Fruchtmann R, Kreisfeld K, Marowski C, Opitz W
Hoppe Seylers Z Physiol Chem. 1981 Feb;362(2):163-74.
The possibility of changing N-terminally protected tripeptides with chemotactic activity into antagonists by variation of the protecting group was investigated. Chemotactic activity in the agarose test was shown for a series of new structurally related formylated tripeptides. The effect could be antagonised with one exception by Boc-analogues. These antagonists are very likely bound to the same membrane receptor of polymorphonuclear leucocytes as the chemotaxins. The antagonists do not influence the activity of the naturally occurring chemotaxin C5a. The syntheses of the test compounds are described.
研究了通过改变保护基团将具有趋化活性的N端保护三肽转变为拮抗剂的可能性。在琼脂糖试验中显示了一系列新的结构相关的甲酰化三肽的趋化活性。除了一个例外,Boc类似物可以拮抗这种作用。这些拮抗剂很可能与趋化因子一样,与多形核白细胞的同一膜受体结合。拮抗剂不影响天然存在的趋化因子C5a的活性。描述了测试化合物的合成。