中文摘要：

哺乳动物的职业人员蛋白质 convertase 皮毛在被发现了在多样的生理、病理学的事件起一个重要作用，例如病毒的 glycoproteins 和细菌的外毒素的激活。小、无毒、高度活跃，在禁止者的皮毛被认为是病毒和细菌引起的疾病的吸引人的药候选人。在这研究，一系列肽禁止者基于 C 终端碎片被设计并且综合嘘一 H1.2，它在皮毛上有禁止的效果在里面。用皮毛的一致底层识别顺序代替禁止者的反应地点在被发现了极大地增加禁止的活动。大多数有势力禁止者，我有 14 氨基酸残余的 ₄, 有 K _{为皮毛的 17 nM 的 i} 价值在里面。尽管大多数综合的肽是暂时的禁止者，禁止者我有九氨基酸的 ₅, ，保留了它的完整的力量，甚至在有皮毛在的 3 h 潜伏期以后在 37 ° C。这些禁止者可以潜在地导致发展抗病毒并且抗菌剂药混合物。

英文摘要：

The mammalian proprotein convertase furin has been found to play an important role in diverse physiological and pathological events, such as the activation of viral glycoproteins and bacterial exotoxins. Small, non-toxic and highly active, furin inhibitors are considered to be attractive drug candidates for diseases caused by virus and bacteria. In this study, a series of peptide inhibitors were designed and synthesized based on the C-terminal fragment of histone H1.2, which has an inhibitory effect on furin. Replacing the reactive site of inhibitors with the consensus substrate recognition sequence of furin has been found to increase inhibitory activity greatly. The most potent inhibitor, I4, with 14 amino acid residues has a Ki value of 17 nM for furin. Although most of the synthesized peptides were temporary inhibitors, the inhibitor I5, with nine amino acids, retained its full potency, even after a 3 h incubation period with furin at 37℃ . These inhibitors may potentially lead to the development of anti-viral and antibacterial drug compounds.