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Wenhui Ma, Fanfan Fu, Jingyi Zhu, Rui Huang, Yizhou Zhu, Zhenwei Liu, Jing Wang, Peter S Conti, Xiangyang Shi, Kai Chen
We report the use of multifunctional folic acid (FA)-modified dendrimers as a platform to radiolabel with 64Cu for PET imaging of folate receptor (FR)-expressing tumors. In this study, amine-terminated generation 5 (G5) poly(amidoamine) dendrimers were sequentially modified with fluorescein isothiocyanate (FI), FA, and 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid (DOTA), followed by acetylation of the remaining dendrimer terminal amines. The as-formed multifunctional DOTA-FA-FI-G5·NHAc dendrimers were then radiolabeled with 64Cu via the DOTA chelation...
March 16, 2018: Nanoscale
Yushen Jin, Kun Wang, Jie Tian
In clinical imaging modalities, MRI is suitable for preoperative examination. And fluorescence imaging has been proposed to improve the detectability of cancer lesions during the operation. However, the specificity and accuracy of the two imaging modalities is limited. To improve the prognosis and survival rate of the patient suffering from hepatocellular carcinoma (HCC), it is very important to develop a specific probe to achieve early detection and precise resection of HCC. We selected HCC targeting peptide SP94 to conjugate with a NIR dye and Gd chelated DOTA to enhance the specificity of different imaging modalities...
March 15, 2018: Bioconjugate Chemistry
E J Meester, B J Krenning, R H de Blois, J P Norenberg, M de Jong, M R Bernsen, K Van der Heiden
BACKGROUND: 111 In-DOTA-butylamino-NorBIRT (DANBIRT) is a novel radioligand which binds to Leukocyte Function-associated Antigen-1 (LFA-1), expressed on inflammatory cells. This study evaluated111 In-DANBIRT for the visualization of atherosclerotic plaque inflammation in mice. METHODS AND RESULTS: ApoE-/- mice, fed an atherogenic diet up to 20 weeks (n = 10), were imaged by SPECT/CT 3 hours post injection of111 In-DANBIRT (~ 200 pmol, ~ 40 MBq). Focal spots of111 In-DANBIRT were visible in the aortic arch of all animals, with an average Target-to-Background Ratio (TBR) of 1...
March 13, 2018: Journal of Nuclear Cardiology: Official Publication of the American Society of Nuclear Cardiology
Mathieu Gauthé, Nathalie Testart Dardel, Fernando Ruiz Santiago, Jessica Ohnona, Valérie Nataf, Françoise Montravers, Jean-Noël Talbot
OBJECTIVES: To develop criteria to improve discrimination between vertebral metastases from neuroendocrine tumours (NETs) and benign bone lesions on PET combined with CT using DOTA-D-Phe1 -Tyr3 -octreotide labelled with gallium-68 (68 Ga-DOTA-TOC). METHODS: In 535 NET patients,68 Ga-DOTA-TOC PET/CT examinations were reviewed retrospectively for vertebral CT lesions and/or PET foci. For each vertebral PET abnormality, appearance on CT, biological volume (BV), standardized uptake value (SUVmax ) and ratios to those of reference organs were determined...
March 12, 2018: European Radiology
Marie Paquet, Mathieu Gauthé, Jules Zhang Yin, Valérie Nataf, Ophélie Bélissant, Philippe Orcel, Christian Roux, Jean-Noël Talbot, Françoise Montravers
PURPOSE: Oncogenic osteomalacia is an endocrine disorder induced by small benign tumours (TIO) producing excessive fibroblast growth factor-23 (FGF23). The only way of curing oncogenic osteomalacia is surgical resection of the culprit TIO, which is extremely difficult to detect using conventional imaging modalities due to its small size and variable location in the body. Since TIO frequently overexpress somatostatin receptors, a clinical utility of SPECT or PET with radiolabelled somatostatin analogues has been reported...
March 12, 2018: European Journal of Nuclear Medicine and Molecular Imaging
Irina Velikyan, Örjan Lindhe
Monitoring general disease marker such as angiogenesis may contribute to the development of personalized medicine and improve therapy outcome. Readily availability of positron emitter based imaging agents providing quantification would expand clinical positron emission tomography (PET) applications. Generator produced68 Ga provides PET images of high resolution and the half-life time frame is compatible with the pharmacokinetics of small peptides comprising arginine-glycine-aspartic acid (RGD) sequence specific to αv β3 integrin receptors...
2018: American Journal of Nuclear Medicine and Molecular Imaging
Alessandra Zilli, Ilaria Fanetti, Dario Conte, Sara Massironi
Gallium-68 DOTA-peptide positron emission tomography/computed tomography (68 Ga-PET/CT) has emerged as a promising tool for the diagnosis and staging of gastro-entero-pancreatic neoplasms, thanks to its high sensitivity and specificity. Heterotopic pancreas, which is relatively rare, has never been reported as a possible cause of false positives of68 Ga-PET/CT. We report on the first case of a heterotopic pancreas showing pathological uptake at68 Ga-PET/CT, thus mimicking an intestinal neuroendocrine tumor...
March 6, 2018: Clinical Imaging
Eszter Boros, Omar R Pinkhasov, Peter Caravan
Background: Current analytical methods for characterizing pharmacokinetic and metabolic properties of positron emission tomography (PET) and single photon emission computed tomography (SPECT) probes are limited. Alternative methods to study tracer metabolism are needed. The study objective was to assess the potential of high performance liquid chromatography - inductively coupled plasma - mass spectrometry (HPLC-ICP-MS) for quantification of molecular probe metabolism and pharmacokinetics using stable isotopes...
2018: EJNMMI Radiopharm Chem
Rosemery Membreno, Brendon E Cook, Kimberly Fung, Jason S Lewis, Brian M Zeglis
Pretargeted radioimmunotherapy (PRIT) based on the inverse electron demand Diels-Alder (IEDDA) reaction between tetrazine (Tz) and trans-cyclooctene (TCO) represents a promising strategy for leveraging the affinity and specificity of antibodies without their pharmacokinetic drawbacks. Herein, we present an investigation of the in vivo efficacy and dosimetry of a PRIT strategy for colorectal carcinoma based on the ligation between a177 Lu-labeled Tz radioligand (177 Lu-DOTA-PEG7 -Tz) and a TCO-bearing immunoconjugate of the huA33 antibody (huA33-TCO)...
March 5, 2018: Molecular Pharmaceutics
Marek Pruszynski, Matthias D'Huyvetter, Frank Bruchertseifer, Alfred Morgenstern, Tony Lahoutte
Human epidermal growth factor receptor type 2 (HER2) is overexpressed in numerous carcinomas. Nanobodies (Nbs) are the smallest antibody-derived fragments with beneficial characteristics for molecular imaging and radionuclide therapy. Therefore, HER2-targeting nanobodies could offer a valuable platform for radioimmunotherapy, especially when labeled with α-particle emitters, which provide highly lethal and localized radiation to targeted cells with minimal exposure to surrounding healthy tissues. In this study, the anti-HER2 2Rs15d-nanobody was conjugated with 2-(4-isothiocyanatobenzyl)-1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid ( p-SCN-Bn-DOTA) and radiolabeled with an α-emitter225 Ac with a high yield (>90%) and a radiochemical purity above 95%...
March 5, 2018: Molecular Pharmaceutics
Xuan Mei, Wei Wang, Liang Yan, Tingting Hu, Ruizheng Liang, Dan Yan, Min Wei, David G Evans, Xue Duan
Recently, theranostic has drawn tremendous attention by virtue of the nanotechnology development and new material exploration. Herein, we reported a novel theranostic system by loading Au nanoclusters (AuNCs) and Chlorin e6 (photosensitizer, Ce6) onto the monolayer nanosheet surface of Gd-doped layered double hydroxide (Gd-LDH). The as-prepared Ce6&AuNCs/Gd-LDH exhibits a largely enhanced fluorescence quantum yield (QY) of 18.5% relative to pristine AuNCs (QY = 3.1%) as well as superior T1 magnetic resonance imaging (MRI) performance (r1  = 17...
February 19, 2018: Biomaterials
Ulrike Garske-Román, Mattias Sandström, Katarzyna Fröss Baron, Lars Lundin, Per Hellman, Staffan Welin, Silvia Johansson, Tanweera Khan, Hans Lundqvist, Barbro Eriksson, Anders Sundin, Dan Granberg
PURPOSE: Peptide receptor radionuclide therapy in patients with neuroendocrine tumours has yielded promising results. This prospective study investigated the feasibility of dosimetry of the kidneys and bone marrow during therapy and its impact on efficacy and outcome. METHODS: The study group comprised 200 consecutive patients with metastasized somatostatin receptor-positive neuroendocrine tumours progressing on standard therapy or not suitable for other therapeutic options...
March 1, 2018: European Journal of Nuclear Medicine and Molecular Imaging
Vojtěch Kubíček, Zuzana Böhmová, Romana Ševčíková, Jakub Vaněk, Přemysl Lubal, Zuzana Poláková, Romana Michalicová, Jan Kotek, Petr Hermann
H3 nota derivatives are among the most studied macrocyclic ligands and are widely used for metal ion binding in biology and medicine. Despite more than 40 years of chemical research on H3 nota, the comprehensive study of its solution chemistry has been overlooked. Thus, the coordination behavior of H3 nota with several divalent metal ions was studied in detail with respect to its application as a chelator for copper radioisotopes in medical imaging and therapy. In the solid-state structure of the free ligand in zwitterionic form, one proton is bound in the macrocyclic cavity through a strong intramolecular hydrogen-bond system supporting the high basicity of the ring amine groups (log Ka = 13...
February 28, 2018: Inorganic Chemistry
Elisabeth Eppard, Ana de la Fuente, Nicole Mohr, Mareli Allmeroth, Rudolf Zentel, Matthias Miederer, Stefanie Pektor, Frank Rösch
BACKGROUND: In this work, the in vitro and in vivo stabilities and the pharmacology of HPMA-made homopolymers were studied by means of radiometal-labeled derivatives. Aiming to identify the fewer amount and the optimal DOTA-linker structure that provides quantitative labeling yields, diverse DOTA-linker systems were conjugated in different amounts to HPMA homopolymers to coordinate trivalent radiometals Me(III)* = gallium-68, scandium-44, and lutetium-177. RESULTS: Short linkers and as low as 1...
February 27, 2018: EJNMMI Research
Lixiong Dai, Chloe M Jones, Wesley Ting Kwok Chan, Tiffany A Pham, Xiaoxi Ling, Eric M Gale, Nicholas J Rotile, William Chi-Shing Tai, Carolyn J Anderson, Peter Caravan, Ga-Lai Law
Despite established clinical utilisation, there is an increasing need for safer, more inert gadolinium-based contrast agents, and for chelators that react rapidly with radiometals. Here we report the syntheses of a series of chiral DOTA chelators and their corresponding metal complexes and reveal properties that transcend the parent DOTA compound. We incorporated symmetrical chiral substituents around the tetraaza ring, imparting enhanced rigidity to the DOTA cavity, enabling control over the range of stereoisomers of the lanthanide complexes...
February 27, 2018: Nature Communications
Charalambos Tsoukalas, Simonetta Geninatti-Crich, Anastasios Gaitanis, Theodoros Tsotakos, Maria Paravatou-Petsotas, Silvio Aime, Rogelio Jiménez-Juárez, Constantinos D Anagnostopoulos, Kristina Djanashvili, Penelope Bouziotis
PURPOSE: The aim of this study was to demonstrate the potential of Ga-68-labeled macrocycle (DOTA-en-pba) conjugated with phenylboronic vector for tumor recognition by positron emission tomography (PET), based on targeting of the overexpressed sialic acid (Sia). PROCEDURES: The imaging reporter DOTA-en-pba was synthesized and labeled with Ga-68 at high efficiency. Cell binding assay on Mel-C and B16-F10 melanoma cells was used to evaluate melanin production and Sia overexpression to determine the best model for demonstrating the capability of [68 Ga]DOTA-en-pba to recognize tumors...
February 20, 2018: Molecular Imaging and Biology: MIB: the Official Publication of the Academy of Molecular Imaging
Luigi Granato, Luce Vander Elst, Celine Henoumont, Robert N Muller, Sophie Laurent
Thanks to the understanding of the relationships between the residence lifetime τM of the coordinated water molecules to macrocyclic Gd-complexes and the rotational mobility τR of these structures, and according to the theory for paramagnetic relaxation, it is now possible to design macromolecular contrast agents with enhanced relaxivities by optimizing these two parameters through ligand structural modification. We succeeded in accelerating the water exchange rate by inducing steric compression around the water binding site, and by removing the amide function from the DOTA-AA ligand [1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid mono(p-aminoanilide)] (L) previously designed...
December 16, 2017: Chemistry & Biodiversity
Jagannath Palepu, Shailesh V Shrikhande, Debanshu Bhaduri, Rajiv C Shah, Bhawna Sirohi, Verushka Chhabra, Puneet Dhar, Regulagedda Sastry, Sadiq Sikora
INTRODUCTION: Gastroenteropancreatic neuroendocrine tumors (GEP-NETs) are rare tumors. We report data of 407 GEP-NET cases from a neuroendocrine tumor (NET) registry in India. METHODS: The AP-NET registry is an open-label, multicenter, longitudinal observational registry of patients with GEP-NETs in which six tertiary care oncology centers contributed data. Data was prospectively entered in a dedicated computerized database and was reviewed retrospectively. The patients were divided into three cohorts-those diagnosed from 2001 to 2005, from 2006 to 2010, and from 2011 to 2016...
November 2017: Indian Journal of Gastroenterology: Official Journal of the Indian Society of Gastroenterology
Lihui Wei, Julia Petryk, Chantal Gaudet, Maryam Kamkar, Wei Gan, Yin Duan, Terrence D Ruddy
BACKGROUND: Chemokine receptor 5 (CCR5) plays an important role in atherosclerosis. Our objective was to develop a SPECT tracer targeting CCR5 for imaging plaque inflammation by radiolabeling D-Ala-peptide T-amide (DAPTA), a CCR5 antagonist, with 111In. METHODS: 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid (DOTA) conjugated DAPTA (DOTA-DAPTA) was labeled with 111In. Cell uptake studies were conducted in U87-CD4-CCR5 and U87-MG cells. Biodistribution was determined in C57BL/6 mice...
February 7, 2018: Journal of Nuclear Cardiology: Official Publication of the American Society of Nuclear Cardiology
Kusum Vats, Ashis Kumar Satpati, Rohit Sharma, Haladhar Dev Sarma, Drishty Satpati, Ashutosh Dash
This study explores the potential of 177Lu-labeled carbon nanospheres as radio-nanoprobes for molecular imaging and therapy. The carboxyl functionalized surface of carbon nanospheres (CNS) was conjugated with [Gly-Gly-Gly-c(Asn-Gly-Arg)], G3-cNGR peptide through amide bond for targeting tumor vasculature and with [2-(4-Aminobenzyl)-1,4,7,10-tetraazacyclododecane tetraacetic acid], p-NH2-Bz-DOTA for chelation with 177Lu. The nanosphere-peptide conjugate, DOTA-CNS-cNGR, was characterized by dynamic light scattering and zeta potential measurements, IR and UV experiments and did not show any in vitro cytotoxicity...
February 1, 2018: Journal of Pharmaceutical and Biomedical Analysis
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