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https://www.readbyqxmd.com/read/28917649/evaluation-of-novel-111-in-labeled-gonadotropin-releasing-hormone-peptides-for-human-prostate-cancer-imaging
#1
Jingli Xu, Changjian Feng, Yubin Miao
The purpose of this study was to evaluate the tumor targeting and imaging properties of novel (111)In-labeled gonadotropin-releasing hormone (GnRH) peptides for human prostate cancer. Three new 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid (DOTA)-linker-d-Phe-(d-Lys(6)-GnRH) peptides with different hydrocarbon linkers were designed to evaluate their effects on GnRH receptor binding affinities. The Aoc (aminooctanoic acid) linker was better than βAla (3-aminopropanoic acid) and Aun (aminoundecanoic acid) linkers in retaining strong receptor binding affinity...
September 7, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28916621/-64-cu-labeled-repebody-molecules-for-imaging-of-epidermal-growth-factor-receptor-expressing-tumors
#2
Ayoung Pyo, Misun Yun, Hyeon-Sik Kim, Tae-Yoon Kim, Joong-Jae Lee, Jung Young Kim, Sunwoo Lee, Seong Young Kwon, Hee-Seung Bom, Hak-Sung Kim, Dong-Yeon Kim, Jung-Joon Min
The epidermal growth factor receptor (EGFR) is a member of the erbB family of receptors and is overexpressed in many tumor types. A repebody is a newly designed non-antibody protein scaffold for tumor targeting that contains leucine-rich repeat modules. In this study, three (64)Cu-labeled anti-EGFR repebodies with different chelators were synthesized, and their biological characteristics were assessed in cultured cells and tumor-bearing mice. Methods: Repebodies (rEgAs) were synthesized with the chelators p-SCN-Bn-NOTA, DOTA-NHS ester, or p-SCN-Bn-DTPA in 1...
September 15, 2017: Journal of Nuclear Medicine: Official Publication, Society of Nuclear Medicine
https://www.readbyqxmd.com/read/28912884/towards-translational-immunopet-mr-imaging-of-invasive-pulmonary-aspergillosis-the-humanised-monoclonal-antibody-jf5-detects-aspergillus-lung-infections-in-vivo
#3
Genna Davies, Anna-Maria Rolle, Andreas Maurer, Philipp R Spycher, Claudia Schillinger, Djamschid Solouk-Saran, Mike Hasenberg, Juliane Weski, Jesper Fonslet, Adrien Dubois, Frederic Boschetti, Franck Denat, Matthias Gunzer, Martin Eichner, Lauren S Ryder, Mikael Jensen, Roger Schibli, Bernd J Pichler, Stefan Wiehr, Christopher R Thornton
Invasive pulmonary aspergillosis (IPA) is a life-threatening lung disease of hematological malignancy or bone marrow transplant patients caused by the ubiquitous environmental fungus Aspergillus fumigatus. Current diagnostic tests for the disease lack sensitivity as well as specificity, and culture of the fungus from invasive lung biopsy, considered the gold standard for IPA detection, is slow and often not possible in critically ill patients. In a previous study, we reported the development of a novel non-invasive procedure for IPA diagnosis based on antibody-guided positron emission tomography and magnetic resonance imaging (immunoPET/MRI) using a [(64)Cu]DOTA-labeled mouse monoclonal antibody (mAb), mJF5, specific to Aspergillus...
2017: Theranostics
https://www.readbyqxmd.com/read/28912146/cerenkov-activated-sticky-tag-for-in-vivo-fluorescence-imaging
#4
Sudeep Das, Katja Haedicke, Jan Grimm
A big challenge for the clinical utilization of Cerenkov luminescence (CL) imaging is its low signal intensity, which is several orders of magnitude below ambient light. Consequently, highly sensitive cameras, sufficient shielding from background light and long acquisition times are required. To alleviate this problem, we hypothesize a strategy to convert the weak CL signal into a stronger fluorescence signal by using CL-activated formation of nitrenes from azides to locally fix a fluorescent probe in tissue by the formation of a covalent bond...
September 14, 2017: Journal of Nuclear Medicine: Official Publication, Society of Nuclear Medicine
https://www.readbyqxmd.com/read/28910151/synthesis-positron-emission-tomography-imaging-and-therapy-of-diabody-targeted-drug-lipid-nanoparticles-in-a-prostate-cancer-murine-model
#5
Patty Wong, Lin Li, Junie Chea, Melissa K Delgado, Erasmus Poku, Barbara Szpikowska, Nicole Bowles, Megan Minnix, David Colcher, Jeffrey Y C Wong, John E Shively, Paul J Yazaki
The blood clearance of chemotherapeutic drugs such as doxorubicin (Dox) can be extended by incorporation into lipid nanoparticles (LNPs) and further improved by tumor targeting with antibody fragments. We used positron emission tomography (PET) imaging in a murine prostate cancer model to evaluate tumor targeting of LNPs incorporating Dox and antiprostate-specific membrane antigen (PSMA) diabodies. Dox-LNPs were generated by mixing or covalent attachment to water soluble distearoylphosphatidyl ethanolamine-polyethylene glycol (DSPE-PEG)2000...
September 2017: Cancer Biotherapy & Radiopharmaceuticals
https://www.readbyqxmd.com/read/28910148/bulk-scale-formulation-of-therapeutic-doses-of-clinical-grade-ready-to-use-177-lu-dota-tate-the-intricate-radiochemistry-aspects
#6
Anupam Mathur, Vrinda Prashant, Navin Sakhare, Sudipta Chakraborty, K V Vimalnath, Repaka Krishna Mohan, Chanda Arjun, Barkha Karkhanis, Ravi Seshan, Sandip Basu, Aruna Korde, Sharmila Banerjee, Ashutosh Dash, Satbir Singh Sachdev
INTRODUCTION: (177)Lu-DOTA-TATE is a clinically useful and promising therapeutic radiopharmaceutical for peptide receptor radionuclide therapy of neuroendocrine tumors (NETs) overexpressing somatostatin receptors. Currently, the radiopharmaceutical is prepared in-house at nuclear medicine centers, thereby restricting its use to limited centers only. In this article, the authors describe systematic studies toward bulk scale formulation of "ready-to-use" (177)Lu-DOTA-TATE using medium specific activity (177)Lu (740-1110 GBq/mg) at a centralized radiopharmacy facility...
September 2017: Cancer Biotherapy & Radiopharmaceuticals
https://www.readbyqxmd.com/read/28903488/an-analysis-of-the-relationship-between-preclinical-and-clinical-qt-interval-related-data
#7
Christopher E Pollard, Matthew Skinner, Stanley E Lazic, Helen M Prior, Kelly M Conlon, Jean-Pierre Valentin, Corina Dota
There has been significant focus on drug-induced QT interval prolongation caused by block of the human ether-a-go-go-related gene (hERG)-encoded potassium channel. Regulatory guidance has been implemented to assess QT interval prolongation risk: preclinical guidance requires a candidate drug's potency as a hERG channel blocker to be defined and also its effect on QT interval in a non-rodent species; clinical guidance requires a "Thorough QT Study" during development, although some QT prolonging compounds are identified earlier via a Phase I study...
September 1, 2017: Toxicological Sciences: An Official Journal of the Society of Toxicology
https://www.readbyqxmd.com/read/28898054/synthesis-radiolabeling-and-characterization-of-plasma-protein-binding-ligands-potential-tools-for-modulation-of-the-pharmacokinetic-properties-of-radio-pharmaceuticals
#8
Cristina Müller, Renáta Farkas, Francesca Borgna, Raffaella M Schmid, Martina Benešová, Roger Schibli
The development of (radio)pharmaceuticals with favorable pharmacokinetic profiles is crucial for allowing the optimization of the imaging or therapeutic potential and the minimization of undesired side effects. The aim of this study was, therefore, to evaluate and compare three different plasma protein binders (PPB-01, PPB-02, and PPB-03) that are potentially useful in combination with (radio)pharmaceuticals to enhance their half-life in the blood. The entities were functionalized with a 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid (DOTA) chelator via a l-lysine and β-alanine linker moiety using solid-phase peptide chemistry and labeled with (177)Lu (T1/2 = 6...
September 12, 2017: Bioconjugate Chemistry
https://www.readbyqxmd.com/read/28895598/measurement-of-reaction-kinetics-of-177-lu-lu-dota-tate-using-a-microfluidic-system
#9
Z Liu, K S Schaap, L Ballemans, R de Zanger, E de Blois, M Rohde, E Oehlke
Microfluidic synthesis techniques can offer improvement over batch syntheses which are currently used for radiopharmaceutical production. These improvements are, for example, better mixing of reactants, more efficient energy transfer, less radiolysis, faster reaction optimization, and overall improved reaction control. However, scale-up challenges hinder the routine clinical use, so the main advantage is currently the ability to optimize reactions rapidly and with low reactant consumption. Translating those results to clinical systems could be done based on calculations, if kinetic constants and diffusion coefficients were known...
September 12, 2017: Dalton Transactions: An International Journal of Inorganic Chemistry
https://www.readbyqxmd.com/read/28894897/peptide-receptor-radionuclide-therapy-prrt-in-european-neuroendocrine-tumour-society-enets-grade-3-g3-neuroendocrine-neoplasia-nen-a-single-institution-retrospective-analysis
#10
Sue Ping Thang, Mei Sim Lung, Grace Kong, Michael S Hofman, Jason Callahan, Michael Michael, Rodney J Hicks
PURPOSE: Grade 3 NENs are aggressive tumours with poor prognosis. PRRT+/- radiosensitising chemotherapy is a potential treatment for disease with high somatostatin receptor (SSTR) expression without spatially discordant FDG-avid disease. We retrospectively evaluated the efficacy of PRRT in G3 NEN. METHODS: Kaplan-Meier estimation was used to determine progression-free survival (PFS) and overall survival (OS) defined from start of PRRT. Subgroup analysis was performed for patients with Ki-67 ≤ 55% and >55%...
September 12, 2017: European Journal of Nuclear Medicine and Molecular Imaging
https://www.readbyqxmd.com/read/28876087/preparation-and-evaluation-of-177-lu-labeled-gemcitabine-an-effort-toward-developing-radiolabeled-chemotherapeutics-for-targeted-therapy-applications
#11
Subhajit Ghosh, Tapas Das, Haladhar D Sarma, Ashutosh Dash
OBJECTIVE: Gemcitabine, a nucleoside analogue, is used as a chemotherapeutic drug for the treatment of a wide variety of cancers. Therefore, radiolabeled gemcitabine may have potential as a radiotherapeutic agent for the treatment of various types of cancers. In the present work, an attempt has been made to radiolabel gemcitabine with (177)Lu and study the preliminary biological behavior of (177)Lu-labeled gemcitabine in tumor-bearing animal model. EXPERIMENTAL: Gemcitabine was coupled with p-NCS-benzyl-DOTA, a bifunctional chelating agent, to facilitate radiolabeling with (177)Lu...
September 2017: Cancer Biotherapy & Radiopharmaceuticals
https://www.readbyqxmd.com/read/28872546/68ga-dota-tate-pet-ct-for-molecular-imaging-of-somatostatin-receptor-expression-in-metastasizing-epithelioid-hemangioendothelioma-comparison-with-18f-fdg
#12
Thorsten Derlin, Katja Hueper, Bisharah Soudah
Epithelioid hemangioendothelioma (EHE) is a rare tumor originating from vascular endothelial or pre-endothelial cells. It has the potential to metastasize. We present the case of a 51-year-old woman with metastasizing EHE who underwent both F-FDG and Ga-DOTA-TATE PET/CT for staging of disease and for evaluation of targeted radionuclide therapy potential. On Ga-DOTA-TATE PET scans, intense tracer accumulation was observed in metastases. Besides the increased glucose metabolism in EHE, this case highlights the potential of Ga-DOTA-TATE PET/CT for restaging of EHE and the option of targeted radionuclide therapy in this entity...
September 1, 2017: Clinical Nuclear Medicine
https://www.readbyqxmd.com/read/28867112/pet-computed-tomography-and-precision-medicine-in-pancreatic-adenocarcinoma-and-pancreatic-neuroendocrine-tumors
#13
REVIEW
Daniella F Pinho, Rathan M Subramaniam
(18)F-FDG PET/CT has been described as an accurate tool for initial diagnosis of pancreatic adenocarcinoma. It differentiates benign from malignant causes; detects local and, especially, distant spread of disease; and is a very good predictor of patient prognosis. Pancreatic neuroendocrine tumors are rare tumors that originate from the islet cells of the pancreas. Currently, (68)Ga-DOTA-labeled somatostatin analogs are considered the best modality for detection of well-differentiated neuroendocrine tumors. (18)F-FDG PET/CT has a role in patients with poorly differentiated tumors...
October 2017: PET Clinics
https://www.readbyqxmd.com/read/28864631/radionuclide-tumor-targeting-using-adapt-scaffold-proteins-aspects-of-label-positioning-and-residualizing-properties-of-the-label
#14
Sarah Lindbo, Javad Garousi, Bogdan Mitran, Mohamed Altai, Jos Buijs, Anna Orlova, Sophia Hober, Vladimir Tolmachev
Visualization of cancer-associated alterations of molecular phenotype using radionuclide imaging is a non-invasive approach to stratify patients for targeted therapies. The engineered scaffold protein ABD-.derived affinity protein (ADAPT) is a promising tracer for radionuclide molecular imaging due to its small size (6.5 kDa), that provides precondition for efficient tumor penetration and rapid clearance. Previous studies demonstrated that the human epidermal growth factor receptor type 2 (HER2)-targeting ADAPT6 labeled with radiometals at the N-terminus provides imaging of HER2 expression in xenografts a few hours after injection...
September 1, 2017: Journal of Nuclear Medicine: Official Publication, Society of Nuclear Medicine
https://www.readbyqxmd.com/read/28864614/somatostatin-receptor-antagonists-for-imaging-and-therapy
#15
Melpomeni Fani, Guillaume P Nicolas, Damian Wild
Somatostatin receptor (sstr) scintigraphy for imaging and sstr analogs for treatment have been used for more than 20 y. An important improvement in recent years was the introduction of peptide receptor radionuclide therapy with radiolabeled sstr agonists, such as [(90)Y-DOTA(0),Tyr(3)]octreotide or [(177)Lu-DOTA(0),Tyr(3)]octreotide ((90)Y- or (177)Lu-DOTATOC, respectively) and [(177)Lu-DOTA(0),Tyr(3)]octreotate ((177)Lu-DOTATATE). PET/CT with (68)Ga-labeled sstr agonists, such as (68)Ga-DOTATOC, (68)Ga-DOTATATE, and [(68)Ga-DOTA,1-Nal(3)]octreotide ((68)Ga-DOTANOC), plays an important role in staging and restaging neuroendocrine tumors...
September 2017: Journal of Nuclear Medicine: Official Publication, Society of Nuclear Medicine
https://www.readbyqxmd.com/read/28864020/pre-clinical-evaluation-of-a-nanoparticle-based-blood-pool-contrast-agent-for-mr-imaging-of-the-placenta
#16
Ketan B Ghaghada, Zbigniew A Starosolski, Saakshi Bhayana, Igor Stupin, Chandreshkumar V Patel, Rohan C Bhavane, Haijun Gao, Andrey Bednov, Chandrasekhar Yallampalli, Michael Belfort, Verghese George, Ananth V Annapragada
INTRODUCTION: Non-invasive 3D imaging that enables clear visualization of placental margins is of interest in the accurate diagnosis of placental pathologies. This study investigated if contrast-enhanced MRI performed using a liposomal gadolinium blood-pool contrast agent (liposomal-Gd) enables clear visualization of the placental margins and the placental-myometrial interface (retroplacental space). Non-contrast MRI and contrast-enhanced MRI using a clinically approved conventional contrast agent were used as comparators...
September 2017: Placenta
https://www.readbyqxmd.com/read/28861553/manota-a-promising-bifunctional-chelating-agent-for-copper-64-immunopet
#17
M Moreau, S Poty, J-M Vrigneaud, P Walker, M Guillemin, O Raguin, A Oudot, C Bernhard, C Goze, F Boschetti, B Collin, F Brunotte, F Denat
Improved bifunctional chelating agents (BFC) are required for copper-64 radiolabelling of monoclonal antibodies (mAbs) under mild conditions to yield stable, target-specific imaging agents. Four different bifunctional chelating agents (BFC) were evaluated for Fab (Fragment antigen binding) conjugation and radiolabelling with copper-64. Two DOTA- (1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid) and two NOTA- (1,4,7-triazacyclononane-1,4,7-triacetic acid) derivatives bearing a p-benzyl-isothiocyanate group were conjugated to Fab-trastuzumab - which targets the HER2/neu receptor - and the average number of chelators attached ranged from 2...
September 1, 2017: Dalton Transactions: An International Journal of Inorganic Chemistry
https://www.readbyqxmd.com/read/28856372/erratum-to-guideline-for-pet-ct-imaging-of-neuroendocrine-neoplasms-with-68-ga-dota-conjugated-somatostatin-receptor-targeting-peptides-and-18-f-dopa
#18
Murat Fani Bozkurt, Irene Virgolini, Sona Balogova, Mohsen Beheshti, Domenico Rubello, Clemens Decristoforo, Valentina Ambrosini, Andreas Kjaer, Roberto Delgado-Bolton, Jolanta Kunikowska, Wim J G Oyen, Arturo Chiti, Francesco Giammarile, Anders Sundin, Stefano Fanti
No abstract text is available yet for this article.
August 30, 2017: European Journal of Nuclear Medicine and Molecular Imaging
https://www.readbyqxmd.com/read/28856067/application-of-dendrimer-based-nanoparticles-in-glioma-imaging
#19
Sunalee Gonawala, Meser M Ali
Dendritic polymers or dendrimers present an alternate template for the development of nanoparticulate-based drug delivery and imaging systems. The smaller size (~7-12 nm) of dendrimers have the advantage over the other particles, because its smaller size can possibly improve tumor penetration and the inclusion of tumor specific drug release mechanisms. A Paramagnetic Chemical Exchange Saturation Transfer (PARACEST) MRI contrast agent, Eu-DOTA-Gly4 or a clinical relevant Gd-DOTA was conjugated on the surface of a G5 PAMAM dendrimer...
June 2017: Journal of Nanomedicine & Nanotechnology
https://www.readbyqxmd.com/read/28837117/preclinical-assessment-of-a-68-ga-dota-functionalized-depsipeptide-as-a-radiodiagnostic-infection-imaging-agent
#20
Thomas Ebenhan, Botshelo Brenda Mokaleng, Jacobus Daniel Venter, Hendrik Gert Kruger, Jan Rijn Zeevaart, Mike Sathekge
The study assessed a radiolabeled depsipeptide conjugate ((68)Ga-DOTA-TBIA101) for its potential as an imaging agent targeting infection or infection-associated inflammation. (68)Ga-labeled DOTA-TBIA101 imaging was performed in (NZR1) healthy rabbits; (NZR2) rabbits bearing muscular sterile inflammation and Staphylococcus aureus (SA) infection; and (NZR3) rabbits infected with Mycobacterium tuberculosis (MTB) combined with a subcutaneous scruff infection of SA in the same animal. All animals were imaged using a PET/CT scanner at 5 and 60 min post injection...
August 24, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
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