Synthesis of human pancreatic growth hormone-releasing factor and two omission analogs by segment-coupling method in aqueous solution.
Synthesis of human pancreatic growth hormone-releasing factor and two omission analogs by segment-coupling method in aqueous solution.
复制标题
水溶液中分段偶联法合成人胰腺生长激素释放因子和两种省略类似物。
DOI：
10.1111/j.1399-3011.1984.tb03150.x
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发表时间：
1984
期刊：
影响因子：
--
通讯作者：
Li,CH
中科院分区：
文献类型：
--
作者：
Blake,J;Westphal,M;Li,CH
采用固相法合成了人生长激素释放因子多肽[GlyS15]-GRF-(1-15)(IV)、三氟乙酰-GRF-(20-44)(VI)、三氟乙酰-GRF-(18-44)()和三氟乙酰-GRF-(16-44)(X)。每一种多肽都与柠檬酸酐反应，然后在水中与10%的联氨反应除去三氟乙酰基。通过与硝酸银/N-羟基丁二酰亚胺反应，将柠檬酰化的GRF-(1-15)肽与(20-44)、(18-44)或(16-44)肽偶联，分别得到GRF-(1-15)-(20-44)(XII)、GRF-(1-15)-(18-44)(XIII)或GRF-(1-44)。GRF-(1-44)能刺激大鼠垂体细胞释放生长激素，其ED50=8.8倍10-11M。多肽XII和XIII既不是GRF-(1-44)的激动剂，也是GRF-(44)的拮抗剂。
The human growth hormone‐releasing factor (GRF) peptides [GlyS15]‐GRF‐(1–15) (IV), trifluoroacetyl‐GRF‐(20–44) (VI), trifluoroacetyl‐GRF‐(18–44) (VIII), and trifluoroacetyl‐GRF‐(16–44) (X) were synthesized by the solid‐phase method. Each of the peptides was reacted with citraconic anhydride and the trifluoroacetyl group was removed by reaction with 10% hydrazine in water. The citraconylated GRF‐(1–15) peptide was coupled to the (20–44), (18–44) or (16–44) peptides by reaction with silver nitrate/N‐hydroxysuccinimide to give GRF‐(1–15)‐(20–44) (XII), GRF‐(1–15)‐(18–44) (XIII), or GRF‐(1–44), respectively. GRF‐(1–44) was shown to stimulate the release of rat growth hormone from rat pituitary cells with an ED50= 8.8 times 10‐11M. Peptides XII and XIII were inactive, either as agonists or as antagonists of the action of GRF‐(1–44).