6QXB

NMR structure of peptide 7, characterized by a cis-4-amino-Pro residue, with a significant lower MIC on E. coli

6QXB の概要

• エントリーDOI: 10.2210/pdb6qxb/pdb
• NMR情報: BMRB: 34366
• 分子名称: PHE-VAL-CAP-TRP-PHE-SER-LYS-PHE-LEU-GLY-ARG-ILE-LEU-NH2 (1 entity in total)
• 機能のキーワード: peptide antimicrobial, amps, temporins, proline derivatives, antibiotic
• 由来する生物種: Pseudis bolbodactyla
• タンパク質・核酸の鎖数: 1
• 化学式量合計: 1626.00

構造登録者

Brancaccio, D.,Carotenuto, A.,Merlino, F.,Grieco, P.,Novellino, E. (登録日: 2019-03-07, 公開日: 2019-05-29, 最終更新日: 2024-11-13)

主引用文献

Buommino, E.,Carotenuto, A.,Antignano, I.,Bellavita, R.,Casciaro, B.,Loffredo, M.R.,Merlino, F.,Novellino, E.,Mangoni, M.L.,Nocera, F.P.,Brancaccio, D.,Punzi, P.,Roversi, D.,Ingenito, R.,Bianchi, E.,Grieco, P.
The Outcomes of Decorated Prolines in the Discovery of Antimicrobial Peptides from Temporin-L.
Chemmedchem, 14:1283-1290, 2019

PubMed Abstract: Previously, we identified a potent antimicrobial analogue of temporin L (TL), [Pro ]TL, in which glutamine at position 3 was substituted with proline. In this study, a series of analogues in which position 3 is substituted with non-natural proline derivatives, was investigated for correlations between the conformational properties of the compounds and their antibacterial, cytotoxic, and hemolytic activities. Non-natural proline analogues with substituents at position 4 of the pyrrolidine ring were considered. Structure-activity relationship (SAR) studies of these analogues were performed by means of antimicrobial and cytotoxicity assays along with circular dichroism (CD) and NMR spectroscopic analyses for selected compounds. The most promising peptides were additionally evaluated for their activity against some representative veterinary microbial strains to compare with those from human strains. We identified novel analogues with interesting properties that make them attractive lead compounds.

PubMed: 31087626
DOI: 10.1002/cmdc.201900221

実験手法

SOLUTION NMR