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