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Truncated or folded helix peptides or peptide analogs showing antibacterial activity against Gram-negative bacteria and uses thereof
Truncated or folded helix peptides or peptide analogs showing antibacterial activity against Gram-negative bacteria and uses thereof
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机译:显示出对革兰氏阴性细菌具有抗菌活性的截短或折叠的螺旋肽或肽类似物及其用途
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摘要
PROBLEM TO BE SOLVED: To provide a cleaved or folded helix peptide or peptide analog, an antibacterial composition containing them, a conjugate to which a drug is linked thereto, or an antibiotic containing the same. SOLUTION: An α-helix double-sided peptide composed of a hydrophobic amino acid and a hydrophilic amino acid is a gram-negative bacterial membrane-permeable peptide or a peptide analog having a folded structure, and i) the α-helix double-sided peptide. Some of the hydrophobic amino acids of the above have a folded α-helix structure substituted with one or more selected from the group consisting of proline, aspartic acid, asparagine, glutamic acid, glutamine, its D-type amino acids, and derivatives thereof. Or ii) An α-helix structure in which at least two or more amino acids constituting the α-helix double-sided peptide are linked and folded at one or more positions by a disulfide bond, a carbon-carbon bond, a maleimide bond, or an amide bond. Has. [Selection diagram] Fig. 1
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