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杀卤菌素的单体类似物。

Monomeric analogues of halocidin.

作者信息

Doisy Xavier, Ifrah Dan, Hansen Paul R

机构信息

Chemistry Department, Royal Veterinary and Agricultural University, DK-1871, Frederiksberg C, Copenhagen, Denmark.

出版信息

Org Biomol Chem. 2004 Oct 7;2(19):2757-62. doi: 10.1039/B404826A. Epub 2004 Sep 2.

Abstract

Halocidin is a heterodimeric antimicrobial peptide isolated from a tunicate, Halocynthia aurantium. We used the most active of the two monomers, an 18 residue amidated peptide, as lead structure and determined the role of each amino acid with alanine scanning. The results obtained led to the synthesis of a first generation of analogues with antimicrobial activity. The selectivity towards bacterial versus mammalian cells has been explored, as well as the specificity for gram positive (Staphylococcus aureus ATCC 25923) versus gram negative bacteria (Escherichia coli ATCC 25922). GRAVY (grand average of hydropathicity) was used to analyze the results.

摘要

海兔毒素是从被囊动物海兔中分离出的一种异二聚体抗菌肽。我们使用了两种单体中活性最高的一种,即一种18个残基的酰胺化肽,作为先导结构,并通过丙氨酸扫描确定了每个氨基酸的作用。所得结果促成了第一代具有抗菌活性类似物的合成。研究了对细菌与哺乳动物细胞的选择性,以及对革兰氏阳性菌(金黄色葡萄球菌ATCC 25923)与革兰氏阴性菌(大肠杆菌ATCC 25922)的特异性。使用亲水性总平均值(GRAVY)来分析结果。

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