Zamai M, Caiolfa V R
Research Laboratories, Farmitalia-Carlo Erba, Milano, Italy.
Biochim Biophys Acta. 1993 Oct 6;1202(2):337-40. doi: 10.1016/0167-4838(93)90025-m.
Sequence-directed recognition peptides (SDRPs) were constructed on the basis of their hydropathic complementarity for big-endothelin (bigET). These peptides can inhibit in vitro the proteolytic cleavage that generates endothelin (ET) from its bigET precursor. Comparison of dissociation constants of the complexes SDRP:bigET with kinetic constants obtained for the cleavage of bigET by alpha-chymotrypsin (taken as a model proteinase) provides evidence of the potential of SDRPs. This is a novel application of SDRPs used as inhibitors of a proteolytic reaction.
序列导向识别肽（SDRPs）是基于其与大内皮素（bigET）的亲水性互补性构建的。这些肽在体外可抑制从大内皮素前体产生内皮素（ET）的蛋白水解切割。将SDRP:bigET复合物的解离常数与通过α-胰凝乳蛋白酶（作为模型蛋白酶）切割bigET获得的动力学常数进行比较，为SDRPs的潜力提供了证据。这是SDRPs作为蛋白水解反应抑制剂的一种新应用。
