6PI3

NMR Solution structure of native tachyplesin III peptide

6PI3 の概要

• エントリーDOI: 10.2210/pdb6pi3/pdb
• NMR情報: BMRB: 30618
• 分子名称: Tachyplesin-3 (1 entity in total)
• 機能のキーワード: defense peptide, antimicrobial protein
• 由来する生物種: Tachypleus gigas (Southeast Asian horseshoe crab)
• タンパク質・核酸の鎖数: 1
• 化学式量合計: 2244.80

構造登録者

Harvey, P.J.,Troeira Henriques, S.,Vernen, F. (登録日: 2019-06-25, 公開日: 2019-09-11, 最終更新日: 2023-06-14)

主引用文献

Vernen, F.,Harvey, P.J.,Dias, S.A.,Veiga, A.S.,Huang, Y.H.,Craik, D.J.,Lawrence, N.,Troeira Henriques, S.
Characterization of Tachyplesin Peptides and Their Cyclized Analogues to Improve Antimicrobial and Anticancer Properties.
Int J Mol Sci, 20:-, 2019

PubMed Abstract: Tachyplesin I, II and III are host defense peptides from horseshoe crab species with antimicrobial and anticancer activities. They have an amphipathic β-hairpin structure, are highly positively-charged and differ by only one or two amino acid residues. In this study, we compared the structure and activity of the three tachyplesin peptides alongside their backbone cyclized analogues. We assessed the peptide structures using nuclear magnetic resonance (NMR) spectroscopy, then compared the activity against bacteria (both in the planktonic and biofilm forms) and a panel of cancerous cells. The importance of peptide-lipid interactions was examined using surface plasmon resonance and fluorescence spectroscopy methodologies. Our studies showed that tachyplesin peptides and their cyclic analogues were most potent against Gram-negative bacteria and melanoma cell lines, and showed a preference for binding to negatively-charged lipid membranes. Backbone cyclization did not improve potency, but improved peptide stability in human serum and reduced toxicity toward human red blood cells. Peptide-lipid binding affinity, orientation within the membrane, and ability to disrupt lipid bilayers differed between the cyclized peptide and the parent counterpart. We show that tachyplesin peptides and cyclized analogues have similarly potent antimicrobial and anticancer properties, but that backbone cyclization improves their stability and therapeutic potential.

PubMed: 31455019
DOI: 10.3390/ijms20174184

実験手法

SOLUTION NMR