2M3N

Peptide leucine arginine

2M3N の概要

• エントリーDOI: 10.2210/pdb2m3n/pdb
• 関連するPDBエントリー: 1GM2 1JBL
• NMR情報: BMRB: 18970
• 分子名称: Peptide leucine arginine (1 entity in total)
• 機能のキーワード: bowman birk inhibitor, hydrolase inhibitor
• 由来する生物種: Rana pipiens (Northern leopard frog)
• 細胞内の位置: Secreted: Q90WP7
• タンパク質・核酸の鎖数: 1
• 化学式量合計: 2141.60

構造登録者

Polte, T. (登録日: 2013-01-23, 公開日: 2013-09-11, 最終更新日: 2024-10-30)

主引用文献

Rothemund, S.,Sonnichsen, F.D.,Polte, T.
Therapeutic potential of the Peptide leucine arginine as a new nonplant bowman-birk-like serine protease inhibitor.
J.Med.Chem., 56:6732-6744, 2013

PubMed Abstract: The peptide leucine arginine (pLR) belongs to a new class of cyclic peptides isolated from frog skin. Its primary sequence is similar to the reactive loop of plant Bowman-Birk inhibitors (BBI), and the recently discovered circular sunflower trypsin inhibitor-1 (SFTI-1). The conformational properties of pLR in solution were determined by NMR spectroscopy and revealed excellent structural similarity to BBI and SFTI-1. Moreover, pLR is a highly potent trypsin inhibitor, with Ki values in the nanomolar range, and, due to its small size, a potential inhibitor of the serine protease tryptase. Since tryptase plays a crucial role in the development of allergic airway inflammation, the therapeutic potential of pLR in a murine asthma model was investigated. Treatment of ovalbumin-sensitized mice with pLR during allergen challenge reduced the acute asthma phenotype. Most importantly, application even at the end of a long-lasting chronic asthma model decreased the development of chronic airway inflammation and tissue remodeling.

PubMed: 23988198
DOI: 10.1021/jm4005362

実験手法

SOLUTION NMR