Gastrointestinal hormones: Edited by Robert LoweBombesin-related peptides and their receptors: recent advances in their role in physiology and disease statesGonzalez, Nievesa; Moody, Terry Wb; Igarashi, Hisatoc; Ito, Tetsuhidec; Jensen, Robert TaAuthor Information aDigestive Diseases Branch, National Institutes of Health, Bethesda, Maryland, USA bNational Cancer Institute, National Institutes of Health, Bethesda, Maryland, USA cDepartment of Medicine and Bioregulatory Science, Graduate School of Medical Science, Kyushu University, Fukuoka, Japan Correspondence to Dr R. T. Jensen, National Institutes of Health, Building 10, Room 9C-103, Bethesda, MD 20892, USA Tel: +1 301 496 4201; fax: +1 301 402 0600; e-mail: [email protected] Current Opinion in Endocrinology, Diabetes and Obesity: February 2008 - Volume 15 - Issue 1 - p 58-64 doi: 10.1097/MED.0b013e3282f3709b Buy Metrics Abstract Purpose of review Mammalian bombesin-related peptides, gastrin-releasing peptide and neuromedin B actions are mediated by two receptors (BB1-receptor, BB2-receptor), which are closely related to the orphan receptor BRS-3 (BB3-receptor). The purpose of this review is to highlight advances in the understanding of these peptides in physiology/disease states. Recent findings Pharmacologic/receptor-knockout studies show involvement of these receptors in a number of new processes/diseases. Neuromedin B/BB1-receptor is an important physiological regulator of pituitary–thyroid function; in mediating behavior, especially feas/anxiety; in mediating satiety through different cascades than gastrin-releasing peptide/BB2 receptors and for its autocrine tumor-growth effects. Gastrin-releasing peptide/BB2-receptor plays important roles in mediating signals for pruritus, lung development/injury, small intestinal mucosal defense, and central nervous system processes such as learning/memory. The signaling mechanisms of its potent growth effects are being elucidated and their possible therapeutic targets identified. BB3-receptor knockout mice provided insights for their obesity/glucose intolerance and demonstrated that this receptor may be important in the lung response to injury, tumor growth and gastrointestinal motility. Each receptor is frequently overexpressed in human tumors and has potent growth effects. This effect is being explored to develop new antitumor treatments, such as bombesin-receptor ligands conjugated to cytotoxic agents. Summary This receptor family is involved in an increasing number of central nervous system/peripheral processes physiologically and in disease states, and increased understanding of its role may lead to novel treatments. © 2008 Lippincott Williams & Wilkins, Inc.