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Orally Active Peptidic Bradykinin B1 Receptor Antagonists Engineered from a Cyclotide Scaffold for Inflammatory Pain Treatment

Authors

  • Clarence T. T. Wong,

    1. School of Biological Sciences, Nanyang Technological University, 60 Nanyang Drive, Singapore 637551 (Singapore)
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  • Dr. Dewi K. Rowlands,

    1. Laboratory Animal Service Centre, Faculty of Medicine, The Chinese University of Hong Kong, Prince of Wales Hospital, Hong Kong (China)
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  • Dr. Chi-Hang Wong,

    1. School of Biological Sciences, Nanyang Technological University, 60 Nanyang Drive, Singapore 637551 (Singapore)
    2. Current address: State Key Laboratory in Oncology in South China, Sir YK Pao Centre for Cancer, Department of Clinical Oncology, Hong Kong Cancer Institute, The Chinese University of Hong Kong (China)
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  • Dr. Theodore W. C. Lo,

    1. Laboratory Animal Service Centre, Faculty of Medicine, The Chinese University of Hong Kong, Prince of Wales Hospital, Hong Kong (China)
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  • Giang K. T. Nguyen,

    1. School of Biological Sciences, Nanyang Technological University, 60 Nanyang Drive, Singapore 637551 (Singapore)
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  • Prof. Hoi-Yeung Li,

    1. School of Biological Sciences, Nanyang Technological University, 60 Nanyang Drive, Singapore 637551 (Singapore)
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  • Prof. James P. Tam

    Corresponding author
    1. School of Biological Sciences, Nanyang Technological University, 60 Nanyang Drive, Singapore 637551 (Singapore)
    • School of Biological Sciences, Nanyang Technological University, 60 Nanyang Drive, Singapore 637551 (Singapore)
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  • This research was supported by Biomedical Research Council (BMRC 09/1/22/19/612) of A*STAR and Academic Research Fund (ARC21/08) of Ministry of Education in Singapore.

Abstract

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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 B1 receptor antagonist DALK (red in scheme) to obtain the cyclic bradykinin antagonist ckb-kal.

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