2MN1

Solution Structure of kalata B1[W23WW]

2MN1 の概要

• エントリーDOI: 10.2210/pdb2mn1/pdb
• NMR情報: BMRB: 19874
• 分子名称: kalata B1[W23WW] (1 entity in total)
• 機能のキーワード: cyclotide, unknown function
• 由来する生物種: Oldenlandia affinis
• タンパク質・核酸の鎖数: 1
• 化学式量合計: 3103.55

構造登録者

Henriques, S.T.,Huang, Y.H.,Chaousis, S.,Wang, C.K.,Craik, D.J. (登録日: 2014-03-26, 公開日: 2015-05-27, 最終更新日: 2024-11-20)

主引用文献

Henriques, S.T.,Huang, Y.H.,Chaousis, S.,Wang, C.K.,Craik, D.J.
Anticancer and toxic properties of cyclotides are dependent on phosphatidylethanolamine phospholipid targeting.
Chembiochem, 15:1956-1965, 2014

PubMed Abstract: Cyclotides, ultrastable disulfide-rich cyclic peptides, can be engineered to bind and inhibit specific cancer targets. In addition, some cyclotides are toxic to cancer cells, though not much is known about their mechanisms of action. Here we delineated the potential mode of action of cyclotides towards cancer cells. A novel set of analogues of kalata B1 (the prototypic cyclotide) and kalata B2 and cycloviolacin O2 were examined for their membrane-binding affinity and selectivity towards cancer cells. By using solution-state NMR, surface plasmon resonance, flow cytometry and bioassays we show that cyclotides are toxic against cancer and non-cancerous cells and their toxicity correlates with their ability to target and disrupt lipid bilayers that contain phosphatidylethanolamine phospholipids. Our results suggest that the potential of cyclotides as anticancer therapeutics might best be realised by combining their amenability to epitope engineering with their ability to bind cancer cell membranes.

PubMed: 25099014
DOI: 10.1002/cbic.201402144

実験手法

SOLUTION NMR