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Bombesin Receptor Subtype-3 in Human Diseases
Mei Li1, Peng Liang1, Di Liu1
1Hunan Key Laboratory of Kidney Disease and Blood Purification, Department of Nephrology, The Second Xiangya Hospital of Central South University, Changsha, Hunan, China.
Archives of Medical Research
|January 9, 2020
Summary
Bombesin receptor subtype-3 (BRS-3) plays a key role in tumor growth, metabolism, and lung development. Research into BRS-3 agonists and antagonists is advancing our understanding of its involvement in diseases like cancer and diabetes.
Area of Science:
- Pharmacology
- Endocrinology
- Oncology
Background:
- Bombesin receptor subtype-3 (BRS-3) is a G protein-coupled receptor involved in various physiological processes.
- Its natural ligand remains unidentified, classifying it as an orphan receptor.
- Two mammalian bombesin-like peptides, GRP and NMB, bind to three receptors, including BRS-3, mediating diverse functions.
Purpose of the Study:
- To review recent findings on the roles of BRS-3 in diverse patho-physiological conditions.
- To summarize the impact of BRS-3 on tumor growth, energy homeostasis, glucose regulation, satiety, and lung development.
- To discuss the implications of BRS-3 modulation in diseases such as lung cancer, obesity, diabetes, asthma, and kidney diseases.
Main Methods:
- Review of existing literature on BRS-3.
- Analysis of knockout studies in mice to understand BRS-3 functions.
- Examination of synthesized agonists and antagonists for BRS-3 characterization.
Main Results:
- BRS-3 knockout mice exhibit significant alterations in tumor growth, energy balance, glucose metabolism, satiety, and lung development.
- Selective, high-affinity BRS-3 agonists (e.g., (D-Tyr6, β-Ala11, Phe13, Nle14) Bn-(6-14), MK-5046) and antagonists (e.g., ML-18, Bantag-1) have been developed.
- These pharmacological tools have provided insights into BRS-3's biological effects in various disease models.
Conclusions:
- BRS-3 is implicated in critical physiological functions and pathological conditions.
- Targeting BRS-3 with specific agonists or antagonists holds therapeutic potential for lung cancer, metabolic disorders, and other diseases.
- Further research into BRS-3's natural ligand and signaling pathways is warranted.
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