Synthesis and disulfide structure determination of porcine endothelin: an endothelium-derived vasoconstricting peptide.
Synthesis and disulfide structure determination of porcine endothelin: an endothelium-derived vasoconstricting peptide.
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猪内皮素的合成和二硫键结构测定：内皮源性血管收缩肽。
DOI：
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发表时间：
2009
期刊：
影响因子：
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通讯作者：
S. Sakakibara
中科院分区：
文献类型：
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作者：
S. Kumagaye;H. Kuroda;K. Nakajima;Takushi X. Watanabe;Terutoshi Kimura;T. Masaki;S. Sakakibara
本文合成了猪或人内皮素的所有二硫键类似物（A、B和C型），并与天然内皮素的保留时间进行了比较。发现在位置1和15之间以及在位置3和11之间具有二硫键的类似物之一（A型）与天然内皮素相同。完全还原的内皮素的随机氧化以3：1的比例形成A型和B型的混合物，几乎没有C型，其在位置1和3之间以及11和15之间具有二硫键。应用我们的最大保护策略，还通过溶液中的片段缩合程序合成了A型内皮素。在大鼠肺动脉环制备物中发现该产品具有完全的血管收缩活性;效力与天然产物一样高。
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.