使用S-三甲基乙酰氨基甲基半胱氨酸进行猪脑钠肽（pBNP）的溶液相合成。
Solution-phase synthesis of porcine brain natriuretic peptide (pBNP) using S-trimethylacetamidomethylcysteine.
作者信息
Kiso Y, Yoshida M, Kimura T, Fujiwara Y, Shimokura M, Akaji K
机构信息
Department of Medicinal Chemistry, Kyoto Pharmaceutical University, Japan.
出版信息
Chem Pharm Bull (Tokyo). 1990 May;38(5):1192-9. doi: 10.1248/cpb.38.1192.
The hexadodecapeptide corresponding to the entire amino acid sequence of porcine brain natriuretic peptide (pBNP) was synthesized by assembling four segments in solution, followed by HF deprotection and subsequent oxidation to establish an intramolecular disulfide bridge. The synthesis using the newly developed S-trimethylacetamidomethylcysteine [Cys(Tacm)] derivative gave a better yield than that using the S-2,4,6-trimethylbenzylcysteine [Cys(Tmb)] derivative. The chick rectum relaxant activity of the synthetic pBNP was 2.9 times more potent than that of alpha-rat atrial natriuretic peptide (alpha-rANP).
通过在溶液中组装四个片段合成了与猪脑利钠肽（pBNP）完整氨基酸序列相对应的十二肽，随后进行HF脱保护并随后氧化以形成分子内二硫键。使用新开发的S-三甲基乙酰氨基甲基半胱氨酸[Cys（Tacm）]衍生物进行的合成比使用S-2,4,6-三甲基苄基半胱氨酸[Cys（Tmb）]衍生物的合成产率更高。合成的pBNP对雏鸡直肠的舒张活性比α-大鼠心房利钠肽（α-rANP）强2.9倍。
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