Bombesin

Ladenheim, Ellen E.

doi:10.1016/b978-0-12-385095-9.00142-1

Cited by 6 publications

(8 citation statements)

References 30 publications

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“…It has long been reported that bombesin has an effect on satiety and pharmacological studies using selective agonists and antagonists suggested that GRPR and likely also the NMBR mediated these effects [129,161,171]. Studies using targeted disruption of the GRPR, NMBR and BRS-3 demonstrate that all three BnR subtypes have a role in satiety and energy homeostasis [129,161–163,249,259].…”

Section: Bnr Function In Normal Tissues (Table 2)mentioning

confidence: 99%

Insights into bombesin receptors and ligands: Highlighting recent advances

et al. 2015

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This following article is written for Prof. Abba Kastin’s Festschrift, to add to the tribute to his important role in the advancement of the role of peptides in physiological, as well as pathophysiological processes. There have been many advances during the 35 years of his prominent role in the Peptide field, not only as editor of the journal Peptides, but also as a scientific investigator and editor of two volumes of the Handbook of Biological Active Peptides [146,147]. Similar to the advances with many different peptides, during this 35 year period, there have been much progress made in the understanding of the pharmacology, cell biology and the role of (Bombesin) Bn receptors and their ligands in various disease states, since the original isolation of bombesin from skin of the European frog Bombina bombina in 1970 [76]. This paper will briefly review some of these advances over the time period of Prof Kastin 35 years in the peptide field concentrating on the advances since 2007 when many of the results from earlier studies were summarized [128,129]. It is appropriate to do this because there have been 280 articles published in Peptides during this time on Bombesin-related peptides and it accounts for almost 5% of all publications. Furthermore, 22 Bn publications we have been involved in have been published in either Peptides [14,39,55,58,81,92,93,119,152,216,225,226,231,280,302,309,355,361,362] or in the Prof Kastin’s Handbook of Biological Active Peptides [137,138,331].

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Section: Bnr Function In Normal Tissues (Table 2)mentioning

confidence: 99%

Insights into bombesin receptors and ligands: Highlighting recent advances

et al. 2015

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“…GRPR and NMBR)[2–4,8,9], it was found that BRS-3 knockout mice had alterations in feeding including increased feeding efficiency and hyperphagia[1,12,70,100–102]. In addition they developed mild obesity, hyperleptinemia, demonstrated impaired glucose metabolism, and even though they show reduced metabolic rates[1,12,70,100–102], which is not seen in many studies on human obesity, nevertheless, some authors[12] suggest, because of the other similarities, they could be a new model to study human obesity and associated diseases, such as diabetes. In addition to effects on energy and glucose homeostasis, BRS-3 knockout mice demonstrated behavioral changes[5,8,9,103,104], which possibly could affect feeding behavior.…”

Section: Brs-3 In Obesity; Energy and Glucose Homeostasis And Diabmentioning

confidence: 99%

“… Data are principally from [8,10,14,25,65,77,79,89,90] Abbreviations: NMB , neuromedin B; GRP , gastrin-releasing peptide; PLC -phospholipase C; Tyr kinase , tyrosine kinase cascades. Agonist/Antagonist structures : structure MK-5046 ,(2S)-1,1,1-trifluoro-2-[4-(1H-pyrazol-1-yl)phenyl]-3-(4-[[1-(trifluoromethyl)cyclopropyl]methyl]-1H-imidazol-2-yl)propan-2-ol[79]; 9f, [(5R)-4-((3-[(6-methylpyridin-3-yl)oxy]phenyl)acetyl)-8-(trifluoromethyl)-2,3,4,5-tetrahydro-1H-pyrido[2,3-e][1,4]diazepin-5-yl]acetic acid [77]; 9g , [(5R)-4-([3-(2-methylpropoxy)phenyl]acetyl)-8-(trifluoromethyl)- 2,3,4,5-tetrahydro-1H-pyrido[2,3-e][1,4]diazepin-5-yl]acetic acid (9g)[77]; 17c, 2-[(5 R )-4-[2-[3-(3-Methylbutanoyloxy)phenyl]acetyl]-8-(trifluoromethyl)-1,2,3,5-tetrahydropyrido[2,3- e ][1,4]diazepin-5-yl]acetic acid [76]; Bantag-1 , Boc-Phe-His-4-amino-5-cyclohexyl-2,4,5-trideoxypentonyl-Leu-(3-dimethylamino) benzylamide N-methylammonium trifluoroacetate [31,34]; PD168368, (3-(1H-indol-3-yl)-2-methyl-2-[3(4-nitro-phenyl)- ureido]-N-(1-pyridin-2-yl-cyclohexylmethyl)-propionamide) [27,99,132]. Alytesin , pGlu-Gln-Arg-Leu-Gly-Thr-Gln-Trp-Ala-Val-Gly-His-Phe-Met-NH 2 ; Bn, pGlu-Gln-Arg-Leu-Gly-Asn-Gln-Trp-Ala-Val-Gly-His-Phe-Met-NH 2 ; GRP, Ala-Pro-Val-Ser-Val-Gly-Gly-Gly-Thr-Val-Leu-Ala-Lys-Met-Tyr-Pro-Arg-Gly-Asn-His-Trp-Ala-Val-Gly-His-Leu-Met-NH 2 ; Litorin, pGlu- Gln-Trp-Ala-Val-Gly-His-Phe-Met-NH 2 ; NMB, Gly-Asn-Leu-Trp-Ala-Thr-Gly-His-Phe-Met-NH 2; ; Ranatensin, pGlu-Val-Pro-Gln-Trp-Ala-Val-Gly-His-Phe-Met-NH 2 ; pGlu denotes pyroglutamate…”

Section: Figmentioning

confidence: 99%

“…Ac , acetyl; Apa , 3-amino,propionic acid; Apa-4Cl , 4-chloro,3-amino,propionic acid; Bag-1 , (2-(4-(2-[5-(2,2-dimethylbutyl)-1H-imidazol-2-yl]ethyl)phenyl)pyridine[34]; Bag-2 (4′-(2-[5-(cyclopentylmethyl)- 1H-imidazol-2-yl]-1,2-ditritium-ethyl)biphenyl-2-carboxylic acid[34]; Cpa , chlorophenylalamine,; His(tBzl), histidine(tBenzl ); Cmpd 9, 2-(2-[4-(pyridin-2-yl)phenyl] ethyl)-5-(2,2-dimethylbutyl)- 1H-imidazole; Cmpd 16, phenyacetyl-Ala,DTrp, phenthylamide[68,69]; ML-18 , S-enantiomer of PD176252; Cpd 1t [88]: MK-7725 ,2-(3-(6-((4-(trifluoromethoxy)phenyl)sulfonyl)-2-(trifluoromethyl)-6,11-dihydro-5H-benzo[b]pyrido[2,3-e][1,4]diazepin-7-yl)-1,2,4-oxadiazol-5-yl)propan-2-ol[80,81]; Nip, piperidine-3 carboxylic acid; Nal, β-napthylalanine; Orn , ornithine; ψ ; pseudopeptide bond, ( i.e., CONH changed to CH 2 NH); Ph-Pr , phenylpropanolamine; PD176252 , (3-(1H-Indol-3-yl)-N-[1-(5-methoxy-pyridin-2-yl)-cyclohexylmethyl]-2-methyl-2-[3-(4-nitro-phenyl)-ureido]-propionamide); RY-337 [83]. …”

Section: Figmentioning

confidence: 99%

“…It has been well established by various experimental approaches, including the use of selective agonists and antagonists[1,2] and more recently, by receptor knockout studies[1,3–5], that two original members of the mammalian bombesin receptor(BnR) family, the gastrin releasing peptide receptor(GRPR,BB2) and the neuromedin B receptor(NMBR, BB1), play an important role in satiety. A third member of the mammalian BnR receptor family has been described[6,7], also a G-protein-coupled receptor, but, as will be reviewed in the next section, it is an orphan receptor at present, but because of close homology to the other two mammalian BnRs(i.e.…”

Section: Introductionmentioning

confidence: 99%

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Bombesin receptor subtype 3 as a potential target for obesity and diabetes

González

Moreno

Jensen

2015

Expert Opinion on Therapeutic Targets

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Summary Introduction Diabetes mellitus and obesity are important health issues; increasing in prevalence, both in the US and globally. There are only limited pharmacological treatments, and although bariatric surgery is effective, new effective pharmacologic treatments would be of great value. This review covers one area of increasing interest that could yield new novel treatments of obesity/diabetes mellitus. It involves recognition of the central role the G-protein-coupled receptor, bombesin receptor subtype 3(BRS-3) plays in energy/glucose metabolism. Areas covered Since the initial observation that BRS-3-knockout mice develop obesity, hypertension, impaired glucose-metabolism, and hyperphagia, there has been numerous studies of the mechanisms involved and the development of selective BRS-3-agonists/ antagonists which have marked effects on body weight, feeding, and glucose/insulin homeostasis. In this review each of these areas will be briefly reviewed. Expert opinion BRS-3 plays an important role in glucose/energy homeostasis. The development of potent, selective BRS-3 agonists demonstrates promise as a novel approach to treat obesity/diabetic states. One important question that needs to be addressed is whether BRS-3 agonists need to be centrally-acting. This is particular important in light of recent animal and human studies that report transient cardiovascular side-effects with centrally acting oral BRS-agonists.

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