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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/28626916/unexpected-functions-of-angiotensin-converting-enzyme-beyond-its-enzymatic-activity
#2
REVIEW
Jean Martinez
Angiotensin converting enzyme (ACE) is a well-known enzyme, largely studied for its action on hypertension, as it produces angiotensin II from angiotensin I. This paper describes two original behaviours of ACE. We showed that ACE could hydrolyse gastrin, a neuropeptide from the gastrointestinal tract, releasing the C-terminal amidated dipeptide H-Asp-Phe-NH2 . This dipeptide is believed to be involved in the gastrin-induced acid secretion in the stomach. This hypothetic mechanism of action of gastrin resulted in a strategy to rationally design gastrin receptor antagonists...
June 19, 2017: Journal of Peptide Science: An Official Publication of the European Peptide Society
https://www.readbyqxmd.com/read/28626400/long-term-efficacy-of-s-1-chemotherapy-plus-administration-of-octreotide-for-a-patient-with-metastatic-neuroendocrine-tumor-gastrinoma
#3
Sakura Hiraide, Sadahide Ono, Satoshi Kato
Metastatic neuroendocrine tumors (gastrinomas) have a poor prognosis. Octreotide can reduce gastrin levels and alleviate hormonal symptoms, and possibly slow tumor growth as well. No drugs were available except streptozocin for the treatment of metastatic pancreatic neuroendocrine tumor (PNET) in 2008. We report a case of PNET in a 53-year-old woman with multiple liver tumors treated with S-1 plus octreotide. After 6 months from the initiation of the treatment, the pancreatic tumor and liver metastases regressed, and the patient achieved partial response without the development of any serious adverse event...
May 2017: Case Reports in Oncology
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
#4
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/28621684/expression-of-hypothalamic-neurohormones-and-their-receptors-in-the-human-eye
#5
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/28609362/everolimus-effect-on-gastrin-and-glucagon-in-pancreatic-neuroendocrine-tumors
#6
Marianne E Pavel, David Chen, Wei He, Stephanie Cushman, Maurizio Voi, Elisabeth G E de Vries, Eric Baudin, James C Yao
OBJECTIVES: The pharmacodynamic effects of everolimus on gastrointestinal hormone levels have not been described in patients with pancreatic neuroendocrine tumors (pNETs). We report the effects of everolimus on gastrin and glucagon levels in patients with progressive pNET in RADIANT-1 (a single-arm phase II trial) and RADIANT-3 (a placebo-controlled, randomized, phase III trial). METHODS: Serum gastrin and glucagon levels were determined by immunoassay at baseline and at predose in subsequent treatment cycles in patients with elevated baseline hormone levels...
July 2017: Pancreas
https://www.readbyqxmd.com/read/28608155/pathophysiology-of-gastric-nets-role-of-gastrin-and-menin
#7
REVIEW
Sinju Sundaresan, Anthony J Kang, Juanita L Merchant
PURPOSE OF REVIEW: Neuroendocrine tumors (NETs) were initially identified as a separate entity in the early 1900s as a unique malignancy that secretes bioactive amines. GI-NETs are the most frequent type and represent a unique subset of NETs, because at least 75% of these tumors represent gastrin stimulation of the enterochromaffin-like cell located in the body of the stomach. The purpose of this review is to understand the specific role of gastrin in the generation of Gastric NETs (G-NETs)...
July 2017: Current Gastroenterology Reports
https://www.readbyqxmd.com/read/28596489/nanobubbles-as-ultrasound-contrast-agent-for-facilitating-small-cell-lung-cancer-imaging
#8
Jin-Ping Wang, Xiao-Lin Zhou, Ji-Ping Yan, Rong-Qin Zheng, Wei Wang
BACKGROUND: This study is to investigate whether liposome-loaded nanobubbles (NBs) have the potentials to carry anti-pro-gastrin releasing peptide (proGRP) antibody and enhance ultrasound imaging of small cell lung cancer (SCLC). METHODS: NBs were loaded with an antibody against SCLC (H446 cell line). A nude mouse model of SCLC tumor was established by a subcutaneous injection of tumor cell suspension in the dorsal skin. Images for contrast-enhanced ultrasound (CEUS) of xenograft tumors in the model were obtained through an intravenous injection of blank and targeting NBs...
May 24, 2017: Oncotarget
https://www.readbyqxmd.com/read/28595197/high-serum-pepsinogen-i-and-beta-helicobacter-pylori-infection-are-risk-factors-for-aspirin-induced-gastroduodenal-injury
#9
Jing Shan, Hongjun Lei, Wei Shi, Xiaobin Sun, Yu Tang, Chunrong Ren
BACKGROUND: Whether gastric hyperchlorhydria and Helicobacter pylori infection contribute to aspirin-induced gastroduodenal injury still lacks evidence. Because serum pepsinogens (PGs) and gastrin-17 (G17) can reflect gastric acid secretion, this study intended to elucidate whether serum PGs, serum G17, and H. pylori infection are associated with aspirin-induced gastrointestinal injury. SUMMARY: A total of 60 patients taking low-dose aspirin for more than 1 month were enrolled in this study...
June 9, 2017: Digestive Diseases
https://www.readbyqxmd.com/read/28587329/mosapride-combined-with-probiotics-on-gastrointestinal-function-and-growth-in-premature-infants
#10
Ai-Mei Zhang, Zhi-Qun Sun, Li-Ming Zhang
The aim of this study was to investigate the effects of mosapride combined with probiotics on gastrointestinal function and growth and development in premature infants. A total of 240 premature infants treated at Weifang People's Hospital between June 2012 and May 2015 who matched our criteria were randomly divided into three groups of 80 cases each. Group A received routine treatment, group B received routine treatment combined with live B. subtilis and E. faecium granules with multivitamins (Medilac-Vita), and group C received routine treatment and Saccharomyces boulardii sachets (Bioflor)...
June 2017: Experimental and Therapeutic Medicine
https://www.readbyqxmd.com/read/28576168/theranostic-prospects-of-gastrin-releasing-peptide-receptor-radioantagonists-in-oncology
#11
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/28566601/challenging-differential-diagnosis-of-hypergastremia-and-hyperglucagonemia-with-chronic-renal-failure-report-of-a-case-with-multiple-endocrine-neoplasia-type-1
#12
Takaaki Murakami, Takeshi Usui, Yuji Nakamoto, Akio Nakajima, Yuki Mochida, Sumio Saito, Takahiro Shibayama, Nobuhisa Yamazaki, Tomonobu Hatoko, Tomoko Kato, Shin Yonemitsu, Seiji Muro, Shogo Oki
A 53-year-old woman developed end-stage renal failure during a 15-year clinical course of primary hyperparathyroidism and was referred to our hospital for evaluation of suspected multiple endocrine neoplasia type 1 (MEN1). Genetic testing revealed a novel deletion mutation at codon 467 in exon 10 of the MEN1 gene. Systemic and selective arterial calcium injection (SACI) testing revealed hyperglucagonemia and hypergastrinemia with positive gastrin responses. A pathological examination revealed glucagonoma and a lymph node gastrinoma...
2017: Internal Medicine
https://www.readbyqxmd.com/read/28560291/gastrin-and-gastric-cancer
#13
REVIEW
Jill P Smith, Sandeep Nadella, Nick Osborne
Gastric cancer is the third leading cause of cancer-related mortality worldwide. Despite progress in understanding its development, challenges with treatment remain. Gastrin, a peptide hormone, is trophic for normal gastrointestinal epithelium. Gastrin also has been shown to play an important role in the stimulation of growth of several gastrointestinal cancers including gastric cancer. We sought to review the role of gastrin and its pathway in gastric cancer and its potential as a therapeutic target in the management of gastric cancer...
July 2017: Cellular and Molecular Gastroenterology and Hepatology
https://www.readbyqxmd.com/read/28510260/markers-of-enteral-adaptation-in-pediatric-cases-with-short-bowel-syndrome
#14
Masahiro Chiba, Yutaka Sanada, Akira Toki
BACKGROUND: This study aimed to ascertain if prospective determinations of specific gut hormones and growth factors could predict bowel adaptation in children with short bowel syndrome (SBS). METHODS: We studied parenteral nutrition (PN) independency as the short-term result and discontinuation of enteral nutrition (EN) as the long-term result from a retrospective chart review of 7 patients with SBS, who were managed in the absence of growth retardation. The correlation between increased numbers of enteral feedings or enteral nutrients and fasting levels of serum gastrin, glucagon-like peptide 2 (GLP-2), citrulline, and diamine oxidase (DAO) activity was analyzed...
May 16, 2017: Pediatrics International: Official Journal of the Japan Pediatric Society
https://www.readbyqxmd.com/read/28508274/the-sleeping-remnant-effect-of-roux-en-y-gastric-bypass-on-plasma-levels-of-gastric-biomarkers-in-morbidly-obese-women-a-prospective-longitudinal-study
#15
Federico Marchesi, Francesco Tartamella, Giuseppina De Sario, Clarissa Forlini, Alberta Caleffi, Matteo Riccò, Francesco Di Mario
BACKGROUND: Morpho-functional modifications of the gastric remnant after Roux-en-Y gastric bypass (RYGB) have not been completely defined, due to its inaccessibility for bioptic mapping. The aim of the study is to evaluate such modifications using Gastropanel®, a non-invasive blood test cross-checking four gastric biomarkers, able to provide a snapshot of mucosa conditions. SUBJECTS AND METHODS: Twenty-four women undergoing RYGB were prospectively enrolled. Gastropanel® parameters (pepsinogens, Gastrin-17 and immunoglobulins against Helicobacter pylori), biometrical/clinical data were collected preoperatively and at 6-months follow-up...
May 15, 2017: Obesity Surgery
https://www.readbyqxmd.com/read/28506620/bombesin-administration-impairs-memory-and-does-not-reverse-memory-deficit-caused-by-sleep-deprivation
#16
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/28501979/endocrine-cells-producing-peptide-hormones-in-the-intestine-of-nile-tilapia-distribution-and-effects-of-feeding-and-fasting-on-the-cell-density
#17
Raquel Tatiane Pereira, Thaiza Rodrigues de Freitas, Izabela Regina Cardoso de Oliveira, Leandro Santos Costa, Fabricio Andrés Vigliano, Priscila Vieira Rosa
Endocrine cells (ECs) act as a luminal surveillance system responding to either the presence or absence of food in the gut through the secretion of peptide hormones. The aim of this study was to analyze the effects of feeding and fasting on the EC peptide-specific distribution along the intestine of Nile tilapia. We assessed the density of ECs producing gastrin (GAS), cholecystokinin-8 (CCK-8), neuropeptide Y (NPY), and calcitonin gene-related peptide (CGRP) in nine segments of the intestine using immunohistochemistry...
May 13, 2017: Fish Physiology and Biochemistry
https://www.readbyqxmd.com/read/28500250/characterization-of-nmb-grp-and-their-receptors-brs3-nmbr-and-grpr-in-chickens
#18
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/28498440/gastrin-induces-multidrug-resistance-via-the-degradation-of-p27kip1-in-the-gastric-carcinoma-cell-line-sgc7901
#19
Kun Zhuang, Lingxia Zhang, Xin Zhang, Hailing Tang, Jun Zhang, Yuan Yan, Kun Han, Hanqing Guo
Multidrug resistance (MDR) is one of the major reasons for the failure of chemotherapy-based gastric carcinoma (GC) treatments, hence, biologically based therapies are urgently needed. Gastrin (GAS), a key gastrointestinal (GI) hormone, was found to be involved in tumor formation, progression, and metastasis. In this study, quantitative real-time polymerase chain reaction (qRT-PCR) and immunohistochemical staining analysis revealed a high level of expression of GAS in drug-insensitive GC tissues (P<0.01) and similar results were revealed in GC cell lines SGC7901 and its multidrug-resistant variants SGC7901/VCR and SGC7901/ADR...
May 4, 2017: International Journal of Oncology
https://www.readbyqxmd.com/read/28489853/novel-genes-involved-in-severe-early-onset-obesity-revealed-by-rare-copy-number-and-sequence-variants
#20
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
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