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An Orally Active Bradykinin B1 Receptor Antagonist Engineered as a Bifunctional Chimera of Sunflower Trypsin Inhibitor
Qiu Y.1; Taichi M.2; Wei N.1; Yang H.3; Luo K.Q.4; Tam J.P.1
2017-01-12
Source PublicationJournal of Medicinal Chemistry
ISSN15204804 00222623
Volume60Issue:1Pages:504-510
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.

DOI10.1021/acs.jmedchem.6b01011
URLView the original
Indexed BySCI
WOS Research AreaPharmacology & Pharmacy
WOS SubjectChemistry, Medicinal
WOS IDWOS:000392035100035
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Cited Times [WOS]:12   [WOS Record]     [Related Records in WOS]
Document TypeJournal article
CollectionFaculty of Health Sciences
Affiliation1.Nanyang Technological University
2.Riken
3.Jiangsu University
4.Universidade de Macau
Recommended Citation
GB/T 7714
Qiu Y.,Taichi M.,Wei N.,et al. An Orally Active Bradykinin B1 Receptor Antagonist Engineered as a Bifunctional Chimera of Sunflower Trypsin Inhibitor[J]. Journal of Medicinal Chemistry,2017,60(1):504-510.
APA Qiu Y.,Taichi M.,Wei N.,Yang H.,Luo K.Q.,&Tam J.P..(2017).An Orally Active Bradykinin B1 Receptor Antagonist Engineered as a Bifunctional Chimera of Sunflower Trypsin Inhibitor.Journal of Medicinal Chemistry,60(1),504-510.
MLA Qiu Y.,et al."An Orally Active Bradykinin B1 Receptor Antagonist Engineered as a Bifunctional Chimera of Sunflower Trypsin Inhibitor".Journal of Medicinal Chemistry 60.1(2017):504-510.
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