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https://www.readbyqxmd.com/read/28417160/diagnosis-of-recurrent-prostate-cancer-with-pet-ct-imaging-using-the-gastrin-releasing-peptide-receptor-antagonist-68-ga-rm2-preliminary-results-in-patients-with-negative-or-inconclusive-18-f-fluoroethylcholine-pet-ct
#1
Gesche Wieser, Ilinca Popp, H Christian Rischke, Vanessa Drendel, Anca-Ligia Grosu, Mark Bartholomä, Wolfgang A Weber, Rosalba Mansi, Ulrich Wetterauer, Wolfgang Schultze-Seemann, Philipp T Meyer, Cordula Annette Jilg
PURPOSE/BACKGROUND: [(18)F]fluoroethylcholine ((18)FECH) has been shown to be a valuable PET-tracer in recurrent prostate cancer (PCa), but still has limited accuracy. RM2 is a gastrin-releasing peptide receptor (GRPr) antagonist that binds to GRPr on PCa cells. Recent studies suggest that GRPr imaging with PET/CT is a promising technique for staging and restaging of PCa. We explore the value of GRPr-PET using the (68)Ga-labeled GRPr antagonist RM2 in a selected population of patients with biochemically recurrent PCa and a negative/inconclusive (18)FECH-PET/CT...
April 18, 2017: European Journal of Nuclear Medicine and Molecular Imaging
https://www.readbyqxmd.com/read/28294319/grpr-antagonist-protects-from-drug-induced-liver-injury-by-impairing-neutrophil-chemotaxis-and-motility
#2
Rafael S Czepielewski, Natália Jaeger, Pedro E Marques, Maísa M Antunes, Maurício M Rigo, Débora M Alvarenga, Rafaela V Pereira, Rodrigo D da Silva, Tiago G Lopes, Vinícius D da Silva, Bárbara N Porto, Gustavo B Menezes, Cristina Bonorino
Drug-induced liver injury (DILI) is a major cause of acute liver failure (ALF), where hepatocyte necrotic products trigger liver inflammation, release of CXCR2 ligands (IL-8) and other neutrophil chemotactic molecules. Liver infiltration by neutrophils is a major cause of the life threatening tissue damage that ensues. A GRPR (gastrin-releasing peptide receptor) antagonist impairs IL-8-induced neutrophil chemotaxis in vitro. We investigated its potential to reduce acetaminophen-induced ALF, neutrophil migration and mechanisms underlying this phenomenon...
March 10, 2017: European Journal of Immunology
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/28228560/expression-of-il-22-in-the-skin-causes-th2-biased-immunity-epidermal-barrier-dysfunction-and-pruritus-via-stimulating-epithelial-th2-cytokines-and-the-grp-pathway
#5
Hongfei Lou, Jingning Lu, Eun Byul Choi, Min Hee Oh, Mingeum Jeong, Sara Barmettler, Zhou Zhu, Tao Zheng
Increased expression of Th22 cytokine IL-22 is a characteristic finding in atopic dermatitis (AD). However, the specific role of IL-22 in the pathogenesis of AD in vivo has yet to be elucidated. Consistent with observations in human AD, IL-22 was significantly increased in the AD skin of mice after epicutaneous sensitization to house dust mite allergen. Utilizing a skin-specific inducible transgenic system, we show in the present study that expression of IL-22 in the skin of mice caused an AD-like phenotype characterized by chronic pruritic dermatitis associated with Th2-biased local and systemic immune responses, downregulation of epidermal differentiation complex genes, and enhanced dermatitis upon epicutaneous allergen exposure...
April 1, 2017: Journal of Immunology: Official Journal of the American Association of Immunologists
https://www.readbyqxmd.com/read/28157737/spinal-cord-interneurons-expressing-the-gastrin-releasing-peptide-receptor-convey-itch-through-vglut2-mediated-signaling
#6
Bejan Aresh, Fabio B Freitag, Sharn Perry, Edda Blümel, Joey Lau, Marina C M Franck, Malin C Lagerström
Itch is a sensation that promotes the desire to scratch, which can be evoked by mechanical and chemical stimuli. In the spinal cord, neurons expressing the gastrin-releasing peptide receptor (GRPR) have been identified as specific mediators of itch. However, our understanding of the GRPR population in the spinal cord, and thus how these neurons exercise their functions, is limited. For this purpose, we constructed a Cre line designed to target the GRPR population of neurons (Grpr-Cre). Our analysis revealed that Grpr-Cre cells in the spinal cord are predominantly excitatory interneurons that are found in the dorsal lamina, especially in laminae II-IV...
May 2017: Pain
https://www.readbyqxmd.com/read/28134770/review-receptor-targeted-nuclear-imaging-of-breast-cancer
#7
REVIEW
Simone U Dalm, John Fred Verzijlbergen, Marion De Jong
Receptor targeted nuclear imaging directed against molecular markers overexpressed on breast cancer (BC) cells offers a sensitive and specific method for BC imaging. Currently, a few targets such as estrogen receptor (ER), progesterone receptor (PR), human epidermal growth factor receptor 2 (HER2), somatostatin receptor (SSTR), and the gastrin releasing peptide receptor (GRPR) are being investigated for this purpose. Expression of these targets is BC subtype dependent and information that can be gained from lesion visualization is dependent on the target; ER-targeting radiotracers, e...
January 26, 2017: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/28129446/impact-of-dianionic-and-dicationic-linkers-on-tumor-uptake-and-biodistribution-of-64-cu-cu-nota-peptide-based-gastrin-releasing-peptide-receptors-antagonists
#8
Nematallah Mansour, Véronique Dumulon-Perreault, Samia Ait-Mohand, Michel Paquette, Roger Lecomte, Brigitte Guérin
In this study, we investigated for the first time the influence of 2-aminoethyl-piperazine-1-carboxylic acid (APCA) and amino-hexanedioic-1-acid (AHDA) on tumor uptake and elimination kinetics of [(64) Cu]-radiolabeled gastrin releasing peptide receptors (GRPR) antagonists. Three GRPR antagonists containing the RM26 sequence were synthesized and conjugated with NOTA via different linkers (LK): polyethylene glycol (PEG-neutral), APCA (dicationic) or AHDA (dianionic). The NOTA-LK-RM26 peptides were radiolabeled with (64) Cu to assess their pharmacokinetic and positron emission tomography (PET) imaging properties using PC3 tumor-bearing athymic nude mice...
January 27, 2017: Journal of Labelled Compounds & Radiopharmaceuticals
https://www.readbyqxmd.com/read/28108545/bombesin-antagonist-based-radiotherapy-of-prostate-cancer-combined-with-wst-11-vascular-targeted-photodynamic-therapy
#9
Kwanghee Kim, Hanwen Zhang, Stephen La Rosa, Sylvia Jebiwott, Pooja Desai, Simon Kimm, Avigdor Scherz, Joseph A O'Donoghue, Wolfgang A Weber, Jonathan A 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 (90)Y. 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/28107508/prospects-of-targeting-the-gastrin-releasing-peptide-receptor-and-somatostatin-receptor-2-for-nuclear-imaging-and-therapy-in-metastatic-breast-cancer
#10
Simone U Dalm, Willemijne A M E Schrijver, Anieta M Sieuwerts, Maxime P Look, Angelique C J Ziel-van der Made, Vanja de Weerd, John W Martens, Paul J van Diest, Marion de Jong, Carolien H M van Deurzen
BACKGROUND: The gastrin releasing peptide receptor (GRPR) and the somatostatin receptor 2 (SSTR2) are overexpressed on primary breast cancer (BC), making them ideal candidates for receptor-mediated nuclear imaging and therapy. The aim of this study was to determine whether these receptors are also suitable targets for metastatic BC. METHODS: mRNA expression of human BC samples were studied by in vitro autoradiography and associated with radioligand binding. Next, GRPR and SSTR2 mRNA levels of 60 paired primary BCs and metastases from different sites were measured by quantitative reverse transcriptase polymerase chain reaction...
2017: PloS One
https://www.readbyqxmd.com/read/27865999/approaches-to-improve-metabolic-stability-of-a-statine-based-grp-receptor-antagonist
#11
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/27827443/tm1-ir680-peptide-for-assessment-of-surgical-margin-and-lymph-node-metastasis-in-murine-orthotopic-model-of-oral-cancer
#12
Annie A Suganya S, K J Kochurani, Madhumathy G Nair, Jiss Maria Louis, Santhosh Sankaran, R Rajagopal, K Santhosh Kumar, Parvin Abraham, Balagopal P G, Paul Sebastian, Thara Somananthan, Tessy Thomas Maliekal
Treatment outcome after surgical removal in oral carcinoma is poor due to inadequate methodologies available for marking surgical margins. Even though some methodologies for intraoperative margin assessment are under clinical and preclinical trials for other solid tumours, a promising modality for oral cancer surgery is not developed. Fluorescent-based optical imaging using Near Infrared (NIR) dyes tagged to tumour specific target will be an optimal tool for this purpose. One such target, Gastrin Releasing Peptide Receptor (GRPR) was selected for the study, and its binding peptide, TM1-IR680, was tested for its efficacy for surgical margin prediction in murine orthotopic model of oral cancer, derived from primary samples...
November 9, 2016: Scientific Reports
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
#13
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/27675066/monitoring-prostate-cancer-treatment-response-to-radiation-therapy-and-androgen-deprivation-with-novel-radiolabeled-and-dual-labeled-gastrin-releasing-peptide-receptor-grpr-antagonists
#14
N K Taunk, H Zhang, S Carlin, W Weber
No abstract text is available yet for this article.
October 1, 2016: International Journal of Radiation Oncology, Biology, Physics
https://www.readbyqxmd.com/read/27670095/investigation-of-bombesin-peptide-as-a-targeting-ligand-for-the-gastrin-releasing-peptide-grp-receptor
#15
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/27609789/68ga-177lu-neobomb1-a-novel-radiolabeled-grpr-antagonist-for-theranostic-use-in-oncology
#16
Simone U Dalm, Ingrid L Bakker, Erik de Blois, Gabriela N Doeswijk, Mark W Konijnenberg, Francesca Orlandi, Donato Barbato, Mattia Tedesco, Theodosia Maina, Berthold A Nock, Marion de Jong
INTRODUCTION: Since overexpression of the gastrin releasing peptide receptor (GRPR) has been reported on various cancer types, e.g. prostate cancer and breast cancer, targeting this receptor with radioligands might have significant impact on staging and treatment of GRPR-expressing tumors. NeoBOMB1 is a novel DOTA-coupled GRPR antagonist with high affinity for GRPR and excellent in vivo stability. The purpose of this preclinical study was to further explore the use of NeoBOMB1 for theranostic application by determining the biodistribution of (68)Ga-NeoBOMB1 and (177)Lu-NeoBOMB1...
September 8, 2016: Journal of Nuclear Medicine: Official Publication, Society of Nuclear Medicine
https://www.readbyqxmd.com/read/27539743/gastrin-releasing-peptide-facilitates-glutamatergic-transmission-in-the-hippocampus-and-effectively-prevents-vascular-dementia-induced-cognitive-and-synaptic-plasticity-deficits
#17
Jiajia Yang, Yang Yao, Ling Wang, Chunxiao Yang, Faqi Wang, Jie Guo, Zhiyun Wang, Zhuo Yang, Dong Ming
Neuronal gastrin-releasing peptide (GRP) has been proved to be an important neuromodulator in the brain and involved in a variety of neurological diseases. Whether GRP could attenuate cognition impairment induced by vascular dementia (VD) in rats, and the mechanism of synaptic plasticity and GRP's action on synaptic efficiency are still poorly understood. In this study, we first investigated the effects of GRP on glutamatergic transmission with patch-clamp recording. We found that acute application of GRP enhanced the excitatory synaptic transmission in hippocampal CA1 neurons via GRPR in a presynaptic mechanism...
August 15, 2016: Experimental Neurology
https://www.readbyqxmd.com/read/27516447/dual-modality-imaging-of-prostate-cancer-with-a-fluorescent-and-radiogallium-labeled-gastrin-releasing-peptide-receptor-antagonist
#18
Hanwen Zhang, Pooja Desai, Yusuke Koike, Jacob Houghton, Sean Carlin, Nidhi Tandon, Karim Touijer, Wolfgang A Weber
Gastrin-releasing peptide (GRP) receptors (GRPr) are frequently overexpressed in human prostate cancer, and radiolabeled GRPr affinity ligands have shown promise for in vivo imaging of prostate cancer with PET. The goal of this study was to develop a dual-modality imaging probe that can be used for noninvasive PET imaging and optical imaging of prostate cancer. METHODS: We designed and synthesized an IRDye 650 and DOTA-conjugated GRPr antagonist, HZ220 (DOTA-Lys(IRDye 650)-PEG4-[D-Phe(6), Sta(13)]-BN(6-14)NH2), by reacting DOTA-Lys-PEG4-[D-Phe(6), Sta(13)]-BN(6-14)NH2 (HZ219) with IRDye 650 N-hydroxysuccinimide (NHS) ester...
January 2017: Journal of Nuclear Medicine: Official Publication, Society of Nuclear Medicine
https://www.readbyqxmd.com/read/27508030/hypothalamic-gastrin-releasing-peptide-receptor-mediates-an-antidepressant-like-effect-in-a-mouse-model-of-stress
#19
Lihua Yao, Jianxin Chen, Hexiang Chen, Dan Xiang, Can Yang, Ling Xiao, Wanhong Liu, Huiling Wang, Gaohua Wang, Fan Zhu, Zhongchun Liu
Evidence has shown that gastrin-releasing peptide receptor (GRPR) is involved in responses to stress and anxiety. The primary role of GRPR is to stimulate corticotrophin-releasing hormone (CRH) or adrenocorticotropic hormone (ACTH) secretion. Thus, the mechanisms of GRPR signaling should be elucidated to discover novel therapeutic targets for treating depression. This study aimed to investigate GRPR alterations in the C57 mouse hypothalamus after the animals were subjected to stress and fluoxetine treatments...
2016: American Journal of Translational Research
https://www.readbyqxmd.com/read/27497631/co-administration-of-succinylated-gelatine-with-a-99m-tc-bombesin-analogue-effects-on-pharmacokinetics-and-tumor-uptake
#20
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
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