (T cells). The new peptide appears to be more potent on a weight basis than thymosin alpha.sub.1 in the protection of subject animals against opportunistic infections.
    • 已经从哺乳动物胸腺中分离出一种新的生物多肽激素,并被赋予了称为胸腺素α。 该肽根据物种含有约107至113个氨基酸残基,其特征在于在其氨基末端具有胸腺素α1序列。 胸腺素α似乎代表在分离胸腺素级分5期间产生胸腺素α1,胸腺素α11和其他片段的天然多肽。胸腺素α是从参与胸腺调节,分化和功能的胸腺组织分离的几种肽之一 依赖淋巴细胞(T细胞)。 在保护受试动物免受机会性感染的情况下,新肽在重量方面似乎比胸腺素α1更有效。