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https://www.readbyqxmd.com/read/29154145/evaluation-of-a-novel-grpr-antagonist-for-prostate-cancer-pet-imaging-64-cu-dotha2-peg-rm26
#1
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-Phe(6)-Sta(13)-Leu(14)-NH2]bombesin(6-14) (DOTHA2-PEG-RM26) to visualize prostate tumors by PET imaging...
October 23, 2017: Nuclear Medicine and Biology
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/29120926/recent-insights-into-biological-functions-of-mammalian-bombesin-like-peptides-and-their-receptors
#3
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/29107299/bombesin-like-receptor-3-brs3-expression-in-glutamatergic-but-not-gabaergic-neurons-is-required-for-regulation-of-energy-metabolism
#4
Cuiying Xiao, Ramón A Piñol, Jesse Lea Carlin, Cuiling Li, Chuxia Deng, Oksana Gavrilova, Marc L Reitman
OBJECTIVE: Bombesin-like receptor 3 (BRS-3) is an orphan G protein-coupled receptor. Brs3 null mice have reduced resting metabolic rate and body temperature, increased food intake, and obesity. Here we study the role of Brs3 in different neuron types. METHODS: Mice able to undergo Cre recombinase-dependent inactivation or re-expression of Brs3 were generated, respectively Brs3(fl/y) and Brs3(loxTB/y). We then studied four groups of mice with Brs3 selectively inactivated or re-expressed in cells expressing Vglut2-Cre or Vgat-Cre...
November 2017: Molecular Metabolism
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/29065544/pharmacological-effects-of-two-novel-bombesin-like-peptides-from-the-skin-secretions-of-chinese-piebald-odorous-frog-odorrana-schmackeri-and-european-edible-frog-pelophylax-kl-esculentus-on-smooth-muscle
#6
Xiaowei Zhou, Chengbang Ma, Mei Zhou, Yuning Zhang, Xinping Xi, Ruimin Zhong, Tianbao Chen, Chris Shaw, Lei Wang
Bombesin-like peptides, which were identified from a diversity of amphibian skin secretions, have been demonstrated to possess several biological functions such as stimulation of smooth muscle contraction and regulation of food intake. Here, we report two novel bombesin-like peptides, bombesin-OS and bombesin-PE, which were isolated from Odorrana schmackeri and Pelophylax kl. esculentus, respectively. The mature peptides were identified and structurally confirmed by high performance Scliquid chromatography (HPLC) and tandem mass spectrometry (MS/MS)...
October 23, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28979118/gastrin-releasing-peptide-receptor-targeted-gadolinium-oxide-based-multifunctional-nanoparticles-for-dual-magnetic-resonance-fluorescent-molecular-imaging-of-prostate-cancer
#7
Danting Cui, Xiaodan Lu, Chenggong Yan, Xiang Liu, Meirong Hou, Qi Xia, Yikai Xu, Ruiyuan Liu
Bombesin (BBN), an analog of gastrin-releasing peptide (GRP), specifically binds to GRP receptors, which are overexpressed in human prostate cancer (PC). Here, we synthesized a BBN-modified gadolinium oxide (Gd2O3) nanoprobe containing fluorescein (Gd2O3-5(6)-carboxyfluorescein [FI]-polyethylene glycol [PEG]-BBN) for targeted magnetic resonance (MR)/optical dual-modality imaging of PC. The Gd2O3-FI-PEG-BBN nanoparticles exhibited a relatively uniform particle size with an average diameter of 52.3 nm and spherical morphology as depicted by transmission electron microscopy...
2017: International Journal of Nanomedicine
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/28792505/fluorescence-imaging-of-bombesin-and-transferrin-receptor-expression-is-comparable-to-18f-fdg-pet-in-early-detection-of-sorafenib-induced-changes-in-tumor-metabolism
#9
COMPARATIVE STUDY
Jen-Chieh Tseng, Nara Narayanan, Guojie Ho, Kevin Groves, Jeannine Delaney, Bagna Bao, Jun Zhang, Jeffrey Morin, Sylvie Kossodo, Milind Rajopadhye, Jeffrey D Peterson
Physical measurement of tumor volume reduction is the most commonly used approach to assess tumor progression and treatment efficacy in mouse tumor models. However, it is relatively insensitive, and often requires long treatment courses to achieve gross physical tumor destruction. As alternatives, several non-invasive imaging methods such as bioluminescence imaging (BLI), fluorescence imaging (FLI) and positron emission tomography (PET) have been developed for more accurate measurement. As tumors have elevated glucose metabolism, 18F-fludeoxyglucose (18F-FDG) has become a sensitive PET imaging tracer for cancer detection, diagnosis, and efficacy assessment by measuring alterations in glucose metabolism...
2017: PloS One
https://www.readbyqxmd.com/read/28780306/neuromedin-b-and-its-receptor-silencing-suppresses-osteoclast-generation-by-modulating-precursor-proliferation-via-m-csf-c-fms-d-type-cyclins
#10
Chae-Eun Yeo, Woo Youl Kang, Sook Jin Seong, Seungil Cho, Hae Won Lee, Young-Ran Yoon, Hyun-Ju Kim
Neuromedin B (NMB), a mammalian bombesin-like peptide, regulates diverse physiological processes, such as energy metabolism, memory and fear behavior, and cellular growth, through its cognate receptor, NMBR. In this study, we report that NMB expression was upregulated during osteoclast development and that silencing NMB or NMBR attenuated osteoclast generation mediated by macrophage colony-stimulating factor (M-CSF) and receptor activator of NF-κB ligand (RANKL). We found that knockdown of NMB or NMBR using a small hairpin RNA suppressed M-CSF-induced proliferation of osteoclast precursor cells without altering osteoclast differentiation...
October 1, 2017: Experimental Cell Research
https://www.readbyqxmd.com/read/28767081/new-insights-in-the-design-of-bioactive-peptides-and-chelating-agents-for-imaging-and-therapy-in-oncology
#11
REVIEW
Anna Lucia Tornesello, Luigi Buonaguro, Maria Lina Tornesello, Franco Maria Buonaguro
Many synthetic peptides have been developed for diagnosis and therapy of human cancers based on their ability to target specific receptors on cancer cell surface or to penetrate the cell membrane. Chemical modifications of amino acid chains have significantly improved the biological activity, the stability and efficacy of peptide analogues currently employed as anticancer drugs or as molecular imaging tracers. The stability of somatostatin, integrins and bombesin analogues in the human body have been significantly increased by cyclization and/or insertion of non-natural amino acids in the peptide sequences...
August 2, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28745296/bbn-conjugated-gnps-a-new-targeting-contrast-agent-for-imaging-of-breast-cancer-in-radiology
#12
Mojtaba Salouti, Faranak Saghatchi
Using of targeted contrast agents in X-ray imaging of breast cancer can improve the accuracy of diagnosis, staging, and treatment planning by providing early detection and superior definition of tumour volume. This study demonstrates a new class of X-ray contrast agents based on gold nanoparticles (GNPs) and bombesin (BBN) for imaging of breast cancer in radiology. GNPs were synthesised in spherical shape in the size range of 15 ± 2 nm and conjugated with BBN followed by coating with polyethyleneglycol (PEG)...
August 2017: IET Nanobiotechnology
https://www.readbyqxmd.com/read/28727978/pulmonary-neuroendocrine-cell-hyperplasia-in-hemoglobin-bart-induced-hydrops-fetalis-a-model-for-chronic-intrauterine-hypoxia
#13
Mana Taweevisit, Boochit Theerasantipong, Kanlaya Taothong, Paul Scott Thorner
The pulmonary neuroendocrine system includes pulmonary neuroendocrine cells (PNECs) and neuroepithelial bodies (NEBs) that are distributed throughout respiratory epithelium and regulate lung growth and maturation antenatally. Abnormalities in this system have been linked to many hypoxia-associated pediatric pulmonary disorders. Hemoglobin (Hb) Bart disease is a severe form of α-thalassemia resulting in marked intrauterine hypoxia with hydrops fetalis (HF) and usually death in utero. Affected fetuses can serve as a naturally occurring human model for the effects of intrauterine hypoxia, and we postulated that these effects should include changes in the pulmonary neuroendocrine system...
July 2017: Pediatric and Developmental Pathology
https://www.readbyqxmd.com/read/28725583/positron-emission-tomography-pet-in-primary-prostate-cancer-staging-and-risk-assessment
#14
REVIEW
Sandra Bednarova, Maria L Lindenberg, Maria Vinsensia, Chiara Zuiani, Peter L Choyke, Baris Turkbey
Prostate cancer (PCa) is one of the few neoplasms that are not well served by 18F-Fluorodeoxyglucose (FDG) positron emission tomography (PET). As a result, a number of PET tracers have been developed to target particular biological features of PCa. Such agents can be used for diagnosis, staging, identification of biochemical recurrence (BCR) and evaluation of metastatic disease. Here, we focus on primary disease and local staging. To date, magnetic resonance imaging (MRI) has proven superior to PET in the imaging of primary PCa...
June 2017: Translational Andrology and Urology
https://www.readbyqxmd.com/read/28711565/new-aspects-of-molecular-imaging-in-prostate-cancer
#15
REVIEW
Francesco Ceci, Paolo Castellucci, Juliano J Cerci, Stefano Fanti
Nowadays several new imaging modalities are available for investigating prostate cancer (PCa) such as magnet resonance imaging (MRI) in the form of whole body MRI and pelvic multiparametric MRI and positron emission tomography (PET) using choline as radiotracers. Nevertheless, these modalities proved sub-optimal accuracy for detecting PCa metastases, particularly in the recurrence setting. A new molecular probe targeting the prostate specific membrane antigen (PSMA) has been recently developed for PET imaging...
November 1, 2017: Methods: a Companion to Methods in Enzymology
https://www.readbyqxmd.com/read/28677620/ranatensin-hl-a-bombesin-related-tridecapeptide-from-the-skin-secretion-of-the-broad-folded-frog-hylarana-latouchii
#16
Yan Lin, Tianbao Chen, Mei Zhou, Lei Wang, Songkun Su, Chris Shaw
Bombesin-related peptides are a family of peptides whose prototype was discovered in amphibian skin and which exhibit a wide range of biological activities. Since the initial isolation of bombesin from Bombina bombina skin, diverse forms of bombesin-related peptides have been found in the skins across Anura. In this study, a novel bombesin-related peptide of the ranatensin subfamily, named ranatensin-HL, was structurally-characterised from the skin secretion of the broad-folded frog, Hylarana latouchii, through combination of molecular cloning and mass spectrometric methodologies...
July 4, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28675470/brain-serotoninergic-nervous-system-is-involved-in-bombesin-induced-frequent-urination-through-brain-5-ht7-receptors-in-rats
#17
Takahiro Shimizu, Shogo Shimizu, Naoki Wada, Shun Takai, Nobutaka Shimizu, Youichirou Higashi, Katsumi Kadekawa, Tsuyoshi Majima, Motoaki Saito, Naoki Yoshimura
BACKGROUND AND PURPOSE: Psychological stress exacerbates symptoms of urinary bladder dysfunction; however, the underlying brain mechanisms are unclear. We have demonstrated that centrally administered bombesin, a stress-related neuropeptide, facilitates the rat micturition reflex. Brain bombesin-like peptides modulate the serotoninergic nervous system activity under stress conditions; therefore, we examined whether brain 5-HT is involved in the bombesin-induced increased frequency of urination in urethane-anaesthetised male Sprague-Dawley rats...
September 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28654384/fluorescent-plasmonic-and-radiotherapeutic-properties-of-the-177-lu-dendrimer-aunp-folate-bombesin-nanoprobe-located-inside-cancer-cells
#18
Héctor Mendoza-Nava, Guillermina Ferro-Flores, Flor de María Ramírez, Blanca Ocampo-García, Clara Santos-Cuevas, Erika Azorín-Vega, Nallely Jiménez-Mancilla, Myrna Luna-Gutiérrez, Keila Isaac-Olivé
The integration of fluorescence and plasmonic properties into one molecule is of importance in developing multifunctional imaging and therapy nanoprobes. The aim of this research was to evaluate the fluorescent properties and the plasmonic-photothermal, therapeutic, and radiotherapeutic potential of (177)Lu-dendrimer conjugated to folate and bombesin with gold nanoparticles in the dendritic cavity ((177)Lu-DenAuNP-folate-bombesin) when it is internalized in T47D breast cancer cells. The intense near-Infrared (NIR) fluorescence emitted at 825 nm from the conjugate inside cells corroborated the usefulness of DenAuNP-folate-bombesin for optical imaging...
January 1, 2017: Molecular Imaging
https://www.readbyqxmd.com/read/28636973/amide-to-triazole-switch-vs-in-vivo-nep-inhibition-approaches-to-promote-radiopeptide-targeting-of-grpr-positive-tumors
#19
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/28622690/exploiting-cancer-s-phenotypic-guise-against-itself-targeting-ectopically-expressed-peptide-g-protein-coupled-receptors-for-lung-cancer-therapy
#20
REVIEW
Mahjabin Khan, Tao Huang, Cheng-Yuan Lin, Jiang Wu, Bao-Min Fan, Zhao-Xiang Bian
Lung cancer, claiming millions of lives annually, has the highest mortality rate worldwide. This advocates the development of novel cancer therapies that are highly toxic for cancer cells but negligibly toxic for healthy cells. One of the effective treatments is targeting overexpressed surface receptors of cancer cells with receptor-specific drugs. The receptors-in-focus in the current review are the G-protein coupled receptors (GPCRs), which are often overexpressed in various types of tumors. The peptide subfamily of GPCRs is the pivot of the current article owing to the high affinity and specificity to and of their cognate peptide ligands, and the proven efficacy of peptide-based therapeutics...
June 7, 2017: Oncotarget
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