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https://www.readbyqxmd.com/read/28636973/amide-to-triazole-switch-vs-in-vivo-nep-inhibition-approaches-to-promote-radiopeptide-targeting-of-grpr-positive-tumors
#1
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...
June 10, 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
#2
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
https://www.readbyqxmd.com/read/28576168/theranostic-prospects-of-gastrin-releasing-peptide-receptor-radioantagonists-in-oncology
#3
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/28506620/bombesin-administration-impairs-memory-and-does-not-reverse-memory-deficit-caused-by-sleep-deprivation
#4
L B T Ferreira, S L B Oliveira, J Raya, L A Esumi, D C Hipolide
Sleep deprivation impairs performance in emotional memory tasks, however this effect on memory is not completely understood. Possible mechanisms may involve an alteration in neurotransmission systems, as shown by the fact that many drugs that modulate neural pathways can prevent memory impairment by sleep loss. Gastrin releasing peptide (GRP) is a neuropeptide that emerged as a regulatory molecule of emotional memory through the modulation of other neurotransmission systems. Thus, the present study addressed the effect of intraperitoneal (IP) administration of bombesin (BB) (2...
May 12, 2017: Behavioural Brain Research
https://www.readbyqxmd.com/read/28500250/characterization-of-nmb-grp-and-their-receptors-brs3-nmbr-and-grpr-in-chickens
#5
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/28485418/in-vitro-in-vivo-peeling-of-multilayered-aminocarboxylate-gold-nanoparticles-evidenced-by-a-kinetically-stable-99m-tc-label
#6
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)...
May 9, 2017: Dalton Transactions: An International Journal of Inorganic Chemistry
https://www.readbyqxmd.com/read/28476309/bombesin-receptor-activated-protein-regulates-neutrophil-elastase-induced-mucin-5ac-hypersecretion-in-human-bronchial-epithelial-cells
#7
Qing Xu, Ling-Xiu Chen, Dan-Hua Ran, Wen-Yue Xie, Xiang-Dong Zhou
Bombesin receptor-activated protein (BRAP) is highly expressed in human bronchial epithelial cells. Recent studies have shown that BRAP reduces oxidative stress, inhibits airway inflammation and suppresses nuclear factor kappaB (NF-κB) activity. Mucus overproduction is an important feature in patients with chronic inflammatory airway diseases. Neutrophil elastase (NE) is a potent inducer of mucin5AC (MUC5AC), which is considered the predominant mucin secreted by human airway epithelial cells. Here, we hypothesize that BRAP may regulate NE-induced MUC5AC hypersecretion in a bronchial epithelial cell line (HBE16)...
May 2, 2017: Experimental Cell Research
https://www.readbyqxmd.com/read/28408623/protein-kinase-d1-pkd1-phosphorylation-on-ser-203-by-type-i-p21-activated-kinase-pak-regulates-pkd1-localization
#8
Jen-Kuan Chang, Yang Ni, Liang Han, James Sinnett-Smith, Rodrigo Jacamo, Osvaldo Rey, Steven H Young, Enrique Rozengurt
Although PKC-mediated phosphorylation of protein kinase D1 (PKD1) has been extensively characterized, little is known about PKD1 regulation by other upstream kinases. Here we report that stimulation of epithelial or fibroblastic cells with G protein-coupled receptor agonists, including angiotensin II or bombesin, induced rapid and persistent PKD1 phosphorylation at Ser(203), a highly conserved residue located within the PKD1 N-terminal domain. Exposure to PKD or PKC family inhibitors did not prevent PKD1 phosphorylation at Ser(203), indicating that it is not mediated by autophosphorylation...
June 9, 2017: Journal of Biological Chemistry
https://www.readbyqxmd.com/read/28347132/radiolabeled-peptides-current-and-new-perspectives
#9
REVIEW
Marta Opalinska, Alicja Hubalewska-Dydejczyk, Anna Sowa-Staszczak
Radiolabeled peptides have been the subject of research for over 20 years and during that time possibility/variety of peptide receptor imaging and later targeted radiotherapy increased significantly. The targeted receptors belong to the large family of G-protein-coupled receptors or tyrosine kinases receptors partially connected with them. They both regulate large signaling networks, control multiple cell functions and are implicated in many diseases including cancers. The essential feature of peptides used in nuclear medicine involves their ability to binding with high affinity and specify to their receptors overexpressed on tumor cells...
June 2017: Quarterly Journal of Nuclear Medicine and Molecular Imaging
https://www.readbyqxmd.com/read/28324017/a-novel-selective-bombesin-receptor-subtype-3-agonist-promotes-weight-loss-in-male-diet-induced-obese-rats-with-circadian-rhythm-change
#10
Yasunori Nio, Natsu Hotta, Minoru Maruyama, Kenichi Hamagami, Toshimi Nagi, Masaaki Funata, Junichi Sakamoto, Masanori Nakakariya, Nobuyuki Amano, Tomohiro Okawa, Yasuyoshi Arikawa, Shinobu Sasaki, Shoki Okuda, Shizuo Kasai, Yugo Habata, Yasutaka Nagisa
Bombesin receptor subtype 3 (BRS-3) is an orphan G-protein-coupled receptor. Based on the obese phenotype of male BRS-3-deficient mice, BRS-3 has been considered an attractive target for obesity treatment. Here, we developed a novel selective BRS-3 agonist (Compound-A) and evaluated its anti-obesity effects. Compound-A showed anorectic effects and enhanced energy expenditure in diet-induced obese (DIO)-F344 rats. Moreover, repeated oral administration of Compound-A for 7 days resulted in a significant body weight reduction in DIO-F344 rats...
March 16, 2017: Endocrinology
https://www.readbyqxmd.com/read/28315588/neuromedin-an-insight-into-its-types-receptors-and-therapeutic-opportunities
#11
REVIEW
Saumitra Gajjar, Bhoomika M Patel
Neuropeptides are small protein used by neurons in signal communications. Neuromedin U was the first neuropeptide discovered from the porcine spinal and showed its potent constricting activities on uterus hence was entitled with neuromedin U. Following neuromedin U another of its isoform was discovered neuromedin S which was observed in suprachiasmatic nucleus hence was entitled neuromedin S. Neuromedin K and neuromedin L are of kanassin class which belong to tachykinin family. Bombesin family consists of neuromedin B and neuromedin C...
June 2017: Pharmacological Reports: PR
https://www.readbyqxmd.com/read/28267454/from-bench-to-bed-new-gastrin-releasing-peptide-receptor-directed-radioligands-and-their-use-in-prostate-cancer
#12
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
#13
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/28117023/an-overview-of-bioactive-peptides-for-in-vivo-imaging-and-therapy-in-human-diseases
#14
Anna Lucia Tornesello, Maria Lina Tornesello, Franco M Buonaguro
Radiolabeled peptides, designed to bind with high affinity receptors selectively expressed on cell membranes of different human tissues, represent valuable tools for in vivo imaging of several human diseases. Solid-phase peptide synthesis as well as availability of bifunctional chelating agents and prosthetic groups allows the production and radiolabeling of several peptide-based molecules which are useful to target specific receptors on different cancer types. Among them, octreotide and other analogues of somatostatin, vasoactive intestinal peptide, CCK analogues, bombesin, α-MSH analogues, neurotensin, exendin, RGD substance P, conjugated to appropriate chelators, such as DTPA, NOTA, DOTA or TETA, and radiolabeled with specific radionuclides, have already been translated into the clinical practice with remarkable sensitivity and diagnostic accurateness...
January 20, 2017: Mini Reviews in Medicinal Chemistry
https://www.readbyqxmd.com/read/28108545/bombesin-antagonist-based-radiotherapy-of-prostate-cancer-combined-with-wst-11-vascular-targeted-photodynamic-therapy
#15
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/28088445/synthesis-and-exploration-of-novel-radiolabeled-bombesin-peptides-for-targeting-receptor-positive-tumor
#16
Kakali De, Indranil Banerjee, Samarendu Sinha, Shantanu Ganguly
Increasing evidence of peptide receptor overexpression in various cancer cells, warrant the development of receptor specific radiolabeled peptides for molecular imaging and therapy in nuclear medicine. Gastrin-releasing-peptide (GRP) receptor, are overexpressed in a variety of human cancer cells. The present study report the synthesis and biological evaluation of new bombesin (BBN) analogs, HYNIC-Asp-[Phe(13)]BBN(7-13)-NH-CH2-CH2-CH3:BA1, HYNIC-Pro-[Tyr(13)Met(14)]BBN(7-14)NH2:BA2 as prospective tumor imaging agent with compare to BBN(7-14)NH2:BS as standard...
March 2017: Peptides
https://www.readbyqxmd.com/read/28040598/radiolabeled-bombesin-derivatives-for-preclinical-oncological-imaging
#17
REVIEW
Carolina de Aguiar Ferreira, Leonardo Lima Fuscaldi, Danyelle M Townsend, Domenico Rubello, André Luís Branco de Barros
Despite efforts, cancer is still one of the leading causes of morbidity and mortality worldwide, with approximately 14 million new cases and 8.2 million cancer-related deaths each year, according to the World Health Organization. Among the strategies to reduce cancer progression and improving its management, implementing early detection technologies is crucial. Based on the fact that several types of cancer cells overexpress surface receptors, small molecule ligands, such as peptides, have been developed to allow tumor identification at earlier stages...
March 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/28034291/radiopharmaceuticals-for-diagnosis-and-therapy-of-neuroendocrine-differentiated-prostate-cancer
#18
Giampiero Giovacchini, Elisabetta Giovannini, Mattia Riondato, Andrea Ciarmiello
Neuroendocrine differentiation of prostate cancer (PCa) is a relatively frequent event, generally understudied, that carries important prognostic information. It is most frequently observed during the advanced stages of disease, when PCa has lost its sensitivity to androgen deprivation therapy or to chemotherapy, moderate to diffuse bone metastatic spread dominates the imaging scenario and it is responsible for painful clinical symptomatology. However, evidences indicate that neuroendocrine differentiation is a progressive phenomenon that starts at the very early part of the pathogenesis of cancer transformation contributing to it...
December 29, 2016: Current Radiopharmaceuticals
https://www.readbyqxmd.com/read/27902882/glycated-99m-tc-tricarbonyl-labeled-peptide-conjugates-for-tumor-targeting-by-click-to-chelate
#19
Karolin Römhild, Christiane A Fischer, Thomas L Mindt
Attaching polar pharmacological modifiers to molecular imaging probes is a common strategy to modulate their pharmacokinetic profiles to improve such parameters as the clearance rate of radiotracers and/or metabolites, and to enhance signal-to-background ratios. We combined the tumor-targeting peptide sequence of bombesin (BBN) with glucuronic acid and the single-photon emission computed tomography (SPECT) radionuclide (99m) Tc by the "click-to-chelate" methodology. The (99m) Tc-tricarbonyl-labeled glucuronated BBN conjugate was compared with a reference compound lacking the carbohydrate...
January 5, 2017: ChemMedChem
https://www.readbyqxmd.com/read/27875420/molecular-imaging-in-neuroendocrine-tumors-recent-advances-controversies-unresolved-issues-and-roles-in-management
#20
Tetsuhide Ito, Robert T Jensen
PURPOSE OF REVIEW: The purpose is to review recent advances in molecular imaging of neuroendocrine tumors (NETs), discuss unresolved issues, and review how these advances are affecting clinical management. RECENT FINDINGS: Molecular imaging of NETs underwent a number of important changes in the last few years, leading to some controversies, unresolved issues, and significant changes in clinical management. The most recent changes are reviewed in this article. Particularly important is the rapid replacement in somatostatin receptor scintigraphy of In-diethylenetriamine penta-acetic acid-single-photon emission computed tomography/computed tomography (CT) by Ga-fluorodopa(F-D)PA), 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid (DOTA)-peptide-PET/CT imaging, which is now approved in many countries including the USA...
February 2017: Current Opinion in Endocrinology, Diabetes, and Obesity
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