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Effect of Acylation on the Antimicrobial Activity of Temporin B Analogues
ChemMedChem ( IF 3.4 ) Pub Date : 2018-07-06 , DOI: 10.1002/cmdc.201800289
Concetta Avitabile 1 , Luca Domenico D'Andrea 1 , Elisabetta D'Aversa 2 , Roberta Milani 2 , Roberto Gambari 2 , Alessandra Romanelli 3
Affiliation  

New peptides derived from the natural antimicrobial temporin B were obtained. The design, antimicrobial activity, and characterization of the secondary structure of peptides in the presence of bacterial cells is described herein. TB_KKG6K (KKLLPIVKNLLKSLL) has been identified as the most active analogue against Gram‐positive and ‐negative bacteria, compared with natural temporin B (LLPIVGNLLKSLL) and TB_KKG6A (KKLLPIVANLLKSLL). Acylation with hydrophobic moieties generally led to reduced activity; however, acylation at the 6‐position of TB_KKG6K led to retained sub‐micromolar activity against Staphylococcus epidermidis.

中文翻译:

酰化对Temporin B类似物抗菌活性的影响

获得了衍生自天然抗微生物temporin B的新肽。本文描述了在细菌细胞存在下肽的二级结构的设计,抗微生物活性和表征。与天然temporin B(LLPIVGNLLKSLL)和TB_KKG6A(KKLLPIVANLLKSLL)相比,TB_KKG6K(KKLLPIVKNLLKSLL)被确定为对革兰氏阳性和阴性细菌活性最高的类似物。与疏水性部分酰化通常导致活性降低;然而,在TB_KKG6K的6位酰化导致保留了对表皮葡萄球菌的亚微摩尔活性。
更新日期:2018-07-06
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