5H1H

NMR structure of SLBA, a chimera of SFTI

5H1H の概要

• エントリーDOI: 10.2210/pdb5h1h/pdb
• 関連するPDBエントリー: 5H1I
• NMR情報: BMRB: 36023
• 分子名称: Bradykinin-trypsin inhibitor secondary loop chimera (1 entity in total)
• 機能のキーワード: slba, sunflower trypsin inhibitor, cyclic peptide, disulphide bond, de novo protein
• 由来する生物種: Helianthus annuus
• タンパク質・核酸の鎖数: 1
• 化学式量合計: 1780.10

構造登録者

Xiao, T.,Tam, J.P. (登録日: 2016-10-10, 公開日: 2017-04-19, 最終更新日: 2024-11-20)

主引用文献

Qiu, Y.,Taichi, M.,Wei, N.,Yang, H.,Luo, K.Q.,Tam, J.P.
An Orally Active Bradykinin B1 Receptor Antagonist Engineered as a Bifunctional Chimera of Sunflower Trypsin Inhibitor.
J. Med. Chem., 60:504-510, 2017

PubMed Abstract: An orally active and metabolically stable peptide TIBA was successfully engineered as a chimera by fusing an analgesic bradykinin receptor antagonist peptide and the trypsin inhibitory loop of sunflower trypsin inhibitor-1. As a fusion cyclic peptide, the metabolically labile analgesic peptide is protected from degradation by exopeptidases as well as the endopeptidases, and its serum half-life extended from <5 min to >6 h as a chimera. Moreover, the chimera TIBA was also found to be orally active in an animal pain model using a hot plate assay.

PubMed: 27977181
DOI: 10.1021/acs.jmedchem.6b01011

実験手法

SOLUTION NMR