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Updated: Aug 3, 2026
10:07
High-throughput Screening for Small-molecule Modulators of Inward Rectifier Potassium Channels
Published on: January 27, 2013
Bradykinin antagonists: present progress and future prospects
J M Stewart1, L Gera, E J York
1Department of Biochemistry and Molecular Genetics, University of Colorado Medical School, Denver 80262, USA. john.stewart@uchsc.edu
Immunopharmacology
|December 22, 1999
Summary
Bradykinin (BK) antagonists are valuable research tools and drug candidates for inflammation and cancer. The best peptide antagonist is orally available, stable, and effective against cancers in vivo.
Area of Science:
- Pharmacology
- Biochemistry
- Oncology
Background:
- Bradykinin (BK) antagonists are crucial for understanding kinin roles in physiology and disease.
- Peptide antagonists targeting BK B1 or B2 receptors, or both, are currently available.
- Non-peptide BK B2 antagonists are emerging as investigational drugs.
Purpose of the Study:
- To review the development and applications of bradykinin antagonist peptides.
- To highlight the potential of BK antagonists in treating inflammatory conditions and cancers.
- To discuss the characteristics and efficacy of advanced BK antagonists.
Main Methods:
- Review of existing literature on bradykinin antagonists.
- Analysis of peptide and non-peptide antagonist specificities and potencies.
- Evaluation of in vitro and in vivo data for cancer activity.
Main Results:
- Potent peptide antagonists exist for BK B1, B2, or both receptors.
- A superior peptide B1-B2 antagonist demonstrates stability, oral availability, and long in vivo half-life.
- Certain dimers and smaller molecules of this antagonist show activity against various cancers.
Conclusions:
- Bradykinin antagonist peptides are effective tools in physiological and pathological research.
- Advanced peptide antagonists offer therapeutic promise for inflammatory diseases and cancers.
- Further investigation into BK antagonist dimers and small molecules may yield novel cancer treatments.
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