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Biology and pharmacology of bombesin receptor subtype-3.

AbstractPURPOSE OF REVIEW:
This review summarizes the results of recent studies regarding the biology and pharmacology of novel synthetic agonists and antagonists of the bombesin receptor subtype-3 (BRS-3).
RECENT FINDINGS:
All three mammalian bombesin receptors including gastrin-releasing peptide receptor, the neuromedin B receptor, and the BRS-3 have been shown to regulate energy balance and appetite and satiety. Studies indicate that the orphan BRS-3 is an important regulator of body weight, energy expenditure, and glucose homeostasis. Endogenous bombesin-like peptides bombesin, gastrin-releasing peptide, and neuromedin B receptor do not bind to BRS-3 and the endogenous BRS-3 ligand remains unknown. The novel synthesis of selective, high-affinity BRS-3 agonists and antagonists has recently been accomplished and showed that BRS-3 regulates energy balance independent of other established pathways and glucose-stimulated insulin secretion in the pancreatic islet cells. The availability of new BRS-3 selective agonists and antagonists will facilitate further elucidation of its role in energy homeostasis, and provides a potential approach for the pharmacological treatment of obesity and type 2 diabetes.
SUMMARY:
The native ligand of the G protein-coupled BRS-3 has not been identified as of now. However, novel synthesis of small-molecule, high-affinity agonists and antagonists on the BRS-3 was used in the recent studies and demonstrated an important role of BRS-3 in the regulation of energy homeostasis and glucose metabolism.
AuthorsIshita D Majumdar, Horst C Weber
JournalCurrent opinion in endocrinology, diabetes, and obesity (Curr Opin Endocrinol Diabetes Obes) Vol. 19 Issue 1 Pg. 3-7 (Feb 2012) ISSN: 1752-2978 [Electronic] England
PMID22157398 (Publication Type: Journal Article, Research Support, N.I.H., Extramural, Review)
Chemical References
  • Appetite Depressants
  • Blood Glucose
  • Receptors, Bombesin
  • bombesin receptor subtype 3
  • Gastrin-Releasing Peptide
Topics
  • Animals
  • Appetite Depressants (pharmacology)
  • Appetite Regulation (drug effects)
  • Blood Glucose
  • Diabetes Mellitus, Type 2 (drug therapy, metabolism)
  • Energy Metabolism
  • Gastrin-Releasing Peptide (pharmacology)
  • Homeostasis
  • Humans
  • Mice
  • Mice, Knockout
  • Obesity (drug therapy, metabolism)
  • Receptors, Bombesin (agonists, antagonists & inhibitors, metabolism)
  • Satiety Response (drug effects)
  • Signal Transduction (drug effects)

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