Ufkes J G, Visser B J, Heuver G, Wynne H J, Van der Meer C
Eur J Pharmacol. 1982 Apr 8;79(1-2):155-8. doi: 10.1016/0014-2999(82)90590-8.
Several pentapeptides were synthesized and tested for bradykinin-potentiating activity. From these and previous data it appeared that an (L)-aromatic amino acid residue (preferably Trp) in position 3 is essential for high activity. Position 3 represents a stereospecific pillar function, whereas the other positions and the lipophilicity/hydrophilicity balance are important for additional activity. So far, BPP5a seems to have the optimal structure for a bradykinin-potentiating pentapeptide.
合成了几种五肽并测试其缓激肽增强活性。从这些以及之前的数据来看，第3位的（L）-芳香族氨基酸残基（最好是色氨酸）对于高活性至关重要。第3位代表一种立体特异性的支柱功能，而其他位置以及亲脂性/亲水性平衡对于额外的活性很重要。到目前为止，BPP5a似乎具有作为缓激肽增强五肽的最佳结构。
