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https://www.readbyqxmd.com/read/29721096/first-in-human-study-of-pet-and-optical-dual-modality-image-guided-surgery-in-glioblastoma-using-68-ga-irdye800cw-bbn
#1
Deling Li, Jingjing Zhang, Chongwei Chi, Xiong Xiao, Junmei Wang, Lixin Lang, Iqbal Ali, Gang Niu, Liwei Zhang, Jie Tian, Nan Ji, Zhaohui Zhu, Xiaoyuan Chen
Purpose : Despite the use of fluorescence-guided surgery (FGS), maximum safe resection of glioblastoma multiforme (GBM) remains a major challenge. It has restricted surgeons between preoperative diagnosis and intraoperative treatment. Currently, an integrated approach combining preoperative assessment with intraoperative guidance would be a significant step in this direction. Experimental design : We developed a novel 68 Ga-IRDye800CW-BBN PET/near-infrared fluorescence (NIRF) dual-modality imaging probe targeting gastrin-releasing peptide receptor (GRPR) in GBM...
2018: Theranostics
https://www.readbyqxmd.com/read/29669290/non-canonical-opioid-signaling-inhibits-itch-transmission-in-the-spinal-cord-of-mice
#2
Admire Munanairi, Xian-Yu Liu, Devin M Barry, Qianyi Yang, Jun-Bin Yin, Hua Jin, Hui Li, Qing-Tao Meng, Jia-Hang Peng, Zhen-Yu Wu, Jun Yin, Xuan-Yi Zhou, Li Wan, Ping Mo, Seungil Kim, Fu-Quan Huo, Joseph Jeffry, Yun-Qing Li, Rita Bardoni, Michael R Bruchas, Zhou-Feng Chen
Chronic itch or pruritus is a debilitating disorder that is refractory to conventional anti-histamine treatment. Kappa opioid receptor (KOR) agonists have been used to treat chronic itch, but the underlying mechanism remains elusive. Here, we find that KOR and gastrin-releasing peptide receptor (GRPR) overlap in the spinal cord, and KOR activation attenuated GRPR-mediated histamine-independent acute and chronic itch in mice. Notably, canonical KOR-mediated Gαi signaling is not required for desensitizing GRPR function...
April 17, 2018: Cell Reports
https://www.readbyqxmd.com/read/29664606/radiometal-dependent-biological-profile-of-the-radiolabeled-grpr-antagonist-sb3-in-cancer-theranostics-metabolic-and-biodistribution-patterns-defined-by-neprilysin
#3
Emmanouil Lymperis, Aikaterini Kaloudi, Werner Sallegger, Ingrid L Bakker, Eric P Krenning, Marion DeJong, Theodosia Maina, Berthold Artur Nock
Recent advances in oncology involve the use of diagnostic/therapeutic radionuclide-carrier pairs that target cancer cells, offering exciting opportunities for personalized patient treatment. Theranostic gastrin-releasing peptide receptor (GRPR)-directed radiopeptides have been proposed for the management of GRPR-expressing prostate and breast cancers. We have recently introduced the PET tracer 68Ga-SB3 (SB3, DOTA-p-aminomethylaniline-diglycolic acid-DPhe-Gln-Trp-Ala-Val-Gly-His-Leu-NHEt), a receptor-radioantagonist that enables the visualization of GRPR-positive lesions in human...
April 17, 2018: Bioconjugate Chemistry
https://www.readbyqxmd.com/read/29556947/in-vivo-stabilized-sb3-an-attractive-grpr-antagonist-for-pre-and-intra-operative-imaging-for-prostate-cancer
#4
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/29556030/circuit-dissection-of-the-role-of-somatostatin-in-itch-and-pain
#5
Jing Huang, Erika Polgár, Hans Jürgen Solinski, Santosh K Mishra, Pang-Yen Tseng, Noboru Iwagaki, Kieran A Boyle, Allen C Dickie, Mette C Kriegbaum, Hendrik Wildner, Hanns Ulrich Zeilhofer, Masahiko Watanabe, John S Riddell, Andrew J Todd, Mark A Hoon
Stimuli that elicit itch are detected by sensory neurons that innervate the skin. This information is processed by the spinal cord; however, the way in which this occurs is still poorly understood. Here we investigated the neuronal pathways for itch neurotransmission, particularly the contribution of the neuropeptide somatostatin. We find that in the periphery, somatostatin is exclusively expressed in Nppb+ neurons, and we demonstrate that Nppb+ somatostatin+ cells function as pruriceptors. Employing chemogenetics, pharmacology and cell-specific ablation methods, we demonstrate that somatostatin potentiates itch by inhibiting inhibitory dynorphin neurons, which results in disinhibition of GRPR+ neurons...
May 2018: Nature Neuroscience
https://www.readbyqxmd.com/read/29542916/gastrin-releasing-peptide-receptor-and-prostate-specific-membrane-antigen-specific-ultrasmall-gold-nanoparticles-for-characterization-and-diagnosis-of-prostate-carcinoma-via-fluorescence-imaging
#6
Marc Pretze, Andreas Hien, Matthias Rädle, Ralf Schirrmacher, Carmen Wängler, Björn Wängler
Gold nanoparticles (AuNPs) have widely been used for 70 years in cancer treatment, but only in the last 15 years has the focus been on specific AuNPs with homogeneous size and shape for various areas in science. They constitute a perfect platform for multifunctionalization and therefore enable the enhancement of target affinity. Here we report on the development of tumor specific AuNPs as diagnostic tools intended for the detection of prostate cancer via fluorescence imaging and positron emission tomography (PET)...
May 16, 2018: Bioconjugate Chemistry
https://www.readbyqxmd.com/read/29517903/new-gastrin-releasing-peptide-receptor-directed-99m-tc-demobesin-1-mimics-synthesis-and-comparative-evaluation
#7
Berthold A Nock, David Charalambidis, Werner Sallegger, Beatrice Waser, Rosalba Mansi, Guillaume P Nicolas, Eleni Ketani, Anastasia Nikolopoulou, Melpomeni Fani, Jean-Claude Reubi, Theodosia Maina
We have previously reported on the gastrin releasing peptide receptor (GRPR) antagonist [99m Tc]1, ([99m Tc]demobesin 1, 99m Tc-[N4 '-diglycolate-dPhe6 ,Leu-NHEt13 ]BBN(6-13)). [99m Tc]1 has shown superior biological profile compared to analogous agonist-based 99m Tc-radioligands. We herein present a small library of [99m Tc]1 mimics generated after structural modifications in (a) the linker ([99m Tc]2, [99m Tc]3, [99m Tc]4), (b) the peptide chain ([99m Tc]5, [99m Tc]6), and (c) the C-terminus ([99m Tc]7 or [99m Tc]8)...
April 12, 2018: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29464003/-68-ga-bbn-rgd-pet-ct-for-grpr-and-integrin-%C3%AE-v-%C3%AE-3-imaging-in-patients-with-breast-cancer
#8
Jingjing Zhang, Feng Mao, Gang Niu, Li Peng, Lixin Lang, Fang Li, Hongyan Ying, Huanwen Wu, Boju Pan, Zhaohui Zhu, Xiaoyuan Chen
Purpose: This study was to assess a gastrin-releasing peptide receptor (GRPR) and integrin αvβ3 dual targeting tracer 68 Ga-BBN-RGD for positron emission tomography (PET)/computed tomography (CT) imaging of breast cancer and metastasis. Materials and Methods: Twenty-two female patients were recruited either with suspected breast cancer on screening mammography (n = 16) or underwent breast cancer radical mastectomy (n = 6). All the 22 patients underwent PET/CT at 30-45 min after intravenous injection of 68 Ga-BBN-RGD...
2018: Theranostics
https://www.readbyqxmd.com/read/29463009/docosahexaenoic-acid-helps-to-lessen-extinction-memory-in-rats
#9
Michio Hashimoto, Shahdat Hossain, Masanori Katakura, Abdullah Al Mamun, Osamu Shido
Abstract : Memory extinction is referred to as a learning process in which a conditioned response (CR) progressively reduces over time as an animal learns to uncouple a response from a stimulus. Extinction occurs when the rat is placed into a context without shock after training. Docosahexaenoic acid (DHA, C22:6, n-3) is implicated in memory formation in mammalian brains. In a two-way active shuttle-avoidance apparatus, we examined whether DHA affects the extinction memory and the expression of brain cognition-related proteins, including gastrin-releasing peptide receptor (GRPR), brain-derived neurotrophic factor receptor (BDNFR) tyrosine kinase receptor B (TrKB), and N-methyl-d-aspartate receptor (NMDAR) subunits NR2A and NR2B...
February 18, 2018: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
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
#10
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
#11
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/29154145/evaluation-of-a-novel-grpr-antagonist-for-prostate-cancer-pet-imaging-64-cu-dotha-2-peg-rm26
#12
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/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
#13
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
#14
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-68ga-rm26-in-healthy-volunteers-and-prostate-cancer-patients
#15
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 68Ga-RM26, to assess its clinical diagnostic value in prostate cancer patients, and to perform a direct comparison between GRPR antagonist 68Ga-RM26 and agonist 68Ga-BBN. Methods: Five healthy volunteers were enrolled to validate the safety of 68Ga-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
#16
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...
February 2018: 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
#17
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
#18
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
#19
Andrei Iagaru
No abstract text is available yet for this article.
December 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
#20
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)...
January 2018: Peptides
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