Bombesin receptor antagonists☆
References (215)
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Gastrin-releasing peptide (GRP) is not mammalian bombesin. Identification and molecular cloning of a true amphibian GRP distinct from amphibian bombesin in Bombina orientalis
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Parallel bioassay of 27 bombesin-like peptides on 9 smooth muscle preparations. Structure-activity relationships and bombesin receptor subtypes
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Progress in the development of potent bombesin receptor antagonists
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Spantide-induced antinociception in the opioid mechanism
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Effect of substance P/bombesin antagonists on the release of growth hormone by GHRP and GHRH
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Antagonism by GRP(18–27) and substance P analogues on insulin release stimulated by GRP(18–27)
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Des-Met carboxyl terminal modified analogues of bombesin function as potent bombesin receptor antagonists, partial agonists, or agonists
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Comparison of prolonged in vivo inhibitory activity of several potent bombesin (BN) antagonists on BN-stimulated amylase secretion in the rat
Peptides
A novel bombesin receptor antagonist (2258U89) potently inhibits bombesin evoked release of gastrointestinal hormones from rats and dogs, in vitro and in vivo
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[Des-Met14] bombesin analogues function as small cell lung cancer bombesin receptor antagonists
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Effect of bombesin antagonist D-Phe6-BN(6–13)OMe on vagally induced gastrin release from perfused rat stomach
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Effect of potent bombesin receptor antagonist on release of gut hormones in rats
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Effects of potent bombesin antagonist on exocrine pancreatic secretion in rats
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Development of a potent bombesin receptor antagonist with prolonged in vivo inhibitory activity on bombesin-stimulated amylase and protein release in the rat
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Bombesin receptor antagonists differentiate receptor subtypes in rat brain
Eur J Pharmacol
Structure-activity requirements of bombesin for gastrin-releasing peptide- and neuromedin B-preferring bombesin receptors in rat brain
Eur J Pharmacol
Identification and initial characterization of a putative neuromedin B-type receptor from rat urinary bladder membranes
Eur J Pharmacol
Metabolic stability and tumor inhibition of bombesin/GRP receptor antagonists
Peptides
Purification and characterization of the bombesin/gastrin releasing peptide receptor from Swiss 3T3 cells
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Gastrin releasing peptide (GRP): central nervous system (CNS) action to inhibit gastric secretion in rats
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Carboxyl-terminal modification of a gastrin releasing peptide derivative generates potent antagonists
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Isolation and structure of bombesin and alytesin, two analogous active peptides from the skin of the European amphibian Bombina and Alytes
Experientia
Amino acid composition and sequence of litorin, a bombesin-like nonapeptide occurring in methanol extracts of the skin of the Australian leptodactylid frog Litoria aurea
Experientia
Isolation and structure of a new vasoactive polypeptide
Two new frog skin peptides, phyllolitorins, of the bombesin-ranatensin family Phyllomedusa sauvagei
Biomed Res
Characterization of a gastrin releasing peptide from porcine non-antral gastric tissue
FEBS Lett
Neuromedin B: a novel bombesin-like peptide identified in porcine spinal cord
Biochem Biophys Res Commun
Production of neuromedin B and neuromedin B gene expression in human lung tumor cell lines
Cancer Res
Cloning and characterization of cDNAs encoding human gastrin-releasing peptides
Molecular cloning of cDNAs encoding the human bombesin-like peptide neuromedin B
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Receptors for neurokinins, tachykinins, and bombesin: a pharmacological study
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Neuromedin B receptor in esophagus: evidence for subtypes of bombesin receptor
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Receptor heterogeneity for bombesin-like peptides in the rat central nervous system
Brain Res
Potent bombesin receptor antagonists distinguish receptor subtypes
Am J Physiol
Two distinct bombesin receptor subtypes are expressed and functional in human lung carcinoma cells
J Biol Chem
Evidence for the existence of separate receptors for gastrin releasing peptide, neuromedin B and phyllolitorin in human tumour cell lines
Br J Cancer
Bombesin stimulation of mitogenesis. Specific receptors, signal transduction, and early events
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Receptor for bombesin with associated tyrosine kinase activity
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Bombesin, vasopressin, and endothelin rapidly stimulate tyrosine phosphorylation in intact Swiss 3T3 cells
Cited by (38)
Peptide radiopharmaceuticals for targeted diagnosis & therapy of human tumors
2022, Nuclear Medicine and Molecular Imaging: Volume 1-4Theranostic Prospects of Gastrin-Releasing Peptide Receptor–Radioantagonists in Oncology
2017, PET ClinicsCitation Excerpt :Selected sst2-radioantagonists with improved biological features are currently undergoing clinical trials as candidate radiopharmaceuticals in the theranostic management of NETs and other sst2-positive tumors.57,58 An additional asset in the development of GRPR-radioantagonists is the great number of GRPR-antagonists developed since many decades by peptide chemists with the aim to better unravel the pharmacology and the role of bombesin receptors in health and disease.59 These analogues were designed and synthesized after site-directed structural modifications at several positions of the native BBN and GRP sequences, including amino acid substitutions, reduction of peptide bonds, or peptide-chain truncations.
Pharmacological characteristics of bombesin receptor mediating hypothermia in the central nervous system of rats
2003, Brain ResearchCitation Excerpt :Pretreatment with 7 μg of this antagonist did not influence the hypothermia with statistical significance. However, 2–30 μg of [d-Tyr6]BN(6–13)methylester (TBNME), one of the most selective and potent GRP-R antagonists [3,12], dose-dependently blocked the hypothermia (Fig. 2). In addition, the influence of BIM23127 (30 μg), an NMB-R antagonist [11,14], on the BN-induced effect was examined.
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This paper was reviewed by Dr Robert T. Jensen, NIH/NIDDK/DDB, 10/9C103, 10 Center DR MSC 1804, Bethesda, MD20892-1804, USA and Jean Martinez, C.P.M.I.B., FacultC de Pharmacie, 15, avenue Charles Flahault, 34060 Montpellier Cedex 1, France.
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Presently retired.