Gerardy-Schahn R, Ambrosius D, Casaretto M, Grötzinger J, Saunders D, Wollmer A, Brandenburg D, Bitter-Suermann D
Institut für Medizinische Mikrobiologie, Universität Mainz, F.R.G.
Biochem J. 1988 Oct 1;255(1):209-16.
Based on published X-ray crystallographic data of the anaphylatoxic complement peptide C3a, we have synthesized a series of peptides with appropriate amino acid exchanges and a maximal length of 13 amino acids. N-terminal acylation of these optimized structures with epsilon-aminohexanoic acid and complex aromatic structures like fluorenylmethoxycarbonyl, 2-nitro-4-azidophenyl, fluoresceinyl and rhodaminyl leads to a dramatic increase in biological activity. The culmination of our synthetic efforts is a C3a analogue with 13 amino acid residues and a biological activity six times that of native C3a.
基于已发表的过敏毒素补体肽C3a的X射线晶体学数据，我们合成了一系列进行了适当氨基酸置换且最长为13个氨基酸的肽。用ε-氨基己酸以及芴甲氧羰基、2-硝基-4-叠氮基苯基、荧光素基和罗丹明基等复杂芳香结构对这些优化结构进行N端酰化，会使生物活性显著提高。我们合成工作的成果是一种具有13个氨基酸残基且生物活性为天然C3a六倍的C3a类似物。
