An Orally Active
Bradykinin B<sub>1</sub> Receptor
Antagonist Engineered as a Bifunctional Chimera of Sunflower Trypsin
Inhibitor
Yibo Qiu
Misako Taichi
Na Wei
Huan Yang
Kathy Qian Luo
James P. Tam
10.1021/acs.jmedchem.6b01011.s002
https://acs.figshare.com/articles/journal_contribution/An_Orally_Active_Bradykinin_B_sub_1_sub_Receptor_Antagonist_Engineered_as_a_Bifunctional_Chimera_of_Sunflower_Trypsin_Inhibitor/4451189
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.
2016-12-05 00:00:00
serum half-life
Sunflower Trypsin Inhibitor
6 h
fusion cyclic peptide
bradykinin receptor antagonist peptide
sunflower trypsin inhibitor -1.
Bifunctional Chimera
plate assay
metabolically
peptide TIBA
Bradykinin B 1 Receptor Antagonist Engineered
animal pain model
chimera TIBA