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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
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
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
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
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
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
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
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
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
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
Berthold A Nock, Aikaterini Kaloudi, Emmanouil Lymperis, Athina Giarika, Harshad R Kulkarni, Ingo Klette, Aviral Singh, Eric P Krenning, Marion de Jong, Theodosia Maina, Richard P Baum
: We recently introduced the potent gastrin-releasing peptide receptor (GRPR) antagonist (68)Ga-SB3 ((68)Ga-DOTA-p-aminomethylaniline-diglycolic acid-DPhe-Gln-Trp-Ala-Val-Gly-His-Leu-NHEt), showing excellent tumor localizing efficacy in animal models and in patients. By replacement of the C-terminal Leu(13)-Met(14)-NH2 dipeptide of SB3 by Sta(13)-Leu(14)-NH2, the novel GRPR antagonist NeoBOMB1 was generated and labeled with different radiometals for theranostic use. We herein report on the biologic profile of resulting (67/68)Ga-, (111)In-, and (177)Lu-NeoBOMB1 radioligands in GRPR-expressing cells and mouse models...
January 2017: Journal of Nuclear Medicine: Official Publication, Society of Nuclear Medicine
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
Christian Stoykow, Thalia Erbes, Helmut R Maecke, Stefan Bulla, Mark Bartholomä, Sebastian Mayer, Vanessa Drendel, Peter Bronsert, Martin Werner, Gerald Gitsch, Wolfgang A Weber, Elmar Stickeler, Philipp T Meyer
INTRODUCTION: The gastrin-releasing peptide receptor (GRPR) is overexpressed in breast cancer. The present study evaluates GRPR imaging as a novel imaging modality in breast cancer by employing positron emission tomography (PET) and the GRPR antagonist (68)Ga-RM2. METHODS: Fifteen female patients with biopsy confirmed primary breast carcinoma (3 bilateral tumors; median clinical stage IIB) underwent (68)Ga-RM2-PET/CT for pretreatment staging. In vivo tumor uptake of (68)Ga-RM2 was correlated with estrogen (ER) and progesterone (PR) receptor expression, HER2/neu status and MIB-1 proliferation index in breast core biopsy specimens...
2016: Theranostics
Yao Sun, Xiaowei Ma, Zhe Zhang, Ziyan Sun, Mathias Loft, Bingbing Ding, Changhao Liu, Liying Xu, Meng Yang, Yuxin Jiang, Jianfeng Liu, Yuling Xiao, Zhen Cheng, Xuechuan Hong
Gastrin-releasing peptide receptor (GRPR) targeted positron emission tomography (PET) is a highly promising approach for imaging of prostate cancer (PCa) in small animal models and patients. Developing a GRPR-targeted PET probe with excellent in vivo performance such as high tumor uptake, high contrast, and optimal pharmacokinetics is still very challenging. Herein, a novel bombesin (BBN) analogue (named SCH1) based on JMV594 peptide modified with an 8-amino octanoic acid spacer (AOC) was thus designed and conjugated with the metal chelator 1,4,7-triazacyclononane,1-glutaric acid-4,7-acetic acid (NODAGA)...
August 17, 2016: Bioconjugate Chemistry
Christos Liolios, Martin Schäfer, Uwe Haberkorn, Matthias Eder, Klaus Kopka
No abstract text is available yet for this article.
July 20, 2016: Bioconjugate Chemistry
Fumiya Kusube, Mitsutoshi Tominaga, Hiroaki Kawasaki, Fumiyuki Yamakura, Hisashi Naito, Hideoki Ogawa, Yasuhiro Tomooka, Kenji Takamori
Spinal itch transmission has been reported to be mediated by at least two neuronal populations in spinal dorsal horn, neurons expressing brain-natriuretic peptide (BNP) receptor (Npra) and gastrin-releasing peptide (GRP) receptor (GRPR). Although Npra-expressing neurons were shown to be upstream of GRPR- expressing neurons in spinal itch transmission, the roles of BNP and GRP in the spinal neurotransmission of histamine-dependent and -independent itch remains unclear. Using in vivo electrophysiology and behavior analysis, this study examined the responses of chloroquine (histamine-independent pruritogen)-responsive and histamine-responsive dorsal horn neurons to spinal applications of BNP and GRP...
August 3, 2016: Neuroscience Letters
Yonglin Yu, Lingtong Zhi, Qiuli Wu, Lina Jing, Dayong Wang
npr-9 encodes a homologue of the gastrin-releasing peptide receptor (GRPR) and is expressed in AIB interneurons. In this study, we investigated the role of NPR-9 in the neuronal control of innate immunity using the model system Caenorhabditis elegans. After exposure to Pseudomonas aeruginosa PA14, npr-9(tm1652) mutants showed resistance to infection, decreased PA14 colonization and increased expression of immunity-related genes. Nematodes overexpressing NPR-9 exhibited increased susceptibility to infection, increased PA14 colonization and reduced expression of immunity-related genes...
May 2, 2016: Cellular & Molecular Immunology
Fan Pu, Shenghui Xue, Jenny J Yang
No abstract text is available yet for this article.
May 2016: Biomarkers in Medicine
Devin M Barry, Hui Li, Xian-Yu Liu, Kai-Feng Shen, Xue-Ting Liu, Zhen-Yu Wu, Admire Munanairi, Xiao-Jun Chen, Jun Yin, Yan-Gang Sun, Yun-Qing Li, Zhou-Feng Chen
There are substantial disagreements about the expression of gastrin-releasing peptide (GRP) in sensory neurons and whether GRP antibody cross-reacts with substance P (SP). These concerns necessitate a critical revaluation of GRP expression using additional approaches. Here, we show that a widely used GRP antibody specifically recognizes GRP but not SP. In the spinal cord of mice lacking SP (Tac1KO), the expression of not only GRP but also other peptides, notably neuropeptide Y (NPY), is significantly diminished...
2016: Molecular Pain
Ibai E Valverde, Sandra Vomstein, Thomas L Mindt
The peptide bombesin (BBN) is a peptide with high affinity for the gastrin-releasing peptide receptor (GRPr), a receptor that is overexpressed by, for example, breast and prostate cancers. Thus, GRPr agonists can be used as cancer-targeting vectors to shuttle diagnostic and therapeutic agents into tumor cells. With the aim of optimizing the tumor targeting properties of a radiolabeled [Nle(14)]BBN(7-14) moiety, novel BBN(7-14)- and BBN(6-14)-based radioconjugates were synthesized, labeled with Lu-177, and fully evaluated in vitro and in vivo...
April 28, 2016: Journal of Medicinal Chemistry
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