Orally active peptidic bradykinin B 1 receptor antagonists engineered from a cyclotide scaffold for inflammatory pain treatment

Clarence T.T. Wong; Dewi K. Rowlands; Chi Hang Wong; Theodore W.C. Lo; Giang K.T. Nguyen; Hoi Yeung Li; James P. Tam

doi:10.1002/anie.201200984

Orally active peptidic bradykinin B ₁ receptor antagonists engineered from a cyclotide scaffold for inflammatory pain treatment

Clarence T.T. Wong, Dewi K. Rowlands, Chi Hang Wong, Theodore W.C. Lo, Giang K.T. Nguyen, Hoi Yeung Li, James P. Tam^*

^*Corresponding author for this work

Research output: Contribution to journal › Article › peer-review

203 Citations (Scopus)

Abstract

Edible: By grafting natural peptide antagonists onto the cyclotide kalata B1, orally active peptides were engineered, which are potentially useful therapeutics for the treatment of inflammatory pain. For example, the entire loop 6 of kalata B1 was replaced with the peptidic bradykinin B ₁ receptor antagonist DALK (red in scheme) to obtain the cyclic bradykinin antagonist ckb-kal.

Original language	English
Pages (from-to)	5620-5624
Number of pages	5
Journal	Angewandte Chemie - International Edition
Volume	51
Issue number	23
DOIs	https://doi.org/10.1002/anie.201200984
Publication status	Published - Jun 4 2012
Externally published	Yes

ASJC Scopus Subject Areas

Catalysis
General Chemistry

Keywords

analgesics
cyclotides
drug design
peptides
thioester ligations

Access to Document

10.1002/anie.201200984

Cite this

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title = "Orally active peptidic bradykinin B 1 receptor antagonists engineered from a cyclotide scaffold for inflammatory pain treatment",

abstract = "Edible: By grafting natural peptide antagonists onto the cyclotide kalata B1, orally active peptides were engineered, which are potentially useful therapeutics for the treatment of inflammatory pain. For example, the entire loop 6 of kalata B1 was replaced with the peptidic bradykinin B 1 receptor antagonist DALK (red in scheme) to obtain the cyclic bradykinin antagonist ckb-kal.",

keywords = "analgesics, cyclotides, drug design, peptides, thioester ligations",

author = "Wong, {Clarence T.T.} and Rowlands, {Dewi K.} and Wong, {Chi Hang} and Lo, {Theodore W.C.} and Nguyen, {Giang K.T.} and Li, {Hoi Yeung} and Tam, {James P.}",

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AU - Wong, Clarence T.T.

AU - Rowlands, Dewi K.

AU - Wong, Chi Hang

AU - Lo, Theodore W.C.

AU - Nguyen, Giang K.T.

AU - Li, Hoi Yeung

AU - Tam, James P.

PY - 2012/6/4

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AB - Edible: By grafting natural peptide antagonists onto the cyclotide kalata B1, orally active peptides were engineered, which are potentially useful therapeutics for the treatment of inflammatory pain. For example, the entire loop 6 of kalata B1 was replaced with the peptidic bradykinin B 1 receptor antagonist DALK (red in scheme) to obtain the cyclic bradykinin antagonist ckb-kal.

KW - analgesics

KW - cyclotides

KW - drug design

KW - peptides

KW - thioester ligations

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