Biology and pharmacology of bombesin receptor subtype-3
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). All three mammalian bombesin receptors including gastrin-releasing peptide receptor, the neuromedin B receptor, and the...
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Veröffentlicht in: | Current opinion in endocrinology, diabetes, and obesity diabetes, and obesity, 2012-02, Vol.19 (1), p.3-7 |
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description | 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).
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.
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. |
doi_str_mv | 10.1097/MED.0b013e32834ec77d |
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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.
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.</description><identifier>ISSN: 1752-296X</identifier><identifier>EISSN: 1752-2978</identifier><identifier>DOI: 10.1097/MED.0b013e32834ec77d</identifier><identifier>PMID: 22157398</identifier><language>eng</language><publisher>England: Wolters Kluwer Health, Inc. All rights reserved</publisher><subject>Animals ; Appetite Depressants - pharmacology ; Appetite Regulation - drug effects ; Blood Glucose ; Diabetes Mellitus, Type 2 - drug therapy ; Diabetes Mellitus, Type 2 - metabolism ; Energy Metabolism ; Gastrin-Releasing Peptide - pharmacology ; Homeostasis ; Humans ; Mice ; Mice, Knockout ; Obesity - drug therapy ; Obesity - metabolism ; Receptors, Bombesin - agonists ; Receptors, Bombesin - antagonists & inhibitors ; Receptors, Bombesin - metabolism ; Satiety Response - drug effects ; Signal Transduction - drug effects</subject><ispartof>Current opinion in endocrinology, diabetes, and obesity, 2012-02, Vol.19 (1), p.3-7</ispartof><rights>Wolters Kluwer Health, Inc. All rights reserved.</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c3513-e64aa99100de0a5cb47d56e0bf0031ef09933e91fa800e84c63578e0e07d97b63</citedby><cites>FETCH-LOGICAL-c3513-e64aa99100de0a5cb47d56e0bf0031ef09933e91fa800e84c63578e0e07d97b63</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><link.rule.ids>314,780,784,27924,27925</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/22157398$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Majumdar, Ishita D.</creatorcontrib><creatorcontrib>Weber, Horst C.</creatorcontrib><title>Biology and pharmacology of bombesin receptor subtype-3</title><title>Current opinion in endocrinology, diabetes, and obesity</title><addtitle>Curr Opin Endocrinol Diabetes Obes</addtitle><description>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).
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.
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.</description><subject>Animals</subject><subject>Appetite Depressants - pharmacology</subject><subject>Appetite Regulation - drug effects</subject><subject>Blood Glucose</subject><subject>Diabetes Mellitus, Type 2 - drug therapy</subject><subject>Diabetes Mellitus, Type 2 - metabolism</subject><subject>Energy Metabolism</subject><subject>Gastrin-Releasing Peptide - pharmacology</subject><subject>Homeostasis</subject><subject>Humans</subject><subject>Mice</subject><subject>Mice, Knockout</subject><subject>Obesity - drug therapy</subject><subject>Obesity - metabolism</subject><subject>Receptors, Bombesin - agonists</subject><subject>Receptors, Bombesin - antagonists & inhibitors</subject><subject>Receptors, Bombesin - metabolism</subject><subject>Satiety Response - drug effects</subject><subject>Signal Transduction - drug effects</subject><issn>1752-296X</issn><issn>1752-2978</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2012</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNpdkF9LwzAUxYMobk6_gUjffOq8SZqmedQ5_8DEFwXfQtLeumq71KRl7Ntb2Zzgw-UeLuecCz9CzilMKSh59TS_nYIFypGzjCeYS1kckDGVgsVMyexwr9O3ETkJ4QNASCnEMRkxRoXkKhsTeVO52r1vIrMqonZpfGPy7cGVkXWNxVCtIo85tp3zUehtt2kx5qfkqDR1wLPdnpDXu_nL7CFePN8_zq4Xcc4F5TGmiTFKUYACwYjcJrIQKYItATjFEpTiHBUtTQaAWZKnXMgMAUEWStqUT8jltrf17qvH0OmmCjnWtVmh64NWlFHIkkQNzmTrzL0LwWOpW181xm80Bf1DTA_E9H9iQ-xi96C3DRb70C-iv961qzv04bPu1-j1Ek3dLTVQlqbAVMwGBQwA4mGA828pWXbd</recordid><startdate>20120201</startdate><enddate>20120201</enddate><creator>Majumdar, Ishita D.</creator><creator>Weber, Horst C.</creator><general>Wolters Kluwer Health, Inc. All rights reserved</general><scope>CGR</scope><scope>CUY</scope><scope>CVF</scope><scope>ECM</scope><scope>EIF</scope><scope>NPM</scope><scope>AAYXX</scope><scope>CITATION</scope><scope>7X8</scope></search><sort><creationdate>20120201</creationdate><title>Biology and pharmacology of bombesin receptor subtype-3</title><author>Majumdar, Ishita D. ; Weber, Horst C.</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c3513-e64aa99100de0a5cb47d56e0bf0031ef09933e91fa800e84c63578e0e07d97b63</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2012</creationdate><topic>Animals</topic><topic>Appetite Depressants - pharmacology</topic><topic>Appetite Regulation - drug effects</topic><topic>Blood Glucose</topic><topic>Diabetes Mellitus, Type 2 - drug therapy</topic><topic>Diabetes Mellitus, Type 2 - metabolism</topic><topic>Energy Metabolism</topic><topic>Gastrin-Releasing Peptide - pharmacology</topic><topic>Homeostasis</topic><topic>Humans</topic><topic>Mice</topic><topic>Mice, Knockout</topic><topic>Obesity - drug therapy</topic><topic>Obesity - metabolism</topic><topic>Receptors, Bombesin - agonists</topic><topic>Receptors, Bombesin - antagonists & inhibitors</topic><topic>Receptors, Bombesin - metabolism</topic><topic>Satiety Response - drug effects</topic><topic>Signal Transduction - drug effects</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Majumdar, Ishita D.</creatorcontrib><creatorcontrib>Weber, Horst C.</creatorcontrib><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><collection>CrossRef</collection><collection>MEDLINE - Academic</collection><jtitle>Current opinion in endocrinology, diabetes, and obesity</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Majumdar, Ishita D.</au><au>Weber, Horst C.</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Biology and pharmacology of bombesin receptor subtype-3</atitle><jtitle>Current opinion in endocrinology, diabetes, and obesity</jtitle><addtitle>Curr Opin Endocrinol Diabetes Obes</addtitle><date>2012-02-01</date><risdate>2012</risdate><volume>19</volume><issue>1</issue><spage>3</spage><epage>7</epage><pages>3-7</pages><issn>1752-296X</issn><eissn>1752-2978</eissn><abstract>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).
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.
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.</abstract><cop>England</cop><pub>Wolters Kluwer Health, Inc. All rights reserved</pub><pmid>22157398</pmid><doi>10.1097/MED.0b013e32834ec77d</doi><tpages>5</tpages></addata></record> |
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subjects | Animals Appetite Depressants - pharmacology Appetite Regulation - drug effects Blood Glucose Diabetes Mellitus, Type 2 - drug therapy Diabetes Mellitus, Type 2 - metabolism Energy Metabolism Gastrin-Releasing Peptide - pharmacology Homeostasis Humans Mice Mice, Knockout Obesity - drug therapy Obesity - metabolism Receptors, Bombesin - agonists Receptors, Bombesin - antagonists & inhibitors Receptors, Bombesin - metabolism Satiety Response - drug effects Signal Transduction - drug effects |
title | Biology and pharmacology of bombesin receptor subtype-3 |
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