jm6b01011_si_002.pdf (1.36 MB)
An Orally Active Bradykinin B1 Receptor Antagonist Engineered as a Bifunctional Chimera of Sunflower Trypsin Inhibitor
journal contribution
posted on 2016-12-05, 00:00 authored by Yibo Qiu, Misako Taichi, Na Wei, Huan Yang, Kathy Qian Luo, James P. TamAn 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.