10.1021/acs.jmedchem.6b01011.s002
Yibo Qiu
Yibo
Qiu
Misako Taichi
Misako
Taichi
Na Wei
Na
Wei
Huan Yang
Huan
Yang
Kathy Qian Luo
Kathy Qian
Luo
James P. Tam
James P.
Tam
An Orally Active
Bradykinin B<sub>1</sub> Receptor
Antagonist Engineered as a Bifunctional Chimera of Sunflower Trypsin
Inhibitor
American Chemical Society
2016
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
2016-12-05 00:00:00
Journal contribution
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.