Kharchenko E P, Samedov A Sh, Kalikhevich V N, Ardemasova Z A
Ukr Biokhim Zh (1978). 1990 Jul-Aug;62(4):21-6.
Screening of more than twenty short synthetic peptides characteristic of different proteins has revealed antimicrobial activity of the KRFAE peptide--from human preproenkephalin A against gram-negative bacteria. Modification of the peptide structure by means of administration of d-amino acids has permitted obtaining dKRFdLE analogue with the expressed and stable antimicrobial activity in vitro when growing bacteria on the minimum glucose-mineral medium. Changes and rearrangements of aminoacids in the dKRFdLE peptide in the second, third and fourth positions sharply decreased anti-microbial activity. The weaker antimicrobial activity as compared with that in dKRFdLE was peculiar to peptides with the other primary structure. Possible participation of peptides as antibiotics in the mechanisms of nonspecific immunity as well as the methods of their rational search are discussed.
对二十多种不同蛋白质特有的短合成肽进行筛选后发现，来自人前脑啡肽原A的KRFAE肽对革兰氏阴性菌具有抗菌活性。通过施用D-氨基酸对肽结构进行修饰，使得在以最低葡萄糖-矿物质培养基培养细菌时，能够获得具有体外表达且稳定抗菌活性的dKRFdLE类似物。dKRFdLE肽第二、第三和第四位氨基酸的变化和重排显著降低了其抗菌活性。与dKRFdLE相比，具有其他一级结构的肽抗菌活性较弱。讨论了肽作为抗生素可能参与非特异性免疫机制以及合理筛选它们的方法。
