猪内皮素的合成及二硫键结构测定：一种内皮源性血管收缩肽
Synthesis and disulfide structure determination of porcine endothelin: an endothelium-derived vasoconstricting peptide.
作者信息
Kumagaye S, Kuroda H, Nakajima K, Watanabe T X, Kimura T, Masaki T, Sakakibara S
机构信息
Peptide Institute Inc., Protein Research Foundation, Osaka, Japan.
出版信息
Int J Pept Protein Res. 1988 Dec;32(6):519-26. doi: 10.1111/j.1399-3011.1988.tb01383.x.
All disulfide analogs (types A, B and C) of porcine or human endothelin, a 21-amino acid peptide having two intramolecular disulfide bonds, were synthesized and their retention times on HPLC were compared with that of natural endothelin. One of the analogs (type A) having disulfide bonds between positions 1 and 15 and between 3 and 11 was found to be identical with natural endothelin. Random oxidation of fully reduced endothelin formed a mixture of type A and B in a ratio of 3:1, with almost none of type C, which has disulfide bonds between positions 1 and 3 and between 11 and 15. Type A endothelin was also synthesized by the segment condensation procedure in solution applying our maximum protection strategy. This product was found to have full vasoconstricting activity in rat pulmonary artery ring preparations; the potency was as high as that of the natural product.
猪或人内皮素（一种具有两个分子内二硫键的21个氨基酸的肽）的所有二硫键类似物（A、B和C型）均已合成，并将它们在高效液相色谱（HPLC）上的保留时间与天然内皮素的保留时间进行了比较。发现其中一种在1位和15位以及3位和11位之间具有二硫键的类似物（A型）与天然内皮素相同。完全还原的内皮素的随机氧化形成了比例为3:1的A型和B型混合物，几乎没有具有在1位和3位以及11位和15位之间二硫键的C型。A型内皮素也通过应用我们的最大保护策略的溶液中的片段缩合程序合成。该产物在大鼠肺动脉环制剂中被发现具有完全的血管收缩活性；效力与天然产物一样高。
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