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https://www.readbyqxmd.com/read/29786467/bombesin-functionalized-64-cu-copper-sulfide-nanoparticles-for-targeted-imaging-of-orthotopic-prostate-cancer
#1
Huawei Cai, Fang Xie, Aditi Mulgaonkar, Lihong Chen, Xiankai Sun, Jer-Tsong Hsieh, Fangyu Peng, Rong Tian, Lin Li, Changqiang Wu, Hua Ai
AIM: To synthesize and evaluate the imaging potential of Bom-PEG-[64 Cu]CuS nanoparticles (NPs) in orothotopic prostate tumor. MATERIALS & METHODS: [64 Cu]CuS NPs were synthesized in aqueous solution by 64 CuCl2 and Na2 S reaction. Then PEG linker with or without bombesin peptide were conjugated to the surface of [64 Cu]CuS NPs to produce Bom-PEG-[64 Cu]CuS and PEG-[64 Cu]CuS NPs. These two kinds of NPs were used for testing specific uptake in prostate cancer cells in vitro and imaging of orthotopic prostate tumor in vivo...
May 22, 2018: Nanomedicine
https://www.readbyqxmd.com/read/29746998/urokinase-injection-triggered-clearance-enhancement-of-a-4-arm-peg-conjugated-64-cu-bombesin-analog-tetramer-a-novel-approach-for-the-improvement-of-pet-imaging-contrast
#2
Kazushi Matsumura, Maki Zouda, Yasuhiro Wada, Fumiyoshi Yamashita, Mitsuru Hashida, Yasuyoshi Watanabe, Hidefumi Mukai
Radiolabeled antibodies, polyethylene glycol-conjugated (PEGylated) peptides, liposomes, and other materials were investigated as positron-emission tomography (PET) probes. These substances accumulate in tumors but often remain too long in circulation. We investigated the combination of intravenous urokinase injection and its substrate linker as a triggered radioisotope clearance enhancement system to improve imaging contrast. To this end, we synthesized a four-arm PEGylated 64 Cu-bombesin analog tetramer with a urokinase substrate linker...
May 7, 2018: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/29732057/sequence-dependent-attack-on-peptides-by-photoactivated-platinum-anticancer-complexes
#3
Christopher A Wootton, Carlos Sanchez-Cano, Andrea F Lopez-Clavijo, Evyenia Shaili, Mark P Barrow, Peter J Sadler, Peter B O'Connor
Octahedral platinum(iv) complexes such as trans , trans , trans -[Pt(N3 )2 (OH)2 (pyridine)2 ] ( 1 ) are stable in the dark, but potently cytotoxic to a range of cancer cells when activated by UVA or visible light, and active in vivo . Photoactivation causes the reduction of the complex and leads to the formation of unusual Pt(ii) lesions on DNA. However, radicals are also generated in the excited state resulting from photoactivation (J. S. Butler, J. A. Woods, N. J. Farrer, M. E. Newton and P. J. Sadler, J...
March 14, 2018: Chemical Science
https://www.readbyqxmd.com/read/29672153/p21-activated-kinase4-in-pancreatic-acini-is-activated-by-gi-hormones-growth-factors-by-novel-signaling-and-is-needed-to-stimulate-secretory-growth-cascades
#4
Irene Ramos-Alvarez, Robert T Jensen
p21-activated kinases(PAKs) are highly conserved serine/threonine protein kinases, which are divided into two groups:Group-I(PAKs1-3) and Group-II(PAKs4-6). In various tissues, Group-II PAKs play important roles in cytoskeletal dynamics, cell growth as well as neoplastic development/progression. However, little is known about Group-II PAKs role in a number of physiological events including their ability to be activated by gastrointestinal(GI) hormones/neurotransmitters/growth-factors(GFs). We used rat pancreatic acini to explore the ability of GI-hormones/neurotransmitters/GFs to activate Group-II-PAKs and the signaling cascades involved...
April 19, 2018: American Journal of Physiology. Gastrointestinal and Liver Physiology
https://www.readbyqxmd.com/read/29596439/expression-of-progenitor-markers-is-associated-with-the-functionality-of-a-bioartificial-adrenal-cortex
#5
Mariya Balyura, Evgeny Gelfgat, Charlotte Steenblock, Andreas Androutsellis-Theotokis, Gerard Ruiz-Babot, Leonardo Guasti, Martin Werdermann, Barbara Ludwig, Tobias Bornstein, Andrew V Schally, Ana Brennand, Stefan R Bornstein
Encapsulation of primary bovine adrenocortical cells in alginate is an efficacious model of a bioartificial adrenal cortex. Such a bioartificial adrenal cortex can be used for the restoration of lost adrenal function in vivo as well as for in vitro modeling of the adrenal microenvironment and for investigation of cell-cell interactions in the adrenals. The aim of this work was the optimization of a bioartificial adrenal cortex, that is the generation of a highly productive, self-regenerating, long-term functioning and immune tolerant bioartificial organ...
2018: PloS One
https://www.readbyqxmd.com/read/29587479/novel-64-cu-labeled-rgd-2-bbn-heterotrimers-for-pet-imaging-of-prostate-cancer
#6
Ermelinda Lucente, Hongguang Liu, Yang Liu, Xiang Hu, Enza Lacivita, Marcello Leopoldo, Zhen Cheng
Bombesin receptor 2 (BB2 ) and integrin αv β3 receptor are privileged targets for molecular imaging of cancer because their overexpression in a number of tumor tissues. The most recent developments in heterodimer-based radiopharmaceuticals concern BB2 - and integrin αv β3 -targeting compounds, consisting of bombesin (BBN) and RGD peptides, connected through short length linkers. Molecular imaging probes based on RGD-BBN heterodimer design exhibit improved tumor targeting efficacy compared to the single-receptor targeting peptide monomers...
March 27, 2018: Bioconjugate Chemistry
https://www.readbyqxmd.com/read/29571038/a-trithiol-bifunctional-chelate-for-72-77-as-a-matched-pair-theranostic-complex-with-high-in-vivo-stability
#7
Yutian Feng, Anthony J DeGraffenreid, Michael D Phipps, Tammy L Rold, Nkemakonam C Okoye, Fabio A Gallazzi, Charles L Barnes, Cathy S Cutler, Alan R Ketring, Timothy J Hoffman, Silvia S Jurisson
INTRODUCTION: Trithiol chelates are suitable for labeling radioarsenic (72 As: 2.49 MeV β+ , 26 h;77 As: 0.683 MeV β- , 38.8 h) to form potential theranostic radiopharmaceuticals for PET imaging and therapy. To investigate the in vivo stability of trithiol chelates complexed with no carrier added (nca) radioarsenic, a bifunctional trithiol chelate was developed, and conjugated to bombesin(7-14)NH2 as a model peptide. METHODS: A trithiol-BBN(7-14)NH2 bioconjugate and its arsenic complex were synthesized and characterized...
March 10, 2018: Nuclear Medicine and Biology
https://www.readbyqxmd.com/read/29568682/bombesin-receptor-subtype-3-expressing-neurons-regulate-energy-homeostasis-through-a-novel-neuronal-pathway-in-the-hypothalamus
#8
Minoru Maruyama, Natsu Hotta, Yasunori Nio, Kenichi Hamagami, Toshimi Nagi, Masaaki Funata, Junichi Sakamoto, Masanori Nakakariya, Nobuyuki Amano, Mayumi Nishida, Tomohiro Okawa, Yasuyoshi Arikawa, Shinobu Sasaki, Shizuo Kasai, Yasutaka Nagisa, Yugo Habata, Masaaki Mori
Objectives: Bombesin receptor subtype-3 (BRS-3) has been suggested to play a potential role in energy homeostasis. However, the physiological mechanism of BRS-3 on energy homeostasis remains unknown. Thus, we investigated the BRS-3-mediated neuronal pathway involved in food intake and energy expenditure. Materials and Methods: Expression of BRS-3 in the rat brain was histologically examined. The BRS-3 neurons activated by refeeding-induced satiety or a BRS-3 agonist were identified by c-Fos immunostaining...
January 2018: Brain and Behavior
https://www.readbyqxmd.com/read/29556947/in-vivo-stabilized-sb3-an-attractive-grpr-antagonist-for-pre-and-intra-operative-imaging-for-prostate-cancer
#9
Ingrid L Bakker, Sandra T van Tiel, Joost Haeck, Gabriela N Doeswijk, Erik de Blois, Marcel Segbers, Theodosia Maina, Berthold A Nock, Marion de Jong, Simone U Dalm
PURPOSE: The gastrin-releasing peptide receptor (GRPR), overexpressed on various tumor types, is an attractive target for receptor-mediated imaging and therapy. Another interesting approach would be the use of GRPR radioligands for pre-operative imaging and subsequent radio-guided surgery, with the goal to improve surgical outcome. GRPR radioligands were successfully implemented in clinical studies, especially Sarabesin 3 (SB3) is an appealing GRPR antagonist with high receptor affinity...
March 19, 2018: Molecular Imaging and Biology: MIB: the Official Publication of the Academy of Molecular Imaging
https://www.readbyqxmd.com/read/29438170/diffuse-idiopathic-pulmonary-neuroendocrine-cell-hyperplasia-dipnech-syndrome-and-carcinoid-tumors-with-without-nech-a-clinicopathologic-radiologic-and-immunomolecular-comparison-study
#10
Maria Cecilia Mengoli, Giulio Rossi, Alberto Cavazza, Renato Franco, Federica Zito Marino, Mario Migaldi, Letizia Gnetti, Enrico Maria Silini, Luca Ampollini, Marcello Tiseo, Filippo Lococo, Ludovic Fournel, Paolo Spagnolo, Vincent Cottin, Thomas V Colby
The diagnostic criteria of diffuse idiopathic pulmonary neuroendocrine cell hyperplasia (DIPNECH) are not well defined, and DIPNECH can be mistaken for carcinoids associated with neuroendocrine cell hyperplasia (NECH). In this study, we compared clinical, radiologic, histologic, immunohistochemical, and molecular features of DIPNECH and isolated carcinoids with/without NECH. The study population included 151 cases (77 female patients and 74 male patients), 19 with DIPNECH and 132 with carcinoids with/without NECH...
May 2018: American Journal of Surgical Pathology
https://www.readbyqxmd.com/read/29432691/monomeric-and-dimeric-68-ga-labeled-bombesin-analogues-for-positron-emission-tomography-pet-imaging-of-tumors-expressing-gastrin-releasing-peptide-receptors-grprs
#11
Christos Liolios, Benjamin Buchmuller, Ulrike Bauder-Wüst, Martin Schäfer, Karin Leotta, Uwe Haberkorn, Matthias Eder, Klaus Kopka
The GRPr, highly expressed in prostate PCa and breast cancer BCa, is a promising target for the development of new PET radiotracers. The chelator HBED-CC ( N, N'-bis[2-hydroxy-5-(carboxyethyl)benzyl]ethylenediamine- N, N'-diacetic acid) was coupled to the bombesin peptides: HBED-C-BN(2-14) 1, HBED-CC-PEG2 -[d-Tyr6 ,β-Ala11 ,Thi13 ,Nle14 ]-BN(6-14) 2, HBED-CC-Y-[d-Phe6 ,Sta13 ,Leu14 ]-BN(6-14) (Y = 4-amino-1-carboxymethylpiperidine) 3, and HBED-CC-{PEG2 -Y-[d-Phe6 ,Sta13 ,Leu14 ]-BN(6-14)}2 4 (homodimer). Compounds 1-4 presented high binding affinities for GRPr (T47D, 0...
March 8, 2018: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29410320/a-possible-new-target-in-lung-cancer-cells-the-orphan-receptor-bombesin-receptor-subtype-3
#12
Paola Moreno, Samuel A Mantey, Suk H Lee, Irene Ramos-Álvarez, Terry W Moody, Robert T Jensen
Human bombesin receptors, GRPR and NMBR, are two of the most frequently overexpressed G-protein-coupled-receptors by lung-cancers. Recently, GRPR/NMBR are receiving considerable attention because they act as growth factor receptors often in an autocrine manner in different lung-cancers, affect tumor angiogenesis, their inhibition increases the cytotoxic potency of tyrosine-kinase inhibitors reducing lung-cancer cellular resistance/survival and their overexpression can be used for sensitive tumor localization as well as to target cytotoxic agents to the cancer...
March 2018: Peptides
https://www.readbyqxmd.com/read/29402494/activation-of-bombesin-receptor-subtype-3-by-d-tyr-6-%C3%AE-ala-11-phe-13-nle-14-bombesin-6-14-increased-glucose-uptake-and-lipogenesis-in-human-and-rat-adipocytes
#13
Zaida Moreno-Villegas, Antonio Martín-Duce, César Aparicio, Sergio Portal-Núñez, Raúl Sanz, Samuel A Mantey, Robert T Jensen, Oscar Lorenzo, Jesús Egido, Nieves González
BRS-3 has an important role in glucose homeostasis. Its expression was reduced in skeletal muscle from obese and/or diabetic patients, and BRS-3 KO-mice developed obesity. In this work, focused on rat/human adipose tissue, BRS-3 gene-expression was lower than normal-levels in hyperlipidemic, type-2-diabetic (T2D), and type-1-diabetic rats and also in obese (OB) and T2D patients. Moreover, BRS-3 protein levels were decreased in diabetic rat and in obese and diabetic human fat pieces; but neither mutation nor even polymorphism in the BRS-3-gene was found in OB or T2D patients...
January 31, 2018: Molecular and Cellular Endocrinology
https://www.readbyqxmd.com/read/29401613/receptor-specific-crosstalk-between-prostanoid-e-receptor-3-and-bombesin-receptor-subtype-3
#14
Yan Zhang, Yanfang Liu, Lehao Wu, Chao Fan, Zhiwei Wang, Xiuli Zhang, Amal Alachkar, Xinmiao Liang, Olivier Civelli
Bombesin receptor subtype 3 (BRS-3) is a GPCR that is expressed in the CNS, peripheral tissues, and tumors. Our understanding of BRS-3's role in physiology and pathophysiology is limited because its natural ligand is unknown. In an attempt to identify this ligand, we screened toad skin ( Bufo bufo gargarizans Cantor) extracts and identified prostaglandins as putative ligands. In BRS-3-transfected human embryonic kidney (HEK) cells, we found that prostaglandins, with prostaglandin E2 (PGE2) being the most potent, fulfill the pharmacologic criteria of affinity, selectivity, and specificity to be considered as agonists to the BRS-3 receptor...
January 22, 2018: FASEB Journal: Official Publication of the Federation of American Societies for Experimental Biology
https://www.readbyqxmd.com/read/29393253/activation-of-bombesin-receptor-subtype-3-promotes-antigen-presenting-action-in-human-bronchial-epithelial-cells
#15
Huijun Liu, Lihua Peng, Chi Liu, Yurong Tan, Yang Xiang, Xiangping Qu, H Christian Weber, Minhui Dai, Xiaoqun Qin
BACKGROUND: Bombesin receptor subtype-3 (BRS-3) is a member of the bombesin-like peptide receptor family. Our previous studies demonstrated that activation of the human BRS-3 plays a protective role in oxidation-injured human bronchial epithelial cells (HBEC). The present study was designed to determine the role of BRS-3 activation in the antigen-presenting action of HBEC and the corresponding proliferation and differentiation of T cells. MATERIALS AND METHODS: In vivo, an asthma animal model was established and the expression and distribution of BRS-3 were analyzed by immunocytochemistry...
2018: International Archives of Allergy and Immunology
https://www.readbyqxmd.com/read/29352726/corrigendum-to-bombesin-like-receptor-3-brs3-expression-in-glutamatergic-but-not-gabaergic-neurons-is-required-for-regulation-of-energy-metabolism-mol-metabol-6-2017-1540-1550
#16
Cuiying Xiao, Ramón A Piñol, Jesse Lea Carlin, Cuiling Li, Chuxia Deng, Oksana Gavrilova, Marc L Reitman
No abstract text is available yet for this article.
March 2018: Molecular Metabolism
https://www.readbyqxmd.com/read/29277445/biased-g-protein-coupled-receptor-agonism-mediates-neu1-sialidase-and-matrix-metalloproteinase-9-crosstalk-to-induce-transactivation-of-insulin-receptor-signaling
#17
Fiona Haxho, Sabah Haq, Myron R Szewczuk
G protein-coupled receptors (GPCR) can participate in a number of signaling pathways, and this property led to the concept of biased GPCR agonism. Agonists, antagonists and allosteric modulators can bind to GPCRs in different ways, creating unique conformations that differentially modulate signaling through one or more G proteins. A unique neuromedin B (NMBR) GPCR-signaling platform controlling mammalian neuraminidase-1 (Neu1) and matrix metalloproteinase-9 (MMP9) crosstalk has been reported in the activation of the insulin receptor (IR) through the modification of the IR glycosylation...
March 2018: Cellular Signalling
https://www.readbyqxmd.com/read/29192382/multimodal-molecular-3d-imaging-for-the-tumoral-volumetric-distribution-assessment-of-folate-based-biosensors
#18
Gerardo J Ramírez-Nava, Clara L Santos-Cuevas, Isaac Chairez, Liliana Aranda-Lara
The aim of this study was to characterize the in vivo volumetric distribution of three folate-based biosensors by different imaging modalities (X-ray, fluorescence, Cerenkov luminescence, and radioisotopic imaging) through the development of a tridimensional image reconstruction algorithm. The preclinical and multimodal Xtreme imaging system, with a Multimodal Animal Rotation System (MARS), was used to acquire bidimensional images, which were processed to obtain the tridimensional reconstruction. Images of mice at different times (biosensor distribution) were simultaneously obtained from the four imaging modalities...
December 1, 2017: Medical & Biological Engineering & Computing
https://www.readbyqxmd.com/read/29154145/evaluation-of-a-novel-grpr-antagonist-for-prostate-cancer-pet-imaging-64-cu-dotha-2-peg-rm26
#19
Nematallah Mansour, Michel Paquette, Samia Ait-Mohand, Véronique Dumulon-Perreault, Brigitte Guérin
INTRODUCTION: Gastrin releasing peptide receptors (GRPRs) are significantly over-expressed on a large proportion of prostate cancers making them prime candidates for receptor-mediated nuclear imaging by PET. Recently, we synthesized a novel bifunctional chelator (BFC) bearing hydroxamic acid arms (DOTHA2 ). Here we investigated the potential of a novel DOTHA2 -conjugated, 64 Cu-radiolabeled GRPR peptide antagonist, [D-Phe6 -Sta13 -Leu14 -NH2 ]bombesin(6-14) (DOTHA2 -PEG-RM26) to visualize prostate tumors by PET imaging...
January 2018: Nuclear Medicine and Biology
https://www.readbyqxmd.com/read/29133874/distinct-roles-of-nmb-and-grp-in-itch-transmission
#20
Li Wan, Hua Jin, Xian-Yu Liu, Joseph Jeffry, Devin M Barry, Kai-Feng Shen, Jia-Hang Peng, Xue-Ting Liu, Jin-Hua Jin, Yu Sun, Ray Kim, Qing-Tao Meng, Ping Mo, Jun Yin, Ailin Tao, Rita Bardoni, Zhou-Feng Chen
A key question in our understanding of itch coding mechanisms is whether itch is relayed by dedicated molecular and neuronal pathways. Previous studies suggested that gastrin-releasing peptide (GRP) is an itch-specific neurotransmitter. Neuromedin B (NMB) is a mammalian member of the bombesin family of peptides closely related to GRP, but its role in itch is unclear. Here, we show that itch deficits in mice lacking NMB or GRP are non-redundant and Nmb/Grp double KO (DKO) mice displayed additive deficits. Furthermore, both Nmb/Grp and Nmbr/Grpr DKO mice responded normally to a wide array of noxious stimuli...
November 13, 2017: Scientific Reports
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