keyword
MENU ▼
Read by QxMD icon Read
search

bombesin

keyword
https://www.readbyqxmd.com/read/27902882/glycated-99m-tc-tricarbonyl-labeled-peptide-conjugates-for-tumor-targeting-by-click-to-chelate
#1
Karolin Römhild, Christiane A Fischer, Thomas L Mindt
Attaching polar pharmacological modifiers to molecular imaging probes is a common strategy to modulate their pharmacokinetic profiles to improve such parameters as the clearance rate of radiotracers and/or metabolites, and to enhance signal-to-background ratios. We combined the tumor-targeting peptide sequence of bombesin (BBN) with glucuronic acid and the single-photon emission computed tomography (SPECT) radionuclide (99m) Tc by the "click-to-chelate" methodology. The (99m) Tc-tricarbonyl-labeled glucuronated BBN conjugate was compared with a reference compound lacking the carbohydrate...
November 30, 2016: ChemMedChem
https://www.readbyqxmd.com/read/27875420/molecular-imaging-in-neuroendocrine-tumors-recent-advances-controversies-unresolved-issues-and-roles-in-management
#2
Tetsuhide Ito, Robert T Jensen
PURPOSE OF REVIEW: The purpose is to review recent advances in molecular imaging of neuroendocrine tumors (NETs), discuss unresolved issues, and review how these advances are affecting clinical management. RECENT FINDINGS: Molecular imaging of NETs underwent a number of important changes in the last few years, leading to some controversies, unresolved issues, and significant changes in clinical management. The most recent changes are reviewed in this article. Particularly important is the rapid replacement in somatostatin receptor scintigraphy of In-diethylenetriamine penta-acetic acid-single-photon emission computed tomography/computed tomography (CT) by Ga-fluorodopa(F-D)PA), 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid (DOTA)-peptide-PET/CT imaging, which is now approved in many countries including the USA...
November 21, 2016: Current Opinion in Endocrinology, Diabetes, and Obesity
https://www.readbyqxmd.com/read/27865999/approaches-to-improve-metabolic-stability-of-a-statine-based-grp-receptor-antagonist
#3
Ilinca Popp, Luigi Del Pozzo, Beatrice Waser, Jean Claude Reubi, Philipp T Meyer, Helmut R Maecke, Eleni Gourni
: The bombesin receptor family, in particular the gastrin-releasing peptide receptor (GRPr), is an attractive target in the field of nuclear oncology due to the high density of these receptors on the cell surface of several human tumors. The successful clinical implementation of (64)Cu-CB-TE2A-AR06, (68)Ga-RM2 and (68)Ga-NODAGA-MJ9, prompted us to continue the development of GRPr-antagonists. The aim of the present study was to assess if N-terminal modulations of the statine-based GRPr-antagonist influence the binding affinity, the pharmacokinetic performance and the in vivo metabolic stability...
November 4, 2016: Nuclear Medicine and Biology
https://www.readbyqxmd.com/read/27863916/structure-activity-relationship-study-towards-non-peptidic-positron-emission-tomography-pet-radiotracer-for-gastrin-releasing-peptide-receptors-development-of-18-f-s-3-1h-indol-3-yl-n-1-5-2-fluoroethoxy-pyridin-2-yl-cyclohexylmethyl-2-methyl-2-3-4-nitrophenyl
#4
Enza Lacivita, Ermelinda Lucente, Chantal Kwizera, Ines F Antunes, Mauro Niso, Paola De Giorgio, Roberto Perrone, Nicola A Colabufo, Philip H Elsinga, Marcello Leopoldo
Gastrin-releasing peptide receptors (GRP-Rs, also known as bombesin 2 receptors) are overexpressed in a variety of human cancers, including prostate cancer, and therefore they represent a promising target for in vivo imaging of tumors using positron emission tomography (PET). Structural modifications of the non-peptidic GRP-R antagonist PD-176252 ((S)-1a) led to the identification of the fluorinated analog (S)-3-(1H-indol-3-yl)-N-[1-[5-(2-fluoroethoxy)pyridin-2-yl]cyclohexylmethyl]-2-methyl-2-[3-(4-nitrophenyl)ureido]propionamide ((S)-1m) that showed high affinity and antagonistic properties for GRP-R...
October 29, 2016: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/27825431/pet-tracers-beyond-fdg-in-prostate-cancer
#5
REVIEW
David M Schuster, Cristina Nanni, Stefano Fanti
Conventional anatomical imaging with CT and MRI has limitations in the evaluation of prostate cancer. PET is a powerful imaging technique, which can be directed toward molecular targets as diverse as glucose metabolism, density of prostate-specific membrane antigen receptors, and skeletal osteoblastic activity. Although 2-deoxy-2-(18)F-FDG-PET is the mainstay of molecular imaging, FDG has limitations in typically indolent prostate cancer. Yet, there are many useful and emerging PET tracers beyond FDG, which provide added value...
November 2016: Seminars in Nuclear Medicine
https://www.readbyqxmd.com/read/27823569/structural-determinants-in-the-binding-of-bb2-receptor-ligands-in-silico-x-ray-and-nmr-studies-in-pd176252-analogues
#6
Antonio Carrieri, Enza Lacivita, Benny Danilo Belviso, Rocco Caliandro, Piero Mastrorilli, Vito Gallo, Mauro Niso, Marcello Leopoldo
The mammalian bombesin receptor family comprises three G protein-coupled receptors: the neuromedin B receptor, the gastrin-releasing peptide receptor (BB2), and the bombesin receptor subtype 3. BB2 receptor plays a role in gastrointestinal functions; however, at present the role of this subtype in physiological and pathological conditions is unknown due to the lack of specific binders for all subclasses of bombesin receptors. Here, we present a study focused on the properties of the peptoid bombesin antagonist called PD176252, and other structural analogues with the aim to elucidate causes of their different affinity towards the BB2 receptor...
November 4, 2016: Current Topics in Medicinal Chemistry
https://www.readbyqxmd.com/read/27775083/bacterial-mimetics-of-endocrine-secretory-granules-as-immobilized-in-vivo-depots-for-functional-protein-drugs
#7
María Virtudes Céspedes, Yolanda Fernández, Ugutz Unzueta, Rosa Mendoza, Joaquin Seras-Franzoso, Alejando Sánchez-Chardi, Patricia Álamo, Verónica Toledo-Rubio, Neus Ferrer-Miralles, Esther Vázquez, Simó Schwartz, Ibane Abasolo, José Luis Corchero, Ramon Mangues, Antonio Villaverde
In the human endocrine system many protein hormones including urotensin, glucagon, obestatin, bombesin and secretin, among others, are supplied from amyloidal secretory granules. These granules form part of the so called functional amyloids, which within the whole aggregome appear to be more abundant than formerly believed. Bacterial inclusion bodies (IBs) are non-toxic, nanostructured functional amyloids whose biological fabrication can be tailored to render materials with defined biophysical properties. Since under physiological conditions they steadily release their building block protein in a soluble and functional form, IBs are considered as mimetics of endocrine secretory granules...
October 24, 2016: Scientific Reports
https://www.readbyqxmd.com/read/27756093/mice-with-deletion-of-neuromedin-b-receptor-exhibit-decreased-oral-glucose-stimulated-insulin-release
#8
G S M Paula, L L Souza, N O S Bressane, R Maravalhas, M Wilieman, T Bento-Bernardes, K R Silva, L S Mendonca, K J Oliveira, C C Pazos-Moura
Neuromedin B (NB) and gastrin-releasing peptide (GRP) are bombesin-like peptides, found in the gastrointestinal tube and pancreas, among other tissues. Consistent data proposed that GRP stimulates insulin secretion, acting directly in pancreatic cells or in the release of gastrointestinal hormones that are incretins. However, the role of NB remains unclear. We examined the glucose homeostasis in mice with deletion of NB receptor (NBR-KO). Female NBR-KO exhibited similar fasting basal glucose with lower insulinemia (48...
December 2016: Hormone and Metabolic Research, Hormon- und Stoffwechselforschung, Hormones et Métabolisme
https://www.readbyqxmd.com/read/27754750/targeting-gastrointestinal-stromal-tumor-with-68-ga-labeled-peptides-an-in-vitro-study-on-gastrointestinal-stromal-tumor-cell-lines
#9
Achim Paulmichl, Dominik Summer, Claudia Manzl, Christine Rangger, Francesca Orlandi, Sabrina Niedermoser, Takahiro Taguchi, Björn Wängler, Clemens Decristoforo
The gastrointestinal stromal tumor (GIST) is a rare disease with limited therapeutic options when resistance to tyrosine kinase inhibitor (TKI) treatment occurs. The authors investigated binding of various (68)Ga-labeled peptides, targeting receptors reported to be overexpressed in GIST, in different cell lines. For this purpose, three GIST cell lines were tested: GIST-T1, GIST882 (Imatinib sensitive), and GIST430 (Imatinib resistant). DOTA-NT 8-13 (targeting NTR1), DOTA-TATE (targeting SSTR2), CP04 (a minigastrin derivative targeting CCK2-R), VIP-DOTA (targeting VPAC2-R), and 2 DOTA-bombesin derivatives [targeting gastrin releasing peptide receptors (GRPR)] were radiolabeled with (68)Ga and incubated with the respective tumor cell and control cell lines...
October 2016: Cancer Biotherapy & Radiopharmaceuticals
https://www.readbyqxmd.com/read/27694175/bombesin-targeted-pet-of-prostate-cancer
#10
Rosalba Mansi, Ryogo Minamimoto, Helmut Mäcke, Andrei H Iagaru
Imaging plays an important role in prostate cancer (PC), including accurate evaluation of the extent of disease, assessment of sites of recurrent disease, and monitoring of response to treatment. Molecular imaging techniques are among the novel developments related to the imaging of PC, and various SPECT and PET radiopharmaceuticals are now available in clinical trials or commercially. Here we describe the preclinical and clinical use of gastrin-releasing peptide receptors as targets for the imaging of PC, with a focus on the development of PET tracers for the imaging of gastrin-releasing peptide receptor-positive tumors...
October 2016: Journal of Nuclear Medicine: Official Publication, Society of Nuclear Medicine
https://www.readbyqxmd.com/read/27694174/evaluation-of-prostate-cancer-with-radiolabeled-amino-acid-analogs
#11
David M Schuster, Cristina Nanni, Stefano Fanti
Conventional imaging of prostate cancer has limitations related to the frequently indolent biology of the disease. PET is a functional imaging method that can exploit various aspects of tumor biology to enable greater detection of prostate cancer than can be provided by morphologic imaging alone. Radiotracers that are in use or under investigation for targeting salient features of prostate cancer include those directed to glucose, choline, acetate, prostate-specific membrane antigen, bombesin, and amino acids...
October 2016: Journal of Nuclear Medicine: Official Publication, Society of Nuclear Medicine
https://www.readbyqxmd.com/read/27693662/gastrin-releasing-peptide-receptor-mediates-the-excitation-of-preoptic-gabaergic-neurons-by-bombesin
#12
Karine Blais, Jasmine Sethi, Iustin V Tabarean
Bombesin, a pan agonist of the bombesin-like peptide receptor family, elicits potent hypothermia when applied centrally. The signaling mechanisms involved are not known. Here we report that GABAergic preoptic neurons express gastrin-releasing peptide (GRP) receptors and are directly excited by GRP or bombesin. This effect was abolished by a GRP receptor antagonist. A partially overlapping group of preoptic GABAergic neurons express bombesin-like receptor 3 (BRS3), however their activation results in a decrease in firing rate...
October 28, 2016: Neuroscience Letters
https://www.readbyqxmd.com/read/27670095/investigation-of-bombesin-peptide-as-a-targeting-ligand-for-the-gastrin-releasing-peptide-grp-receptor
#13
Anjuman Ara Begum, Peter M Moyle, Istvan Toth
Gastrin releasing peptide (GRP) receptor (GRPR), a bombesin family receptor, is overexpressed in many cancers including breast, prostate, pancreatic and lung. The targeting of therapeutics to GRPR can be achieved using the full-length (14 amino acid) GRP analogue Bombesin (BBN) or the truncated BBN(6-14) sequence, both of which bind GRPR with high affinity and specificity. In this study, we have investigated the level of GRPR expression in various cancerous (Caco-2, HeLa, LNCap, MDA-MB-231, and PC-3) and non-cancerous (WPMY-1) cell lines using a western blotting approach...
September 16, 2016: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/27665193/interaction-of-bombesin-and-its-fragments-with-gold-nanoparticles-analyzed-using-surface-enhanced-raman-spectroscopy
#14
Agnieszka Tąta, Aleksandra Szkudlarek, Younkyoo Kim, Edyta Proniewicz
This work demonstrates the application of commercially available stable surface composed of gold nanograins with diameters ranging from 70 to 226nm deposited onto silicon wafer for surface-enhanced Raman scattering investigations of biologically active compounds, such as bombesin (BN) and its fragments. BN is an important neurotransmitter involved in a complex signaling pathways and biological responses; for instance, hypertensive action, contractive on uterus, colon or ileum, locomotor activity, stimulation of gastric and insulin secretion as well as growth promotion of various tumor cell lines, including: lung, prostate, stomach, colon, and breast...
September 20, 2016: Spectrochimica Acta. Part A, Molecular and Biomolecular Spectroscopy
https://www.readbyqxmd.com/read/27598399/pulmonary-neuroendocrine-cell-hyperplasia-in-hemoglobin-bart-induced-hydrops-fetalis-a-model-for-chronic-intrauterine-hypoxia
#15
Mana Taweevisit, Boochit Theerasantipong, Kanlaya Taothong, Paul Scott Thorner
The pulmonary neuroendocrine system includes pulmonary neuroendocrine cells (PNECs) and neuroepithelial bodies (NEBs) that are distributed throughout respiratory epithelium, and regulate lung growth and maturation antenatally. Abnormalities in this system have been linked to many hypoxia-associated pediatric pulmonary disorders. Hemoglobin (Hb) Bart disease is a severe form of α-thalassemia resulting in marked intrauterine hypoxia with hydrops fetalis (HF) and usually death in utero. Affected fetuses can serve as a naturally occurring human model for the effects of intrauterine hypoxia and we postulated these effects should include changes in the pulmonary neuroendocrine system...
September 6, 2016: Pediatric and Developmental Pathology
https://www.readbyqxmd.com/read/27537699/improved-quantification-of-the-beta-cell-mass-after-pancreas-visualization-with-99m-tc-demobesin-4-and-beta-cell-imaging-with-111-in-exendin-3-in-rodents
#16
Inge van der Kroon, Lieke Joosten, Berthold A Nock, Theodosia Maina, Otto C Boerman, Maarten Brom, Martin Gotthardt
OBJECTIVE: Accurate assessment of the (111)In-exendin-3 uptake within the pancreas requires exact delineation of the pancreas, which is highly challenging by MRI and CT in rodents. In this study, the pancreatic tracer (99m)Tc-demobesin-4 was evaluated for accurate delineation of the pancreas to be able to accurately quantify (111)In-exendin-3 uptake within the pancreas. METHODS: Healthy and alloxan-induced diabetic Brown Norway rats were injected with the pancreatic tracer (99m)Tc-demobesin-4 ([(99m)Tc-N4-Pro(1),Tyr(4),Nle(14)]bombesin) and the beta cell tracer (111)In-exendin-3 ([(111)In-DTPA-Lys(40)]exendin-3)...
October 3, 2016: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/27497631/co-administration-of-succinylated-gelatine-with-a-99m-tc-bombesin-analogue-effects-on-pharmacokinetics-and-tumor-uptake
#17
Christos C Liolios, Stavros Xanthopoulos, George Loudos, Alexandra D Varvarigou, Gregory B Sivolapenko
The bombesin analogue, [(99m)Tc-GGC]-(Ornithine)3-BN(2-14), (99m)Tc-BN-O, targeting gastrin releasing peptide receptors (GRPrs) on the surface of tumors, was pre-clinically investigated as potential imaging agent for single photon emission computed tomography (SPECT). In addition, the improvement of its pharmacokinetic profile (PK) was investigated through the co-administration of a succinylated gelatin plasma expander (Gelofusine), aiming to reduce its kidney accumulation and enhance its tumor-to-normal tissue contrast ratios...
October 2016: Nuclear Medicine and Biology
https://www.readbyqxmd.com/read/27493267/clinical-translation-of-a-dual-integrin-%C3%AE-v%C3%AE-3-and-grpr-targeting-pet-radiotracer-68ga-nota-bbn-rgd
#18
Jingjing Zhang, Gang Niu, Lixin Lang, Fang Li, Xinrong Fan, Xuefeng Yan, Shaobo Yao, Weigang Yan, Li Huo, Libo Chen, Zhiyuan Li, Zhaohui Zhu, Xiaoyuan Chen
: This study aims to document the first-in-human application of a (68)Ga-labeled heterodimeric peptide BBN-RGD (bombesin-RGD) that targets both integrin αvβ3 and gastrin releasing peptide receptor (GRPR). We evaluated the safety and assessed the clinical diagnosis value of (68)Ga- BBN-RGD positron emission tomography (PET)/x-ray computed tomography (CT) in prostate cancer patients in comparison with (68)Ga-BBN. METHODS: Five healthy volunteers (M 4, F 1, 28-53 y) were enrolled to validate the safety of (68)Ga-BBN-RGD...
August 4, 2016: Journal of Nuclear Medicine: Official Publication, Society of Nuclear Medicine
https://www.readbyqxmd.com/read/27491709/synthesis-and-biological-evaluation-of-novel-imidazol-1-ylacetic-acid-derivatives-as-non-brain-penetrant-bombesin-receptor-subtype-3-brs-3-agonists
#19
Yohei Kiyotsuka, Kousei Shimada, Shozo Kobayashi, Masanori Suzuki, Mayuko Akiu, Masayoshi Asano, Yoshitaka Sogawa, Takashi Hara, Masahiro Konishi, Rie Abe-Ohya, Masanori Izumi, Yoko Nagai, Kazuhiro Yoshida, Yasuyuki Abe, Hideo Takamori, Hisashi Takahashi
Novel compounds based on 1a were synthesized with the focus of obtaining agonists acting upon peripheral BRS-3. To identify potent anti-obesity compounds without adverse effects on the central nervous system (CNS), a carboxylic acid moiety and a labile carboxylic ester with an antedrug functionality were introduced. Through the extensive synthetic exploration and the pharmacokinetic studies of intravenous administration in mice, the ester 2b was selected owing to its most suitable pharmacological profile. In the evaluation of food intake suppression in C57BL/6N mice, 2b showed significant in vivo efficacy and no clear adverse effects on blood pressure change in dogs administered the compound by intravenous infusion...
September 1, 2016: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/27487730/intracellular-elemental-patterns-of-apoptosis-resistance-in-transdifferentiated-androgen-dependent-prostatic-carcinoma-cells
#20
Mercedes Salido, Jose Vilches
The acquisition of neuroendocrine (NE) characteristics by prostate cancer (PC) cells relates to tumor progression and hormone resistance. PC cells may survive and function in androgen-deprived environments, where they could establish paracrine signaling networks, providing stimuli for the propagation of local carcinoma cells. We previously demonstrated, using electron probe X-ray microanalysis (EPXMA), in LNCaP, PC-3, and Du 145 cell lines that apoptosis is associated with intracellular elemental changes, and that the NE secretory products, bombesin and calcitonin, inhibit etoposide-induced apoptosis, as well as some of these elemental changes...
August 2016: Microscopy and Microanalysis
keyword
keyword
53332
1
2
Fetch more papers »
Fetching more papers... Fetching...
Read by QxMD. Sign in or create an account to discover new knowledge that matter to you.
Remove bar
Read by QxMD icon Read
×

Search Tips

Use Boolean operators: AND/OR

diabetic AND foot
diabetes OR diabetic

Exclude a word using the 'minus' sign

Virchow -triad

Use Parentheses

water AND (cup OR glass)

Add an asterisk (*) at end of a word to include word stems

Neuro* will search for Neurology, Neuroscientist, Neurological, and so on

Use quotes to search for an exact phrase

"primary prevention of cancer"
(heart or cardiac or cardio*) AND arrest -"American Heart Association"