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Christoph Göbl, Moritz Resch, Madeleine Strickland, Christoph Hartlmüller, Martin Viertler, Nico Tjandra, Tobias Madl
The study of intrinsically disordered proteins (IDPs) by NMR often suffers from highly overlapped resonances that prevent unambiguous chemical-shift assignments, and data analysis that relies on well-separated resonances. We present a covalent paramagnetic lanthanide-binding tag (LBT) for increasing the chemical-shift dispersion and facilitating the chemical-shift assignment of challenging, repeat-containing IDPs. Linkage of the DOTA-based LBT to a cysteine residue induces pseudo-contact shifts (PCS) for resonances more than 20 residues from the spin-labeling site...
October 20, 2016: Angewandte Chemie
Achim Paulmichl, Dominik Summer, Claudia Manzl, Christine Rangger, Francesca Orlandi, Sabrina Niedermoser, Takahiro Taguchi, Björn Wängler, Clemens Decristoforo
The gastrointestinal stromal tumor (GIST) is a rare disease with limited therapeutic options when resistance to tyrosine kinase inhibitor (TKI) treatment occurs. The authors investigated binding of various (68)Ga-labeled peptides, targeting receptors reported to be overexpressed in GIST, in different cell lines. For this purpose, three GIST cell lines were tested: GIST-T1, GIST882 (Imatinib sensitive), and GIST430 (Imatinib resistant). DOTA-NT 8-13 (targeting NTR1), DOTA-TATE (targeting SSTR2), CP04 (a minigastrin derivative targeting CCK2-R), VIP-DOTA (targeting VPAC2-R), and 2 DOTA-bombesin derivatives [targeting gastrin releasing peptide receptors (GRPR)] were radiolabeled with (68)Ga and incubated with the respective tumor cell and control cell lines...
October 2016: Cancer Biotherapy & Radiopharmaceuticals
Ji Woong Lee, Yong Jin Lee, Un Chol Shin, Suhng Wook Kim, Byung Il Kim, Kyo Chul Lee, Jung Young Kim, Ji-Ae Park
Improving the in vivo pharmacokinetics (PK) of positron emission tomography (PET) radiotracers is of critical importance to tumor diagnosis and therapy. In the case of peptide-based radiotracers, the modification and addition of a linker or spacer functional group often offer faster in vivo pharmacokinetic behavior. In this study, the authors introduced two new PEGlyated dimeric c(RGD-ACH-K) conjugates, in which an aminocyclohexane carboxylic acid (ACH) is inserted into the ring chain of the cyclic RGD peptides, with a common bifunctional chelator (DOTA or NOTA) used for labeling with radiometals (including (68)Ga and (64)Cu)...
October 2016: Cancer Biotherapy & Radiopharmaceuticals
Georgios Z Papadakis, Corina Millo, Samira M Sadowski, Ulas Bagci, Nicholas J Patronas
Renal and pancreatic cysts and tumors are the most common visceral manifestations of von Hippel-Lindau (VHL) disease, a heritable multisystem cancer syndrome characterized by development of a variety of malignant and benign tumors. We report a case of a VHL patient with multiple renal cystic and complex cystic/solid lesions. The patient underwent Ga-DOTA-TATE-PET/CT showing intensely increased activity by a solid lesion which demonstrated enhancement on both CT and MRI scans, raising high suspicion for malignancy...
October 5, 2016: Clinical Nuclear Medicine
Ximena Camacho, Victoria Calzada, Marcelo Fernández, Omar Alonso, Roger Chammas, Eloisa Riva, Juan Pablo Gambini, Pablo Cabral
BACKGROUND: Vascular endothelial growth factor (VEGF) is one of the classic factors to tumor-induced angiogenesis in several types, including melanoma. Bevacizumab is a humanized monoclonal antibody directed against VEGF. OBJECTIVE: To radiolabel Bevacizumab with 177-Lutetium as a potential radioimmunotherapy agent for melanoma. METHODS: Bevacizumab was derivatized with DOTA-NHS-ester at 4 ºC for 18 h. DOTA-Bevacizumab was radiolabeled with 177LuCl3 (15 MBq/mg) at 37 ºC for 1 h...
October 10, 2016: Current Radiopharmaceuticals
Christoph Wetz, I Apostolova, I G Steffen, F Hofheinz, C Furth, D Kupitz, J Ruf, M Venerito, S Klose, Holger Amthauer
PURPOSE: The purpose of this study was to assess the value of the spatial heterogeneity of somatostatin receptor (SSR) volume, quantified as asphericity (ASP), and to predict response to peptide receptor radionuclide therapy (PRRT) in patients with metastatic gastroenteropancreatic neuroendocrine neoplasms (GEP-NEN). PROCEDURES: From June 2011 to May 2013, patients suffering from GEP-NEN who underwent pretherapeutic [(111)In-DTPA(0)]octreotide scintigraphy (Octreoscan®) prior to [(177)Lu-DOTA(0)-Tyr(3)]octreotate ([(177)Lu]DOTATATE)-PRRT were enrolled in this retrospective evaluation...
October 14, 2016: Molecular Imaging and Biology: MIB: the Official Publication of the Academy of Molecular Imaging
Javad Garousi, Sarah Lindbo, Hadis Honarvar, Justin Velletta, Bogdan Mitran, Mohamed Altai, Anna Orlova, Vladimir Tolmachev, Sophia Hober
Radionuclide imaging-based stratification of patients to targeted therapies makes cancer treatment more personalized and therefore more efficient. ADAPTs (ABD Derived Affinity ProTeins) constitute a novel group of imaging probes based on the scaffold of an albumin-binding domain (ABD). To evaluate how different compositions of the N-terminal sequence of ADAPTs influence their biodistribution, a series of human epidermal growth factor receptor type 2 (HER2)-binding ADAPT6 derivatives with different N-terminal sequences were created: GCH6DANS (2), GC(HE)3DANS (3), GCDEAVDANS (4) and GCVDANS(5) and compared with the parental variant: GCSS(HE)3DEAVDANS (1)...
October 14, 2016: Bioconjugate Chemistry
Johanna M U Silvola, Helena Virtanen, Riikka Siitonen, Sanna Hellberg, Heidi Liljenbäck, Olli Metsälä, Mia Ståhle, Tiina Saanijoki, Meeri Käkelä, Harri Hakovirta, Seppo Ylä-Herttuala, Pekka Saukko, Matti Jauhiainen, Tibor Z Veres, Sirpa Jalkanen, Juhani Knuuti, Antti Saraste, Anne Roivainen
Given the important role of inflammation and the potential association of the leukocyte trafficking-associated adhesion molecule vascular adhesion protein 1 (VAP-1) with atherosclerosis, this study examined whether functional VAP-1 is expressed in atherosclerotic lesions and, if so, whether it could be targeted by positron emission tomography (PET). First, immunohistochemistry revealed that VAP-1 localized to endothelial cells of intra-plaque neovessels in human carotid endarterectomy samples from patients with recent ischemic symptoms...
October 12, 2016: Scientific Reports
Haroon Ur Rashid, Marco Antonio Utrera Martines, Juliana Jorge, Paula Martin de Moraes, Muhammad Naveed Umar, Kamin Khan, Hanif Ur Rehman
Magnetic Resonance Imaging (MRI) is a noninvasive radiology technique used to examine the internal organs of human body. It is useful for the diagnosis of structural abnormalities in the body. Contrast agents are used to increase the sensitivity of this technique. 1,4,7,10-Tetraazacyclododecane (cyclen) is a macrocyclic tetraamine. Its derivatives act as useful ligands to produce stable complexes with Gd(3+) ion. Such chelates are investigated as MRI contrast agents. Free Gd(3+) ion is extremely toxic for in vivo use...
October 1, 2016: Bioorganic & Medicinal Chemistry
Jin Hee Kim, Ji-Yeon Suh, Dong-Cheol Woo, Yu Sub Sung, Woo-Chan Son, Yoon Seok Choi, Sang Joon Pae, Jeong Kon Kim
Contrast enhancement by an extracellular-fluid contrast agent (CA) (Gd-DOTA) depends primarily on the blood-brain-barrier permeability (bp), and transverse-relaxation change caused by intravascular T2 CA (superparamagnetic iron oxide nanoparticles, SPIONs) is closely associated with the blood volume (BV). Pharmacokinetic (PK) vascular characterization based on single-CA-using dynamic contrast-enhanced MRI (DCE-MRI) has shown significant measurement variation according to the molecular size of the CA. Based on this recognition, this study used a dual injection of Gd-DOTA and SPIONs for tracing the changes of bp and BV in C6 glioma growth (Days 1 and 7 after the tumor volume reached 2 mL)...
October 10, 2016: NMR in Biomedicine
Zhijuan Xiong, Yue Wang, Jingyi Zhu, Yao He, Jiao Qu, Christiane Effenberg, Jindong Xia, Dietmar Appelhans, Xiangyang Shi
We report the design of the fourth generation poly(propylene imine) (PPI) glycodendrimers for magnetic resonance (MR) imaging applications. The glycodendrimers were designed to have a densely organized maltose shell (MAL DS) and several tetraazacyclododecane tetraacetic acid (DOTA) ligands that were attached to the periphery of the PPI dendrimers for Gd(iii) chelation. We show that the formed MAL DS-modified PPI dendrimers possess good cytocompatibility and hemocompatibility in the studied concentration range...
October 18, 2016: Biomaterials Science
Helene Strauch, Jörn Engelmann, Klaus Scheffler, Hermann A Mayer
A fast and simple route was developed to synthesize a new T8-silsesquioxane based contrast agent for potential application in Magnetic Resonance Imaging. For this purpose the novel C2-thiol-functionalized T8-silsesquioxane (3) was constructed as a carrier molecule as well as the DOTA based gadolinium(iii) complex (11) equipped with allyl terminated linkers was prepared. The linkage of the complexes to the T8-silsesquioxane was performed via an UV-light catalyzed thiol-ene click reaction within one hour which affords the desired product 13 in a yield of 80%...
September 27, 2016: Dalton Transactions: An International Journal of Inorganic Chemistry
Katharina Keller, Michal Zalibera, Mian Qi, Vanessa Koch, Julia Wegner, Henrik Hintz, Adelheid Godt, Gunnar Jeschke, Anton Savitsky, Maxim Yulikov
The four Mn(ii) complexes Mn-DOTA, Mn-TAHA, Mn-PyMTA, and Mn-NO3Py were characterized by electron paramagnetic resonance (EPR), electron-nuclear double resonance (ENDOR), and relaxation measurements, to predict their relative performance in the EPR pulse dipolar spectroscopy (PDS) experiments. High spin density localization on the metal ions was proven by ENDOR on (1)H, D, (14)N, and (55)Mn nuclei. The transverse relaxation of the Mn(ii) complexes appears to be slow enough for PDS-based spin-spin distance determination...
September 14, 2016: Physical Chemistry Chemical Physics: PCCP
Max A Kruziki, Brett A Case, Jie Ying Chan, Elizabeth J Zudock, Daniel R Woldring, Douglas Yee, Benjamin J Hackel
PURPOSE: Determine the efficacy of a 45-amino acid Gp2 domain, engineered to bind to epidermal growth factor receptor (EGFR), as a positron emission tomography (PET) probe of EGFR in a xenograft mouse model. METHODS: The EGFR-targeted Gp2 (Gp2-EGFR) and a non-binding control were site-specifically labeled with 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid (DOTA) chelator. Binding affinity was tested towards human EGFR and mouse EGFR. Biological activity on downstream EGFR signaling was examined in cell culture...
October 3, 2016: Molecular Pharmaceutics
Sang-Gyu Lee, Kishore Gangangari, Teja Muralidhar Kalidindi, Blesida Punzalan, Steven M Larson, Naga Vara Kishore Pillarsetty
INTRODUCTION: Bone marrow is the soft tissue compartment inside the bones made up of hematopoietic cells, adipocytes, stromal cells, phagocytic cells, stem cells, and sinusoids. While [(18)F]-FLT has been utilized to image proliferative marrow, to date, there are no reports of particle based positron emission tomography (PET) imaging agents for imaging bone marrow. We have developed copper-64 labeled liposomal formulation that selectively targets bone marrow and therefore serves as an efficient PET probe for imaging bone marrow...
August 27, 2016: Nuclear Medicine and Biology
Roland Darr, Joan Nambuba, Jaydira Del Rivero, Ingo Janssen, Maria Merino, Milena Todorovic, Bela Balint, Ivana Jochmanova, Josef T Prchal, Ronald Lechan, Arthur S Tischler, Vera Popovic, Dragana Miljic, Karen T Adams, F Ryan Prall, Alexander Ling, Meredith R Golomb, Michael Ferguson, Naris Nilubol, Clara Chen, Emily Chew, David Taieb, Constantine A Stratakis, Antonio Fojo, Chunzhang Yang, Electron Kebebew, Zhengping Zhuang, Karel Pacak
The syndrome of paraganglioma (PGL), somatostatinoma (SOM), and early childhood polycythemia in patients with somatic mutations in the hypoxia-inducible factor 2 alpha (HIF2A) gene is described in only a few patients worldwide. The present study provides detailed information about the clinical aspects and course of 7 patients with this syndrome and brings these experiences into perspective with the pertinent literature. Six females and one male presented at a median age of 28 years (range 11-46). Two were found to have HIF2A somatic mosaicism...
September 27, 2016: Endocrine-related Cancer
Grace Kong, Jason Callahan, Michael S Hofman, David A Pattison, Tim Akhurst, Michael Michael, Peter Eu, Rodney J Hicks
PURPOSE: Bulky disease is an adverse prognostic factor for (177)Lu-DOTA-octreotate ((177)Lu-DOTATATE) peptide receptor radionuclide therapy (PRRT). (90)Y-DOTA-octreotate ((90)Y-DOTATATE) has theoretical advantages in this setting but may less effectively treat co-existent smaller deposits and have higher toxicity than (177)Lu-DOTATATE. The aim of this study was to assess the efficacy and safety of using these agents sequentially. METHODS: We reviewed patients (pts) with at least one lesion of a transaxial diameter >4 cm who completed 1-2 cycles of (90)Y-DOTATATE followed by 2-3 cycles of (177)Lu-DOTATATE, with treatment empirically adapted to disease size and burden in individual patients...
September 27, 2016: European Journal of Nuclear Medicine and Molecular Imaging
Chengcheng Zhang, Jinhe Pan, Kuo-Shyan Lin, Iulia Dude, Joseph Lau, Jutta Zeisler, Helen Merkens, Silvia Jenni, Brigitte Guérin, François Bénard
The neuropeptide Y1 receptor (Y1R) is overexpressed in many human cancers, particularly breast cancer. Due to stability issues, limited success has been achieved for Y1R imaging agents, including full length and truncated neuropeptide Y (NPY) analogues. The goal of this study was to evaluate the possibility of using radiolabeled truncated NPY analogues to visualize Y1R expression in a preclinical model of Y1R-positive tumor. Four truncated NPY analogues were synthesized based on the sequence of [Pro(30), Tyr(32), Leu(34)]NPY(28-36), also known as BVD15...
October 3, 2016: Molecular Pharmaceutics
Madeleine Strickland, Charles D Schwieters, Christoph Göbl, Ana C L Opina, Marie-Paule Strub, Rolf E Swenson, Olga Vasalatiy, Nico Tjandra
Lanthanide complexes based on the DOTA (1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid) cage are commonly used as phase contrast agents in magnetic resonance imaging, but can also be utilized in structural NMR applications due to their ability to induce either paramagnetic relaxation enhancement or a pseudocontact shift (PCS) depending on the choice of the lanthanide. The size and sign of the PCS for any given atom is determined by its coordinates relative to the metal center, and the characteristics of the lanthanide's magnetic susceptibility tensor...
September 22, 2016: Journal of Biomolecular NMR
Vincenza Granata, Marco Cascella, Roberta Fusco, Nicoletta dell'Aprovitola, Orlando Catalano, Salvatore Filice, Vincenzo Schiavone, Francesco Izzo, Arturo Cuomo, Antonella Petrillo
Background and Purpose. Contrast media (CM) for magnetic resonance imaging (MRI) may determine the development of acute adverse reactions. Objective was to retrospectively assess the frequency and severity of adverse reactions associated with gadolinium-based contrast agents (GBCAs) injection in patients who underwent MRI. Material and Methods. At our center 10608 MRI examinations with CM were performed using five different GBCAs: Gd-BOPTA (MultiHance), Gd-DTPA (Magnevist), Gd-EOBDTPA (Primovist), Gd-DOTA (Dotarem), and Gd-BTDO3A (Gadovist)...
2016: BioMed Research International
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