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https://www.readbyqxmd.com/read/28336782/functional-imaging-signature-of-patients-presenting-with-polycythemia-paraganglioma-syndromes
#1
Ingo Janssen, Clara Chi Chen, Zhenping Zhuang, Corina M Millo, Katherine Wolf, Alexander Ling, Frank I Lin, Karen T Adams, Peter Herscovitch, Richard A Feelders, Antonio T Fojo, David Taieb, Electron Kebebew, Karel Pacak
Rationale: Pheochromocytoma/paraganglioma (PPGL) syndromes associated with polycythemia have previously been described in association with mutations in the von Hippel-Lindau (VHL) gene. Recently, mutations in the prolyl hydroxylase gene (PHD) 1 and 2 and in the hypoxia-inducible factor 2 alpha (HIF2A) were also found to be associated with multiple and recurrent PPGL. Such patients also presented with PPGL and polycythemia, and later on, some presented with duodenal somatostatinoma. In additional patients presenting with PPGL and polycythemia, no further mutations have been discovered...
March 23, 2017: Journal of Nuclear Medicine: Official Publication, Society of Nuclear Medicine
https://www.readbyqxmd.com/read/28332450/nuclear-medicine-in-patients-with-net-radiolabeled-somatostatin-analogues-and-their-brothers
#2
Vincenzo Cuccurullo, Maria Rosaria Prisco, Giuseppe Danilo Di Stasio, Luigi Mansi
Although Somastostatin (SS) scintigraphy (SRS) has been introduced many years ago, it remains the most diffuse radionuclide diagnostic tool in patients with neuroendocrine tumours (NETs). Being SS receptors (SSTR) expressed in the majority of NETs, radiolabeled SS analogues (SS-A) provide high diagnostic accuracy, mainly in patients with gastro-entero-pancreatic (GEP) tumors. SSTR are the best target for radiotracers used either for diagnostic and therapeutic purposes in NETs due to their presence on the surface of neoplastic cells of clinical interest...
March 23, 2017: Current Radiopharmaceuticals
https://www.readbyqxmd.com/read/28332260/biological-characterization-of-novel-nitroimidazole-peptide-conjugates-in-vitro-and-in-vivo
#3
Ralf Bergmann, Katrin Splith, Jens Pietzsch, Michael Bachmann, Ines Neundorf
Recently, we reported on the design of a multimodal peptide conjugate useful as delivery platform for targeting hypoxic cells. A nitroimidazole (2-(2-nitroimidazol-1-yl)acetic acid, NIA) moiety, which is selectively entrapped in hypoxic cells, was coupled to a cell-penetrating peptide serving as the transporter. Furthermore, attachment of a bifunctional linker allowed the introduction of a diagnostic or therapeutic radiometal. However, although selective tumor accumulation could be detected in vivo, a fast renal clearance of the compound was observed...
March 23, 2017: Journal of Peptide Science: An Official Publication of the European Peptide Society
https://www.readbyqxmd.com/read/28331187/cross-beta-nanostructures-based-on-dinaphthylalanine-gd-conjugates-loaded-with-doxorubicin
#4
Carlo Diaferia, Eliana Gianolio, Teresa Sibillano, Flavia Anna Mercurio, Marilisa Leone, Cinzia Giannini, Nicole Balasco, Luigi Vitagliano, Giancarlo Morelli, Antonella Accardo
Very recently we proposed novel di- and tetra-phenylalanine peptides derivatized with gadolinium complexes as potentials supramolecular diagnostic agents for applications in MRI (Magnetic Resonance Imaging). It was observed that in very short FF dipeptide building blocks, the propensity to aggregate decreases significantly after modification with bulky moiety such as Gd-complexes, thus limiting their potential as CAs. We hypothesized that the replacement of the Phe side chain with more extended aromatic groups could improve the self-assembling...
March 22, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28324047/functional-imaging-in-the-follow-up-of-enteropancreatic-neuroendocrine-tumors-clinical-usefulness-and-indications
#5
Elettra Merola, Marianne E Pavel, Francesco Panzuto, Gabriele Capurso, Noemi Cicchese, Anja Rinke, Thomas M Gress, Elsa Iannicelli, Daniela Prosperi, Patrizia Pizzichini, Vikas Prasad, Patrizia Kump, Rainer Lipp, Stefano Partelli, Massimo Falconi, Bertram Wiedenmann, Gianfranco Delle Fave
Context: Functional imaging tests (FITs) detecting somatostatin receptors expression (i.e., Somatostatin Receptor Scintigraphy, 68Ga-DOTA-peptide positron emission tomography/computed tomography) have a pivotal role in the diagnosis of neuroendocrine tumors (NETs), while their indication during follow-up still needs to be clarified. Objective: Investigate the role of FITs after diagnosis of metastatic enteropancreatic NETs, identifying patients who might benefit from these exams...
January 13, 2017: Journal of Clinical Endocrinology and Metabolism
https://www.readbyqxmd.com/read/28320783/pitfalls-in-the-response-evaluation-after-prrt-with-177-lu-dota-0-tyr-3-octreotate
#6
Tessa Brabander, Wouter Van der Zwan, Jaap J M Teunissen, Boen L R Kam, Wouter W de Herder, R A Feelders, Eric P Krenning, Dik Kwekkeboom
Peptide receptor radionuclide therapy (PRRT) with [177Lu-DOTA0,Tyr3]octreotate (177Lu-DOTATATE) is a treatment with good results in patients with metastatic gastroenteropancreatic neuroendocrine tumour (GEPNETs). However, there are some pitfalls that should be taken into consideration when evaluating the treatment response after PRRT. 354 Dutch patients with GEPNETs who were treated with 177Lu-DOTATATE between March 2000 and December 2011 were retrospectively selected. Liver function parameters and chromogranin A were measured before each therapy and in follow-up...
March 20, 2017: Endocrine-related Cancer
https://www.readbyqxmd.com/read/28317976/albumin-based-nanoparticles-loaded-with-hydrophobic-gadolinium-chelates-as-t1-t2-dual-mode-contrast-agents-for-accurate-liver-tumor-imaging
#7
Lirong Wang, Hongyu Lin, Lingceng Ma, Jianbin Jin, Taipeng Shen, Ruixue Wei, Xiaomin Wang, Hua Ai, Zhong Chen, Jinhao Gao
Magnetic resonance contrast agents with T1-T2 dual mode contrast capability have attracted considerable interest because they offer complementary and synergistic diagnostic information, leading to high imaging sensitivity and accurate diagnosis. Here, we reported a facile strategy to construct albumin based nanoparticles loaded with hydrophobic gadolinium chelates by hydrophobic interaction for magnetic resonance imaging (MRI). We synthesized a glycyrrhetinic acid-containing Gd-DOTA derivative (GGD) and loaded GGD molecules into BSA nanoparticles to form GGD-BSA nanoparticles (GGD-BSA NPs)...
March 20, 2017: Nanoscale
https://www.readbyqxmd.com/read/28317154/development-of-a-novel-fibrin-specific-pet-tracer
#8
Tiemen van Mourik, Michael Claesener, Klaas Nicolay, Holger Gruell
Fibrin deposition is observed in several diseases such as atherosclerosis, deep vein thrombosis and also tumors, where it contributes to the formation of mature tumor stroma. The aim of this study was to develop a gallium-labeled peptide tracer based on the fibrin targeting peptide Epep for PET imaging of fibrin deposition. For this purpose, the peptide Epep was modified with a NOTA moiety for radiolabeling with (67) Ga and (68) Ga and compared with the earlier validated (111) In-DOTA-Epep tracer. In vitro binding assays of (67) Ga-NOTA-Epep displayed an enhanced retention as compared to previously published data showing binding of (111) In-DOTA-Epep to human (84...
March 20, 2017: Journal of Labelled Compounds & Radiopharmaceuticals
https://www.readbyqxmd.com/read/28301261/a-radiolabeled-fully-human-antibody-to-human-aspartyl-asparaginyl-%C3%AE-hydroxylase-is-a-promising-agent-for-imaging-and-therapy-of-metastatic-breast-cancer
#9
Ekaterina Revskaya, Zewei Jiang, Alfred Morgenstern, Frank Bruchertseifer, Muctarr Sesay, Susan Walker, Steven Fuller, Michael S Lebowitz, Claudia Gravekamp, Hossein A Ghanbari, Ekaterina Dadachova
There is a need for novel effective and safe therapies for metastatic breast cancer based on targeting tumor-specific molecular markers of cancer. Human aspartyl (asparaginyl) β-hydroxylase (HAAH) is a highly conserved enzyme that hydroxylates epidermal growth factor-like domains in transformation-associated proteins and is overexpressed in a variety of cancers, including breast cancer. A fully human monoclonal antibody (mAb) PAN-622 has been developed to HAAH. In this study, they describe the development of PAN-622 mAb as an agent for imaging and radioimmunotherapy of metastatic breast cancer...
March 2017: Cancer Biotherapy & Radiopharmaceuticals
https://www.readbyqxmd.com/read/28294439/coordination-of-tetravalent-actinides-an-th-iv-u-iv-np-iv-pu-iv-with-dota-from-dimers-to-hexamers
#10
Christelle Tamain, Thomas Dumas, Christoph Hennig, Philippe Guilbaud
Three tetravalent actinide (An(IV)) hexanuclear clusters with the octahedral core [An6(OH)4O4]12+ (An(IV) = U(IV), Np(IV), Pu(IV)) were structurally characterized in solid state and in aqueous solution using single crystal X-ray diffraction, X-ray absorption, IR, Raman and UV-Visible spectroscopy. The observed structure, [An6(OH)4O4(H2O)8(HDOTA)4].HCl/HNO3.nH2O (An = U (I), Np (II), Pu (III)), consists of a An(IV) hexanuclear pseudo-octahedral cluster stabilized by DOTA (1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid) ligands...
March 10, 2017: Chemistry: a European Journal
https://www.readbyqxmd.com/read/28286746/dota-derivatives-of-octreotide-dicarba-analogs-with-high-affinity-for-somatostatin-sst2-5-receptors
#11
Alessandro Pratesi, Mauro Ginanneschi, Marco Lumini, Anna M Papini, Ettore Novellino, Diego Brancaccio, Alfonso Carotenuto
In vivo somatostatin receptor scintigraphy is a valuable method for the visualization of human endocrine tumors and their metastases. In fact, peptide ligands of somatostatin receptors (sst's) conjugated with chelating agents are in clinical use. We have recently developed octreotide dicarba-analogs, which show interesting binding profiles at sst's. In this context, it was mandatory to explore the possibility that our analogs could maintain their activity also upon conjugation with DOTA. In this paper, we report and discuss the synthesis, binding affinity and conformational preferences of three DOTA-conjugated dicarba-analogs of octreotide...
2017: Frontiers in Chemistry
https://www.readbyqxmd.com/read/28263215/pituitary-adenoma-recurrence-suspected-on-central-hyperthyroidism-despite-empty-sella-and-confirmed-by-68-ga-dota-toc-pet-ct
#12
Mathieu Gauthé, Julie Sarfati, Nathalie Bourcigaux, Sophie Christin-Maitre, Jean-Noël Talbot, Françoise Montravers
Thyrotropin-secreting pituitary adenomas are very rare tumors, known to present overexpression of somatostatin receptor subtype 2 and which may consequently demonstrate abnormal uptake on Ga-DOTA-TOC PET/CT. A 67-year-old woman with a history of operated pituitary macroadenoma presented with symptoms of hyperthyroidism including a large goiter. Her serum thyroid hormone levels were in favor of central hyperthyroidism. Pituitary MRI depicted an empty sella but visualized an ambiguous lesion centered on the left sphenoidal sinus...
March 3, 2017: Clinical Nuclear Medicine
https://www.readbyqxmd.com/read/28257815/gadolinium-released-by-the-linear-gadolinium-based-contrast-agent-gd-dtpa-decreases-the-activity-of-human-epithelial-na-channels-enacs
#13
Fenja Knoepp, Joerg Bettmer, Martin Fronius
BACKGROUND: Gadolinium-based-contrast-agents (GBCAs) are used for magnetic-resonance-imaging and associated with renal and cardiovascular adverse reactions caused by released Gd(3+) ions. Gd(3+) is also a modulator of mechano-gated ion channels, including the epithelial Na(+) channel (ENaC) that is expressed in kidney epithelium and the vasculature. ENaC is important for salt-/water homeostasis and blood pressure regulation and a likely target of released Gd(3+) from GBCAs causing the above-mentioned adverse reactions...
February 28, 2017: Biochimica et Biophysica Acta
https://www.readbyqxmd.com/read/28240661/molecular-imaging-in-neuroendocrine-differentiation-of-prostate-cancer-68-ga-psma-versus-68-ga-dota-noc-pet-ct
#14
Sharjeel Usmani, Najeeb Ahmed, Fahad Marafi, Rashid Rasheed, Henney G Amanguno, Fareeda Al Kandari
We report on a 62-year-old man with metastatic prostate cancer (cT3b N1) diagnosed in 2011, treated with total androgen blockage with flutamide and goserelin acetate (Zoladex). He presented with left suprascapular swelling and low-back pain after being asymptomatic for 5 years. His prostate-specific antigen was 0.049 ng/mL. F-NaF PET-CT and Ga-PSMA scan were negative, whereas Ga-DOTA NOC scan done after 10 days showed multiple somatostatin-avid hepatic and lymph node metastasis.
February 24, 2017: Clinical Nuclear Medicine
https://www.readbyqxmd.com/read/28230065/in-vivo-evaluation-of-a-novel-format-of-a-bivalent-her3-targeting-and-albumin-binding-therapeutic-affibody-construct
#15
Tarek Z Bass, Maria Rosestedt, Bogdan Mitran, Fredrik Y Frejd, John Löfblom, Vladimir Tolmachev, Stefan Ståhl, Anna Orlova
Overexpression of human epidermal growth factor receptor 3 (HER3) is involved in resistance to several therapies for malignant tumours. Currently, several anti-HER3 monoclonal antibodies are under clinical development. We introduce an alternative approach to HER3-targeted therapy based on engineered scaffold proteins, i.e. affibody molecules. We designed a small construct (22.5 kDa, denoted 3A3), consisting of two high-affinity anti-HER3 affibody molecules flanking an albumin-binding domain ABD, which was introduced for prolonged residence in circulation...
February 23, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28229838/-treatment-of-gastroenteropancreatic-neuroendocrine-tumors-with-177lu-dota-tate-experience-of-the-portuguese-institute-of-oncology-in-porto
#16
Inês Lucena Sampaio, Henrique Vara Luiz, Liliana Sobral Violante, Ana Paula Santos, Luís Antunes, Isabel Torres, Cristina Sanches, Isabel Azevedo, Hugo Duarte
INTRODUCTION: The purpose of this article is to report the experience of the Portuguese Institute of Oncology - Porto in the treatment of gastroenteropancreatic neuroendocrine tumors with 177Lu-DOTA-TATE, regarding the safety and efficacy of this treatment modality. MATERIAL AND METHODS: A retrospective analysis of clinical reports of patients with gastroenteropancreatic neuroendocrine tumors undergoing treatment with 177Lu-DOTA-TATE between April 2011 and November 2013 was performed...
November 2016: Acta Médica Portuguesa
https://www.readbyqxmd.com/read/28220538/on-bead-combinatorial-synthesis-and-imaging-of-europium-iii-based-paracest-agents-aids-in-identification-of-chemical-features-that-enhance-cest-sensitivity
#17
Jaspal Singh, Vineeta Rustagi, Shanrong Zhang, A Dean Sherry, D Gomika Udugamasooriya
The rate of water exchange between the inner-sphere of a paramagnetic ion and bulk water is an important parameter in determining the magnitude of the chemical exchange saturation transfer signal from paramagnetic CEST agents (paraCEST). This is governed by various geometric, steric, and ligand field factors created by macrocyclic ligands surrounding the paramagnetic metal ion. Our previous on-bead combinatorial studies of di-peptoid-europium(III)-DOTA-tetraamide complexes revealed that negatively charged groups in the immediate vicinity of the metal center strongly enhances the CEST signal...
February 21, 2017: Magnetic Resonance in Chemistry: MRC
https://www.readbyqxmd.com/read/28218348/radioguided-surgery-with-radiolabeled-somatostatin-analogs-not-only-in-gep-nets
#18
REVIEW
Vincenzo Cuccurullo, Giuseppe Danilo Di Stasio, Luigi Mansi
Radioguided surgery (RGS) is a surgical technique that, using intra-operative probes, enables the surgeon to identify tissues preoperatively "marked" by a radiopharmaceutical. Somatostatin receptors (SSTRs) are present in the majority of neuroendocrine cells and may be over-expressed not only by tumor cells, but also by endothelial cells of peritumoral vessels, inflammatory cells and cells of the immune system, such as activated lymphocytes, monocytes and epithelioid cells. This extra neoplastic uptake is the rationale for the use of radiolabeled somatostatin analogs (SSAs) either in some tumors not expressing SSTRs or in various non-oncological diseases...
2017: Nuclear Medicine Review. Central & Eastern Europe
https://www.readbyqxmd.com/read/28203088/peptide-receptor-radionuclide-therapy-in-the-management-of-gastrointestinal-neuroendocrine-tumors-efficacy-profile-safety-and-quality-of-life
#19
REVIEW
Stefano Severi, Ilaria Grassi, Silvia Nicolini, Maddalena Sansovini, Alberto Bongiovanni, Giovanni Paganelli
Peptide receptor radionuclide therapy (PRRT), developed over the last two decades, is carried out using radiopharmaceuticals such as 90Y-DOTA-Tyr3-octreotide and 177Lu-DOTA-Tyr3-octreotate (177Lu-Dotatate). These radiocompounds are obtained by labeling a synthetic somatostatin analog with a β-emitting radioisotope. The compounds differ from each other in terms of their energetic features (due to the radionuclide) and peptide receptor affinity (due to the analog) but share the common characteristic of binding specific membrane somatostatin receptors that are (generally) overexpressed in neuroendocrine neoplasms (NENs) and their metastases...
2017: OncoTargets and Therapy
https://www.readbyqxmd.com/read/28190898/synthesis-and-opioid-receptor-binding-of-indium-iii-and-111-in-labeled-macrocyclic-conjugates-of-diprenorphine-novel-ligands-designed-for-imaging-studies-of-peripheral-opioid-receptors
#20
Shefali Srivastava, Emily A Fergason-Cantrell, Roger I Nahas, John R Lever
Radiolabeled diprenorphine (DPN) and analogs are widely used ligands for non-invasive brain imaging of opioid receptors. To develop complementary radioligands optimized for studies of the peripheral opioid receptors, we prepared a pair of hydrophilic DPN derivatives, conjugated to the macrocyclic chelator DOTA (1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid), for complexation with trivalent metals. The non-radioactive indium (III) complexes, tethered to the C6-oxygen position of the DPN scaffold by 6- to 9-atom spacers, displayed high affinities for binding to μ, δ and κ opioid receptors in vitro...
October 6, 2016: Tetrahedron
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