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https://www.readbyqxmd.com/read/29137110/neobomb1-a-grpr-antagonist-for-breast-cancer-theragnostics-first-results-of-a-preclinical-study-with-67-ga-neobomb1-in-t-47d-cells-and-tumor-bearing-mice
#1
Aikaterini Kaloudi, Emmanouil Lymperis, Athina Giarika, Simone Dalm, Francesca Orlandi, Donato Barbato, Mattia Tedesco, Theodosia Maina, Marion de Jong, Berthold A Nock
The GRPR-antagonist-based radioligands [(67/68)Ga/(111)In/(177)Lu]NeoBOMB1 have shown excellent theragnostic profiles in preclinical prostate cancer models, while [(68)Ga]NeoBOMB1 effectively visualized prostate cancer lesions in patients. We were further interested to explore the theragnostic potential of NeoBOMB1 in GRPR-positive mammary carcinoma, by first studying [(67)Ga]NeoBOMB1 in breast cancer models; Methods: We investigated the profile of [(67)Ga]NeoBOMB1, a [(68)Ga]NeoBOMB1 surrogate, in GRPR-expressing T-47D cells and animal models; Results: NeoBOMB1 (IC50s of 2...
November 11, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/29133874/distinct-roles-of-nmb-and-grp-in-itch-transmission
#2
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
https://www.readbyqxmd.com/read/29123014/positron-emission-tomography-using-a-grpr-antagonist-68-ga-rm26-in-healthy-volunteers-and-prostate-cancer-patients
#3
Jingjing Zhang, Gang Niu, Xingrong Fan, Lixin Lang, Guozhu Hou, Libo Chen, Huanwen Wu, Zhaohui Zhu, Fang Li, Xiaoyuan Chen
This study was designed to study the safety, biodistribution, radiation dosimetry of a gastrin-releasing peptide receptor (GRPR) antagonist positron emission tomography (PET) tracer (68)Ga-RM26, to assess its clinical diagnostic value in prostate cancer patients, and to perform a direct comparison between GRPR antagonist (68)Ga-RM26 and agonist (68)Ga-BBN. Methods: Five healthy volunteers were enrolled to validate the safety of (68)Ga-RM26 and calculate dosimetry. A total of 28 patients with prostate cancer (17 newly diagnosed and 11 post therapy) were recruited with written informed consent...
November 9, 2017: Journal of Nuclear Medicine: Official Publication, Society of Nuclear Medicine
https://www.readbyqxmd.com/read/29120926/recent-insights-into-biological-functions-of-mammalian-bombesin-like-peptides-and-their-receptors
#4
Xiangping Qu, Hui Wang, Rujiao Liu
PURPOSE OF REVIEW: The current review highlights recent advances in physiological and pharmacological researches in biology of mammalian bombesin-like peptides (BLPs). RECENT FINDINGS: BLPs and their receptors were found to have regulatory roles in many biological processes in central nervous system. Two BLPs, neuromedin B and gastrin-releasing peptide (GRP), and their receptors are required for regulation of basal and induced sighing activity in rodents. This is the first study demonstrating central pathways involved in regulation of sighing activity...
November 7, 2017: Current Opinion in Endocrinology, Diabetes, and Obesity
https://www.readbyqxmd.com/read/29097932/high-contrast-pet-imaging-of-grpr-expression-in-prostate-cancer-using-cobalt-labeled-bombesin-antagonist-rm26
#5
Bogdan Mitran, Helge Thisgaard, Ulrika Rosenström, Johan Hygum Dam, Mats Larhed, Vladimir Tolmachev, Anna Orlova
High gastrin releasing peptide receptor (GRPR) expression is associated with numerous cancers including prostate and breast cancer. The aim of the current study was to develop a (55)Co-labeled PET agent based on GRPR antagonist RM26 for visualization of GRPR-expressing tumors. Labeling with (57)Co and (55)Co, stability, binding specificity, and in vitro and in vivo characteristics of (57)Co-NOTA-PEG2-RM26 were studied. NOTA-PEG2-RM26 was successfully radiolabeled with (57)Co and (55)Co with high yields and demonstrated high stability...
2017: Contrast Media & Molecular Imaging
https://www.readbyqxmd.com/read/28977997/expression-of-hypothalamic-neurohormones-and-their-receptors-in-the-human-eye
#6
Sander R Dubovy, Maria P Fernandez, Jose J Echegaray, Norman L Block, Noriyuki Unoki, Roberto Perez, Irving Vidaurre, Richard K Lee, Mehrdad Nadji, Andrew V Schally
Extrapituitary roles for hypothalamic neurohormones have recently become apparent and clinically relevant, based on the use of synthetic peptide analogs for the treatment of multiple conditions including cancers, pulmonary edema and myocardial infarction. In the eye, it has been suggested that some of these hormones and their receptors may be present in the ciliary body, iris, trabecular meshwork and retina, but their physiological role has yet to be elucidated. Our study intends to comprehensively demonstrate the expression of some hypothalamic neuroendocrine hormones and their receptors within different retinal and extraretinal structures of the human eye...
September 15, 2017: Oncotarget
https://www.readbyqxmd.com/read/28970333/will-grpr-compete-with-psma-as-a-target-in-prostate-cancer
#7
Andrei Iagaru
No abstract text is available yet for this article.
September 28, 2017: Journal of Nuclear Medicine: Official Publication, Society of Nuclear Medicine
https://www.readbyqxmd.com/read/28966141/distribution-of-the-pig-gastrin-releasing-peptide-receptor-and-the-effect-of-grp-on-porcine-leydig-cells
#8
Zhiyu Ma, Ying Zhang, Juan Su, Xiang Li, Sheng Yang, Wenna Qiao, Chuan Suo, Zhihai Lei
Gastrin-releasing peptide (GRP) is a mammalian bombesin (BN)-like peptide which plays a role in a number of important physiological functions via its receptor (gastrin-releasing peptide receptor, GRPR) in most animals. However, little is known about the gene encoding GRPR and its functions (especially reproduction) in pigs. In this study, we first cloned and analyzed the pig GRPR cDNA. Then we systematically investigated the expression levels of GRPR mRNA by relative real-time PCR (RT-PCR), and analyzed the distribution of the GRPR protein in pig tissues via immunohistochemistry (IHC)...
September 28, 2017: Peptides
https://www.readbyqxmd.com/read/28957638/augmented-responses-to-ozone-in-obese-mice-require-il-17a-and-gastrin-releasing-peptide
#9
Joel A Mathews, Nandini Krishnamoorthy, David I Kasahara, John Hutchinson, Youngji Cho, Jeffrey D Brand, Alison S Williams, Allison P Wurmbrand, Luiza Ribeiro, Frank Cuttitta, Mary E Sunday, Bruce D Levy, Stephanie A Shore
Ozone and obesity both increase IL-17A in the lungs. In mice, obesity augments the airway hyperresponsiveness and neutrophil recruitment induced by acute ozone exposure. Therefore, we examined the role of IL-17A in obesity-related increases in the response to ozone observed in obese mice. Lean wildtype and obese db/db mice were pretreated with IL-17A blocking or isotype antibodies, exposed to air or ozone (2 ppm for 3 h), and evaluated 24 h later. Microarray analysis of lung tissue gene expression was used to examine the mechanistic basis for effects of anti-IL-17A...
September 28, 2017: American Journal of Respiratory Cell and Molecular Biology
https://www.readbyqxmd.com/read/28761146/how-gastrin-releasing-peptide-receptor-grpr-and-%C3%AE-v%C3%AE-3-integrin-expression-reflect-reorganization-features-of-tumors-after-hyperthermia-treatments
#10
Sandra Hallasch, Sindy Frick, Maximilian Jung, Ingrid Hilger
The outcome of tumor treatment via hyperthermia in the clinic has been reported to be heterogeneous. Here, we assessed how the presence of gastrin-releasing peptide receptor (GRPR) and αvβ3 integrin together with the morphology of the vascularization reflects the growth behavior of tumors after hyperthermia treatment. MDA-MB-231 tumor bearing mice were treated either with high (46 °C) or low dose (42 °C) water hyperthermia for 60 min. Changes of GRPR and αvβ3 integrin expression were assessed via multiplexed optical imaging...
July 31, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28733141/gastrin-releasing-peptide-and-its-receptor-increase-arthritis-fibroblast-like-synoviocytes-invasiveness-through-activating-the-pi3k-akt-pathway
#11
Vanessa Schuck Clarimundo, Mirian Farinon, Renata Ternus Pedó, Vivian Oliveira Nunes Teixeira, Carolina Nör, Percio S Gulko, Ricardo Machado Xavier, Patricia Gnieslaw de Oliveira
Rheumatoid arthritis (RA) is an autoimmune disease that leads to joint destruction. The fibroblast-like synoviocytes (FLS) has a central role on the disease pathophysiology. The present study aimed to examine the role of gastrin-releasing peptide (GRP) and its receptor (GRPR) on invasive behavior of mice fibroblast-like synoviocytes (FLS), as well as to evaluate GRP-induced signaling on PI3K/AKT pathway. The expression of GRPR in FLS was investigated by immunocytochemistry, western blot (WB) and qRT-PCR. The proliferation and invasion were assessed by SRB and matrigel-transwell assay after treatment with GRP and/or RC-3095 (GRPR antagonist), and/or Ly294002 (inhibitor of PI3K/AKT pathway)...
July 18, 2017: Peptides
https://www.readbyqxmd.com/read/28636973/amide-to-triazole-switch-vs-in-vivo-nep-inhibition-approaches-to-promote-radiopeptide-targeting-of-grpr-positive-tumors
#12
Theodosia Maina, Aikaterini Kaloudi, Ibai E Valverde, Thomas L Mindt, Berthold A Nock
INTRODUCTION: Radiolabeled bombesin (BBN)-analogs have been proposed for diagnosis and therapy of gastrin-releasing peptide receptor (GRPR)-expressing tumors, such as prostate, breast and lung cancer. Metabolic stability represents a crucial factor for the success of this approach by ensuring sufficient delivery of circulating radioligand to tumor sites. The amide-to-triazole switch on the backbone of DOTA-PEG4-[Nle(14)]BBN(7-14) (1) was reported to improve the in vitro stability of resulting (177)Lu-radioligands...
September 2017: Nuclear Medicine and Biology
https://www.readbyqxmd.com/read/28621684/expression-of-hypothalamic-neurohormones-and-their-receptors-in-the-human-eye
#13
Sander R Dubovy, Maria P Fernandez, Jose J Echegaray, Norman L Block, Noriyuki Unoki, Roberto Perez, Irving Vidaurre, Richard K Lee, Mehrdad Nadji, Andrew V Schally
Extrapituitary roles for hypothalamic neurohormones have recently become apparent and clinically relevant, based on the use of synthetic peptide analogs for the treatment of multiple conditions including cancers, pulmonary edema and myocardial infarction. In the eye, it has been suggested that some of these hormones and their receptors may be present in the ciliary body, iris, trabecular meshwork and retina, but their physiological role has yet to be elucidated. Our study intends to comprehensively demonstrate the expression of some hypothalamic neuroendocrine hormones and their receptors within different retinal and extraretinal structures of the human eye...
June 3, 2017: Oncotarget
https://www.readbyqxmd.com/read/28576168/theranostic-prospects-of-gastrin-releasing-peptide-receptor-radioantagonists-in-oncology
#14
REVIEW
Theodosia Maina, Berthold A Nock, Harshad Kulkarni, Aviral Singh, Richard P Baum
Gastrin-releasing peptide receptors (GRPRs) represent attractive targets for cancer diagnosis and therapy owing to their overexpression in widespread human tumors. Bombesin (BBN) analogues coupled to suitable chelators for stable radiometal binding have been proposed for diagnostic imaging and radionuclide therapy (theranostics) of GRPR-positive tumors. Recently, interest has shifted from BBN-like receptor agonists to GRPR-radioantagonists, because radioantagonists do not induce adverse effects after injection to patients and display superior pharmacokinetic in vivo profiles...
July 2017: PET Clinics
https://www.readbyqxmd.com/read/28500250/characterization-of-nmb-grp-and-their-receptors-brs3-nmbr-and-grpr-in-chickens
#15
Chunheng Mo, Long Huang, Lin Cui, Can Lv, Dongliang Lin, Liang Song, Guoqiang Zhu, Juan Li, Yajun Wang
The two structurally and functionally related peptides, gastrin-releasing peptide (GRP) and neuromedin B (NMB) play critical roles in many physiological/pathological processes in mammals. However, the information regarding the expression and functionality of avian NMB, GRP, and their receptors is limited. Here, we characterized cNMB, cGRP and their receptors (cNMBR, cGRPR, cBRS3) in chickens. Our results showed that: 1) cNMBR and cGRPR expressed in CHO cells could be potently activated by cNMB and cGRP respectively, as monitored by cell-based luciferase reporter assays, indicating that cNMBR and cGRPR are cNMB- and cGRP-specific receptors; Strikingly, BRS3 of chickens (/spotted gars), which is orthologous to mouse bombesin receptor subtype-3 (BRS3), could be potently activated by GRP and NMB, demonstrating that both peptides are the endogenous ligands for chicken(/spotted gar) BRS3; 2) Quantitative real-time PCR revealed that cGRPR is widely expressed in chicken tissues with abundant expression in the ovary, pancreas, proventriculus, spinal cord and brain, whereas cNMB, cNMBR and cBRS3 are mainly expressed in the brain and testes; 3) Interestingly, qPCR, Western blot, and immuno-staining revealed that cGRP is predominantly expressed in the anterior pituitary and mainly localized to LH-cells, suggesting that cGRP is likely a novel pituitary hormone in chickens...
May 12, 2017: Journal of Molecular Endocrinology
https://www.readbyqxmd.com/read/28489853/novel-genes-involved-in-severe-early-onset-obesity-revealed-by-rare-copy-number-and-sequence-variants
#16
Clara Serra-Juhé, Gabriel Á Martos-Moreno, Francesc Bou de Pieri, Raquel Flores, Juan R González, Benjamín Rodríguez-Santiago, Jesús Argente, Luis A Pérez-Jurado
Obesity is a multifactorial disorder with high heritability (50-75%), which is probably higher in early-onset and severe cases. Although rare monogenic forms and several genes and regions of susceptibility, including copy number variants (CNVs), have been described, the genetic causes underlying the disease still remain largely unknown. We searched for rare CNVs (>100kb in size, altering genes and present in <1/2000 population controls) in 157 Spanish children with non-syndromic early-onset obesity (EOO: body mass index >3 standard deviations above the mean at <3 years of age) using SNP array molecular karyotypes...
May 2017: PLoS Genetics
https://www.readbyqxmd.com/read/28485418/in-vitro-in-vivo-peeling-of-multilayered-aminocarboxylate-gold-nanoparticles-evidenced-by-a-kinetically-stable-99m-tc-label
#17
Francisco Silva, Lurdes Gano, Maria Paula Cabral Campello, Rosa Marques, Isabel Prudêncio, Ajit Zambre, Anandhi Upendran, António Paulo, Raghuraman Kannan
A thiolated bombesin peptide was conjugated to Au-DTDTPA nanoconstructs to obtain BBN-Au-DTDTPA targeted to the gastrin releasing peptide receptor (GRPr). Different analytical techniques showed that this conjugate shares similar physico-chemical properties with Au-DTDTPA; HPLC and XPS analyses corroborated the attachment of the bioactive peptide to the AuNPs surface. Competitive binding assays in PC3 cancer cells showed that these BBN-containing AuNPs have high affinity for GRPr. BBN-Au-DTDTPA was successfully radiolabeled with (99m)Tc and showed high in vitro stability towards different biological media and substrates, except for glutathione (GSH)...
October 31, 2017: Dalton Transactions: An International Journal of Inorganic Chemistry
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
#18
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...
August 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
#19
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 CXC chemokine receptor 2 (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...
April 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
#20
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
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