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https://www.readbyqxmd.com/read/28324017/a-novel-selective-bombesin-receptor-subtype-3-agonist-promotes-weight-loss-in-male-diet-induced-obese-rats-with-circadian-rhythm-change
#1
Yasunori Nio, Natsu Hotta, Minoru Maruyama, Kenichi Hamagami, Toshimi Nagi, Masaaki Funata, Junichi Sakamoto, Masanori Nakakariya, Nobuyuki Amano, Tomohiro Okawa, Yasuyoshi Arikawa, Shinobu Sasaki, Shoki Okuda, Shizuo Kasai, Yugo Habata, Yasutaka Nagisa
Bombesin receptor subtype 3 (BRS-3) is an orphan G-protein-coupled receptor. Based on the obese phenotype of male BRS-3-deficient mice, BRS-3 has been considered an attractive target for obesity treatment. Here, we developed a novel selective BRS-3 agonist (Compound-A) and evaluated its anti-obesity effects. Compound-A showed anorectic effects and enhanced energy expenditure in diet-induced obese (DIO)-F344 rats. Moreover, repeated oral administration of Compound-A for 7 days resulted in a significant body weight reduction in DIO-F344 rats...
March 16, 2017: Endocrinology
https://www.readbyqxmd.com/read/28315588/neuromedin-an-insight-into-its-types-receptors-and-therapeutic-opportunities
#2
REVIEW
Saumitra Gajjar, Bhoomika M Patel
Neuropeptides are small protein used by neurons in signal communications. Neuromedin U was the first neuropeptide discovered from the porcine spinal and showed its potent constricting activities on uterus hence was entitled with neuromedin U. Following neuromedin U another of its isoform was discovered neuromedin S which was observed in suprachiasmatic nucleus hence was entitled neuromedin S. Neuromedin K and neuromedin L are of kanassin class which belong to tachykinin family. Bombesin family consists of neuromedin B and neuromedin C...
January 22, 2017: Pharmacological Reports: PR
https://www.readbyqxmd.com/read/28267454/from-bench-to-bed-new-gastrin-releasing-peptide-receptor-directed-radioligands-and-their-use-in-prostate-cancer
#3
REVIEW
Theodosia Maina, Berthold A Nock
Gastrin-releasing peptide receptors (GRPRs) are overexpressed in prostate and breast cancer, and are therefore attractive molecular targets for diagnosis and therapy with radiolabeled GRPR-directed peptide probes. The amphibian tetradecapeptide bombesin or the mammalian gastrin-releasing peptide and neuromedin C have been modified with a variety of chelators. As a result, labeling with radiometals attractive for SPECT or PET imaging and for radionuclide therapy has led to the development of peptide radioligands suitable for in vivo targeting of prostate cancer...
April 2017: PET Clinics
https://www.readbyqxmd.com/read/28267450/imaging-of-prostate-cancer-using-gallium-68-labeled-bombesin
#4
REVIEW
Ida Sonni, Lucia Baratto, Andrei Iagaru
Nuclear medicine can play an important role in evaluating prostate cancer combining anatomical and functional information with hybrid techniques. Various PET radiopharmaceuticals have been used for targeting specific biological markers in prostate cancer. Research is ideally oriented towards the development of radiopharmaceuticals targeting antigens overexpressed in prostate cancer, as opposed to normal prostate tissue. In this regard, gastrin-releasing peptide receptors (GRPR) are excellent candidates. Bombesin analogues targeting the GRPR have been investigated...
April 2017: PET Clinics
https://www.readbyqxmd.com/read/28117023/an-overview-of-bioactive-peptides-for-in-vivo-imaging-and-therapy-in-human-diseases
#5
Anna Lucia Tornesello, Maria Lina Tornesello, Franco M Buonaguro
Radiolabeled peptides, designed to bind with high affinity receptors selectively expressed on cell membranes of different human tissues, represent valuable tools for in vivo imaging of several human diseases. Solid-phase peptide synthesis as well as availability of bifunctional chelating agents and prosthetic groups allows the production and radiolabeling of several peptide-based molecules which are useful to target specific receptors on different cancer types. Among them, octreotide and other analogues of somatostatin, vasoactive intestinal peptide, CCK analogues, bombesin, α-MSH analogues, neurotensin, exendin, RGD substance P, conjugated to appropriate chelators, such as DTPA, NOTA, DOTA or TETA, and radiolabeled with specific radionuclides, have already been translated into the clinical practice with remarkable sensitivity and diagnostic accurateness...
January 20, 2017: Mini Reviews in Medicinal Chemistry
https://www.readbyqxmd.com/read/28108545/bombesin-antagonist-based-radiotherapy-of-prostate-cancer-combined-with-wst-11-vascular-targeted-photodynamic-therapy
#6
Kwanghee Kim, Hanwen Zhang, Stephen LaRosa, Sylvia Jebiwott, Pooja Desai, Simon Y Kimm, Avigdor J Scherz, Joseph A O'Donoghue, Wolfgang A Weber, Jonathan Coleman
PURPOSE: DOTA-AR, a bombesin-antagonist peptide, has potential clinical application for targeted imaging and therapy in Gastrin Releasing Peptide receptor (GRPr) positive malignancies when conjugated with a radioisotope such as 90Y. This therapeutic potential is limited by the fast washout of the conjugates from the target tumors. WST-11 (Weizmann STeba-11 drug; a negatively charged water-soluble palladium-bacteriochlorophyll derivative, Tookad® Soluble) Vascular targeted photodynamic therapy (VTP) is a local ablation approach recently approved for use in early stage prostate cancer...
January 20, 2017: Clinical Cancer Research: An Official Journal of the American Association for Cancer Research
https://www.readbyqxmd.com/read/28088445/synthesis-and-exploration-of-novel-radiolabeled-bombesin-peptides-for-targeting-receptor-positive-tumor
#7
Kakali De, Indranil Banerjee, Samarendu Sinha, Shantanu Ganguly
Increasing evidence of peptide receptor overexpression in various cancer cells, warrant the development of receptor specific radiolabeled peptides for molecular imaging and therapy in nuclear medicine. Gastrin-releasing-peptide (GRP) receptor, are overexpressed in a variety of human cancer cells. The present study report the synthesis and biological evaluation of new bombesin (BBN) analogs, HYNIC-Asp-[Phe(13)]BBN(7-13)-NH-CH2-CH2-CH3:BA1, HYNIC-Pro-[Tyr(13)Met(14)]BBN(7-14)NH2:BA2 as prospective tumor imaging agent with compare to BBN(7-14)NH2:BS as standard...
March 2017: Peptides
https://www.readbyqxmd.com/read/28040598/radiolabeled-bombesin-derivatives-for-preclinical-oncological-imaging
#8
REVIEW
Carolina de Aguiar Ferreira, Leonardo Lima Fuscaldi, Danyelle M Townsend, Domenico Rubello, André Luís Branco de Barros
Despite efforts, cancer is still one of the leading causes of morbidity and mortality worldwide, with approximately 14 million new cases and 8.2 million cancer-related deaths each year, according to the World Health Organization. Among the strategies to reduce cancer progression and improving its management, implementing early detection technologies is crucial. Based on the fact that several types of cancer cells overexpress surface receptors, small molecule ligands, such as peptides, have been developed to allow tumor identification at earlier stages...
March 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/28034291/radiopharmaceuticals-for-diagnosis-and-therapy-of-neuroendocrine-differentiated-prostate-cancer
#9
Giampiero Giovacchini, Elisabetta Giovannini, Mattia Riondato, Andrea Ciarmiello
Neuroendocrine differentiation of prostate cancer (PCa) is a relatively frequent event, generally understudied, that carries important prognostic information. It is most frequently observed during the advanced stages of disease, when PCa has lost its sensitivity to androgen deprivation therapy or to chemotherapy, moderate to diffuse bone metastatic spread dominates the imaging scenario and it is responsible for painful clinical symptomatology. However, evidences indicate that neuroendocrine differentiation is a progressive phenomenon that starts at the very early part of the pathogenesis of cancer transformation contributing to it...
December 29, 2016: Current Radiopharmaceuticals
https://www.readbyqxmd.com/read/27902882/glycated-99m-tc-tricarbonyl-labeled-peptide-conjugates-for-tumor-targeting-by-click-to-chelate
#10
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
#11
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...
February 2017: 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
#12
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...
February 2017: 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
#13
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...
January 1, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/27825431/pet-tracers-beyond-fdg-in-prostate-cancer
#14
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
#15
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
#16
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
#17
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
#18
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
#19
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
#20
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
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