Metabolism of receptor targeted 111In-DTPA-glycoproteins: identification of 111In-DTPA-epsilon-lysine as the primary metabolic and excretory product.

Abstract:

:The hepatic and renal retention of indium-111 (111In) from 111In-labeled polypeptides has been the subject of many investigations. Because the lysosome is a common intracellular destination for the degradation of polypeptides, we studied the lysosomal metabolism of 111In-DTPA-labeled glycoproteins targeted to cell surface receptors in vitro and in vivo. We found that 111In-DTPA-glycoproteins were degraded to 111In-DTPA-epsilon-lysine, which was slowly released from cells and recovered intact in urine and feces. These results suggest a mechanism for 111In retention at target and non-target sites.

journal_name

Nucl Med Biol

authors

Franano FN,Edwards WB,Welch MJ,Duncan JR

doi

10.1016/0969-8051(94)90174-0

subject

Has Abstract

pub_date

1994-11-01 00:00:00

pages

1023-34

issue

8

eissn

0969-8051

issn

1872-9614

journal_volume

21

pub_type

杂志文章
  • In vitro evaluation, biodistribution and scintigraphic imaging in mice of radiolabeled anthrax toxins.

    abstract:INTRODUCTION:There is a lot of interest towards creating therapies and vaccines for Bacillus anthracis, a bacterium which causes anthrax in humans and which spores can be made into potent biological weapons. Systemic injection of lethal factor (LF), edema factor (EF) and protective antigen (PA) in mice produces toxicit...

    journal_title:Nuclear medicine and biology

    pub_type: 杂志文章

    doi:10.1016/j.nucmedbio.2008.07.001

    authors: Dadachova E,Rivera J,Revskaya E,Nakouzi A,Cahill SM,Blumenstein M,Xiao H,Rykunov D,Casadevall A

    更新日期:2008-10-01 00:00:00

  • Dopamine transporter imaging in the aged rat: a [¹²³I]FP-CIT SPECT study.

    abstract:INTRODUCTION:Rodent models are extensively used to assess the biochemical and physiological changes associated with aging. They play a major role in the development of therapies for age-related pathologies such as Parkinson's disease. To validate the usefulness of these animal models in aging or age-related disease res...

    journal_title:Nuclear medicine and biology

    pub_type: 杂志文章

    doi:10.1016/j.nucmedbio.2014.12.020

    authors: Niñerola-Baizán A,Rojas S,Roé-Vellvé N,Lomeña F,Ros D,Pavía J

    更新日期:2015-04-01 00:00:00

  • 18F-labeled norepinephrine transporter tracer [18F]NS12137: radiosynthesis and preclinical evaluation.

    abstract:INTRODUCTION:Several psychiatric and neurodegenerative diseases are associated with malfunction of brain norepinephrine transporter (NET). However, current clinical evaluations of NET function are limited by the lack of sufficiently sensitive methods of detection. To this end, we have synthesized exo-3-[(6-[18F]fluoro-...

    journal_title:Nuclear medicine and biology

    pub_type: 杂志文章

    doi:10.1016/j.nucmedbio.2017.10.005

    authors: Kirjavainen AK,Forsback S,López-Picón FR,Marjamäki P,Takkinen J,Haaparanta-Solin M,Peters D,Solin O

    更新日期:2018-01-01 00:00:00

  • A bolus/infusion paradigm for the novel NMDA receptor SPET tracer [123I]CNS 1261.

    abstract::We have previously performed quantitative kinetic modeling of [(123)I]CNS 1261, a new SPET ligand for the MK801 intrachannel site of the NMDA receptor. We now report a bolus-infusion protocol, which eliminates the need for arterial blood sampling. Dynamic SPET scanning and venous blood sampling were performed in 7 hea...

    journal_title:Nuclear medicine and biology

    pub_type: 临床试验,杂志文章

    doi:10.1016/j.nucmedbio.2003.08.008

    authors: Bressan RA,Erlandsson K,Mulligan RS,Gunn RN,Cunningham VJ,Owens J,Cullum ID,Ell PJ,Pilowsky LS

    更新日期:2004-02-01 00:00:00

  • 18F-fluorodeoxyglucose positron emission tomography in management of pancreatic cystic tumors.

    abstract:OBJECTIVES:To evaluate the effectiveness of PET in differentiating malignant from benign pancreatic cystic tumors. METHODS:Between 2009 and 2010, all patients with pancreatic cystic tumors who had PET, triple phase contrast computed tomography (CT) and endoscopic ultrasound (EUS) were reviewed. Clinicopathological cha...

    journal_title:Nuclear medicine and biology

    pub_type: 杂志文章

    doi:10.1016/j.nucmedbio.2012.03.005

    authors: Zhang Y,Frampton AE,Martin JL,Kyriakides C,Bong JJ,Habib NA,Vlavianos P,Jiao LR

    更新日期:2012-10-01 00:00:00

  • Preparation and investigation of tumor affinity, uptake kinetic and transport mechanism of iodine-123-labelled amino acid derivatives in human pancreatic carcinoma and glioblastoma cells.

    abstract::In developing radioiodinated agents for pancreatic and brain tumor imaging by single photon emission tomography (SPET), we prepared p-amino-3-[123I]iodo-l-phenylalanine (IAPA), p-[123I]iodo-l-phenylalanine (IPA), L-8-[123I]iodo-1,2,3,4-tetrahydro-7-hydroxyisoquinoline-3-carboxylic acid (ITIC) and L-3-[123I]iodo-alpha-...

    journal_title:Nuclear medicine and biology

    pub_type: 杂志文章

    doi:10.1016/s0969-8051(00)00176-1

    authors: Samnick S,Schaefer A,Siebert S,Richter S,Vollmar B,Kirsch CM

    更新日期:2001-01-01 00:00:00

  • Sequence-specific binding and cleavage of duplex DNA by a radioiodinated, intercalator-linked, triplex-forming oligonucleotide.

    abstract::Applications of oligodeoxynucleotides to modulate gene expression have been the subject of much recent research. We have sought to develop a method to permanently inactivate a gene, or potentially kill cells containing abnormal genes. In this report, we show that a DNA intercalator conjugated to a triplex-forming olig...

    journal_title:Nuclear medicine and biology

    pub_type: 杂志文章

    doi:10.1016/0969-8051(96)00034-0

    authors: Orson FM,McShan WM,Kinsey BM

    更新日期:1996-05-01 00:00:00

  • Optimal scanning time window for 18F-FP-(+)-DTBZ (18F-AV-133) summed uptake measurements.

    abstract:UNLABELLED:(18)F-9-fluoropropyl-(+)-dihydrotetrabenazine ((18)F-AV-133) is a novel positron emission tomography tracer for imaging the vesicular monoamine transporter II in dopaminergic neuron degeneration, which might be indicative for Parkinson's disease (PD) and other parkinsonism. Studies were performed to optimize...

    journal_title:Nuclear medicine and biology

    pub_type: 杂志文章

    doi:10.1016/j.nucmedbio.2011.05.010

    authors: Lin KJ,Lin WY,Hsieh CJ,Weng YH,Wey SP,Lu CS,Skovronsky D,Yen TC,Chang CJ,Kung MP,Hsiao IT

    更新日期:2011-11-01 00:00:00

  • Animal-specific positioning molds for registration of repeat imaging studies: comparative microPET imaging of F18-labeled fluoro-deoxyglucose and fluoro-misonidazole in rodent tumors.

    abstract:INTRODUCTION:Comparative imaging of multiple radiotracers in the same animal can be invaluable in elucidating and validating their respective mechanisms of localization. Comparative imaging of PET tracers, particularly in small animals, is problematic, however: such tracers must be administered and imaged separately be...

    journal_title:Nuclear medicine and biology

    pub_type: 杂志文章

    doi:10.1016/j.nucmedbio.2005.07.011

    authors: Zanzonico P,Campa J,Polycarpe-Holman D,Forster G,Finn R,Larson S,Humm J,Ling C

    更新日期:2006-01-01 00:00:00

  • Preclinical evaluation of (99m)Tc labeled chondroitin sulfate for monitoring of cartilage degeneration in osteoarthritis.

    abstract:PURPOSE:In previous in-vitro and ex-vivo studies we proved the specific uptake of (99m)Tc radiolabeled chondroitin sulfate (CS) in human articular cartilage. As a logical next step for the clinical use for imaging osteoarthritis we investigated in-vivo uptake of (99m)TcCS in dogs. PROCEDURES:The radiolabeling of CS Co...

    journal_title:Nuclear medicine and biology

    pub_type: 杂志文章

    doi:10.1016/j.nucmedbio.2016.02.009

    authors: Sobal G,Velusamy K,Kosik S,Menzel J,Hacker M,Pagitz M

    更新日期:2016-06-01 00:00:00

  • The human polynucleotide kinase/phosphatase (hPNKP) inhibitor A12B4C3 radiosensitizes human myeloid leukemia cells to Auger electron-emitting anti-CD123 ¹¹¹In-NLS-7G3 radioimmunoconjugates.

    abstract:INTRODUCTION:Leukemia stem cells (LSCs) are believed to be responsible for initiating and propagating acute myeloid leukemia (AML) and for causing relapse after treatment. Radioimmunotherapy (RIT) targeting these cells may improve the treatment of AML, but is limited by the low density of target epitopes. Our objective...

    journal_title:Nuclear medicine and biology

    pub_type: 杂志文章

    doi:10.1016/j.nucmedbio.2014.02.003

    authors: Zereshkian A,Leyton JV,Cai Z,Bergstrom D,Weinfeld M,Reilly RM

    更新日期:2014-05-01 00:00:00

  • Use of PET and the radioligand [carbonyl-(11)C]WAY-100635 in psychotropic drug development.

    abstract::Positron-emission tomography (PET) provides potential in neuropsychiatric drug development by expanding knowledge of drug action in the living human brain and reducing time consumption and costs. The 5-hydroxytryptamine(1A) (5-HT(1A)) receptor is of central interest as a target for the treatment of anxiety, depression...

    journal_title:Nuclear medicine and biology

    pub_type: 杂志文章

    doi:10.1016/s0969-8051(00)00121-9

    authors: Andrée B,Halldin C,Thorberg SO,Sandell J,Farde L

    更新日期:2000-07-01 00:00:00

  • A new nucleophilic fluorine-18 labeling method for aliphatic mesylates: reaction in ionic liquids shows tolerance for water.

    abstract::[see text for equation] Nucleophilic [(18)F]fluorination of some halo- and mesyloxyalkanes to the corresponding [(18)F]fluoroalkanes with fluoride-18 obtained from an (18)O(p,n) [(18)F]F reaction, using an ionic liquid as a reaction medium, has been studied as a new method for fluorine-18 labeling. Of the various ioni...

    journal_title:Nuclear medicine and biology

    pub_type: 杂志文章

    doi:10.1016/s0969-8051(03)00017-9

    authors: Kim DW,Choe YS,Chi DY

    更新日期:2003-05-01 00:00:00

  • First-pass studies of acute lung injury.

    abstract::Mild hydrochloric acid was introduced to a caudal lung section in each of eight dogs to induce injury. Transits of 99mTc-labeled red blood cells (RBC) and [123I]iodoantipyrine (IAP) injected intravenously were recorded by a scintillation camera. Lungs and blood samples were analyzed post-mortem. Peak-to-equilibrium ra...

    journal_title:Nuclear medicine and biology

    pub_type: 杂志文章

    doi:10.1016/0969-8051(93)90154-m

    authors: Chu RY,Sidhu N,Basmadjian G,Burow R,Allen EW

    更新日期:1993-10-01 00:00:00

  • Synthesis and evaluation of benzothiophene derivatives as ligands for imaging beta-amyloid plaques in Alzheimer's disease.

    abstract::The imaging of the distribution of beta-amyloid (Abeta) plaques in the brain is becoming an important diagnostic modality in Alzheimer's disease (AD). Here, we synthesized novel benzothiophene derivatives and labeled them with (18)F for the potential diagnostic imaging of AD patients using positron emission tomography...

    journal_title:Nuclear medicine and biology

    pub_type: 杂志文章

    doi:10.1016/j.nucmedbio.2006.06.006

    authors: Chang YS,Jeong JM,Lee YS,Kim HW,Ganesha RB,Kim YJ,Lee DS,Chung JK,Lee MC

    更新日期:2006-08-01 00:00:00

  • Comparison of the distribution of radioiodinated di- and tri-hydroxyphenylethylene estrogens in the immature female rat.

    abstract::The uptake, retention and tissue to blood ratios of two non-steroidal, 125I-labeled iodoestrogens, an iodotrihydroxyphenylethylene, 2-iodo-1,2-bis(4-hydroxyphenyl)-2-(3-hydroxyphenyl)ethylene and an iododihydroxyphenylethylene, 2-iodo-1,1-bis(4-hydroxyphenyl)-2-phenylethylene, were compared after intraperitoneal injec...

    journal_title:Nuclear medicine and biology

    pub_type: 杂志文章

    doi:10.1016/0969-8051(95)00002-f

    authors: Desombre ER,Pribish J,Hughes A

    更新日期:1995-07-01 00:00:00

  • Evaluation of nigrostriatal damage and its change over weeks in a rat model of Parkinson's disease: small animal positron emission tomography studies with [(11)C]beta-CFT.

    abstract:INTRODUCTION:The cardinal pathological feature of Parkinson's disease (PD) is progressive loss of dopaminergic neurons. Since dopamine transporter (DAT) is a protein located presynaptically on dopaminergic nerve terminals, radioligands that bind to these sites are promising radiopharmaceuticals for evaluation of the in...

    journal_title:Nuclear medicine and biology

    pub_type: 杂志文章

    doi:10.1016/j.nucmedbio.2009.06.005

    authors: Liu L,Wang Y,Li B,Jia J,Sun Z,Zhang J,Tian J,Wang X

    更新日期:2009-11-01 00:00:00

  • Comparison of (18)F-FET and (18)F-FLT small animal PET for the assessment of anti-VEGF treatment response in an orthotopic model of glioblastoma.

    abstract:BACKGROUND:The radiolabeled amino acid O-(2-(18)F-fluoroethyl)-L-tyrosine (FET) and thymidine analogue 3'-deoxy-3'-(18)F-fluorothymidine (FLT) are widely used for positron emission tomography (PET) brain tumor imaging; however, comparative studies are scarce. The aim of this study therefore was to compare FLT and FET P...

    journal_title:Nuclear medicine and biology

    pub_type: 杂志文章

    doi:10.1016/j.nucmedbio.2015.12.002

    authors: Nedergaard MK,Michaelsen SR,Perryman L,Erler J,Poulsen HS,Stockhausen MT,Lassen U,Kjaer A

    更新日期:2016-03-01 00:00:00

  • A strategy for increasing the brain uptake of a radioligand in animals: use of a drug that inhibits plasma protein binding.

    abstract::A positron-emitter labeled radioligand for the glycine-binding site of the N-methyl-D-aspartate (NMDA) receptor, [(11)C]L-703,717, was examined for its ability to penetrate the brain in animals by simultaneous use with drugs having high-affinity separate binding sites on human serum albumin. [(11)C]L-703,717 has poor ...

    journal_title:Nuclear medicine and biology

    pub_type: 杂志文章

    doi:10.1016/s0969-8051(00)00096-2

    authors: Haradahira T,Zhang M,Maeda J,Okauchi T,Kawabe K,Kida T,Suzuki K,Suhara1 T

    更新日期:2000-05-01 00:00:00

  • Synthesis of an I-123 analog of A-85380 and preliminary SPECT imaging of nicotinic receptors in baboon.

    abstract::A radiosynthetic method to prepare the nicotinic acetylcholine receptor radioligand (S)-5-[123I]iodo-3-(2-azetidinylmethoxy)pyridine, 5-IA, has been developed. The two-step sequence produced [123I]-5-IA in high radiochemical yield (52%), high radiochemical purity (98%), and high specific radioactivities (> 8,500 mCi/m...

    journal_title:Nuclear medicine and biology

    pub_type: 杂志文章

    doi:10.1016/s0969-8051(98)00101-2

    authors: Musachio JL,Villemagne VL,Scheffel UA,Dannals RF,Dogan AS,Yokoi F,Wong DF

    更新日期:1999-02-01 00:00:00

  • Current trends in the use of O-(2-[18F]fluoroethyl)-L-tyrosine ([18F]FET) in neurooncology.

    abstract::The diagnostic potential of PET using the amino acid analogue O-(2-[18F]fluoroethyl)-L-tyrosine ([18F]FET) in brain tumor diagnostics has been proven in many studies during the last two decades and is still the subject of multiple studies every year. In addition to standard magnetic resonance imaging (MRI), positron e...

    journal_title:Nuclear medicine and biology

    pub_type: 杂志文章,评审

    doi:10.1016/j.nucmedbio.2020.02.006

    authors: Stegmayr C,Stoffels G,Filß C,Heinzel A,Lohmann P,Willuweit A,Ermert J,Coenen HH,Mottaghy FM,Galldiks N,Langen KJ

    更新日期:2020-02-19 00:00:00

  • Synthesis, characterization and theranostic evaluation of Indium-111 labeled multifunctional superparamagnetic iron oxide nanoparticles.

    abstract::Indium-111 labeled, Trastuzumab-Doxorubicin Conjugated, and APTES-PEG coated magnetic nanoparticles were designed for tumor targeting, drug delivery, controlled drug release, and dual-modal tumor imaging. Superparamagnetic iron oxide nanoparticles (SPIONs) were synthesized by thermal decomposition method to obtain nar...

    journal_title:Nuclear medicine and biology

    pub_type: 杂志文章

    doi:10.1016/j.nucmedbio.2014.09.007

    authors: Zolata H,Abbasi Davani F,Afarideh H

    更新日期:2015-02-01 00:00:00

  • 131I-labeled chitosan hydrogels for radioembolization: A preclinical study in small animals.

    abstract:INTRODUCTION:The purpose of the study was to examine potential of 131I-labeled chitosan hydrogels (Chi) for treatment of liver cancer. METHODS:Orthotopic hepatoma was induced by McA-RH7777-fLuc cells (1×107) that were injected into the left hepatic lobe of rats. Ten days later, tumor-bearing rats evidenced by biolumin...

    journal_title:Nuclear medicine and biology

    pub_type: 杂志文章

    doi:10.1016/j.nucmedbio.2017.05.006

    authors: Hwang H,Kim KI,Kwon J,Kim BS,Jeong HS,Jang SJ,Oh PS,Park HS,Lim ST,Sohn MH,Jeong HJ

    更新日期:2017-09-01 00:00:00

  • Cellular distribution of 111In-LDTPA galactose BSA in normal and asialoglycoprotein receptor-deficient mouse liver.

    abstract::111In-LDTPA galactose BSA (bovine serum albumin) was used to evaluate the asialoglycoprotein receptor (ASGPR) system in both normal and ASGPR-deficient mice. The radiolabeled glycoprotein had complete liver uptake in both normal and ASGPR-deficient mice. Metabolism and hepatic cell-type distribution studies were perfo...

    journal_title:Nuclear medicine and biology

    pub_type: 杂志文章

    doi:10.1016/s0969-8051(97)00222-9

    authors: Deal KA,Cristel ME,Welch MJ

    更新日期:1998-05-01 00:00:00

  • Development of rapid multistep carbon-11 radiosynthesis of the myeloperoxidase inhibitor AZD3241 to assess brain exposure by PET microdosing.

    abstract:INTRODUCTION:The myeloperoxidase inhibitor AZD3241 has been selected as a candidate drug currently being developed to delay progression in patients with neurodegenerative brain disorders. Part of the decision tree for translation of AZD3241 into clinical studies included the need for assessment of brain exposure in non...

    journal_title:Nuclear medicine and biology

    pub_type: 杂志文章

    doi:10.1016/j.nucmedbio.2015.02.001

    authors: Johnström P,Bergman L,Varnäs K,Malmquist J,Halldin C,Farde L

    更新日期:2015-06-01 00:00:00

  • A study on nitroimidazole-99mTc(CO)3 complexes as hypoxia marker: some observations towards possible improvement in in vivo efficacy.

    abstract:INTRODUCTION:Hypoxia plays a negative role in the clinical management of cancer. Detection of hypoxic status of a cancer is important for selecting patients for hypoxia directed therapy. Though [(18)F]fluoromisonidazole ([(18)F]FMISO), a PET radiopharmaceutical, is presently being used in the clinic for the detection o...

    journal_title:Nuclear medicine and biology

    pub_type: 杂志文章

    doi:10.1016/j.nucmedbio.2014.04.103

    authors: Mallia MB,Subramanian S,Mathur A,Sarma HD,Banerjee S

    更新日期:2014-08-01 00:00:00

  • Synthesis and in vitro examination of [124I]-, [125I]- and [131I]-2-(4-iodophenylamino) pyrido[2,3-d]pyrimidin-7-one radiolabeled Abl kinase inhibitors.

    abstract::The pyridopyrimidinones are a potent class of inhibitors of c-Abl kinase and Bcr-Abl kinase, the causative fusion protein in chronic myelogenous leukemia and Src family kinases. A novel method for routine, high-yield no-carrier-added synthesis of [(124)I]-, [(125)I]- and [(131)I]-6-(2,6-dichlorophenyl)-2-(4-iodophenyl...

    journal_title:Nuclear medicine and biology

    pub_type: 杂志文章

    doi:10.1016/j.nucmedbio.2005.01.008

    authors: Veach DR,Namavari M,Beresten T,Balatoni J,Minchenko M,Djaballah H,Finn RD,Clarkson B,Gelovani JG,Bornmann WG,Larson SM

    更新日期:2005-05-01 00:00:00

  • G2M arrest and apoptosis in murine T lymphoma cells following exposure to 212Bi alpha particle irradiation.

    abstract::Asynchronous exponentially growing EL4 murine T lymphoma cells were exposed either to high LET alpha-radiation from 212Bi-DTPA or to gamma-radiation from a 137Cs source. Radiation-induced cell cycle perturbation was studied by flow cytometry. Alpha irradiation, like gamma, transiently arrested cells in the G2M phase i...

    journal_title:Nuclear medicine and biology

    pub_type: 杂志文章

    doi:10.1016/0969-8051(93)90166-r

    authors: Palayoor ST,Humm JL,Atcher RW,Hines JJ,Macklis RM

    更新日期:1993-08-01 00:00:00

  • Imaging recognition of multidrug resistance in human breast tumors using 99mTc-labeled monocationic agents and a high-resolution stationary SPECT system.

    abstract::Imaging recognition of multidrug-resistance by 99mTc-labeled sestamibi, tetrofosmin and furifosmin in mice bearing human breast tumors was evaluated using a high-resolution SPECT, FASTSPECT. Imaging results showed that the washout rates in drug-resistant MCF7/D40 tumors were significantly greater than that in drug-sen...

    journal_title:Nuclear medicine and biology

    pub_type: 杂志文章

    doi:10.1016/s0969-8051(03)00119-7

    authors: Liu Z,Stevenson GD,Barrett HH,Kastis GA,Bettan M,Furenlid LR,Wilson DW,Woolfenden JM

    更新日期:2004-01-01 00:00:00

  • Radiochemical synthesis and in vivo evaluation of [18F]AZ11637326: an agonist probe for the α7 nicotinic acetylcholine receptor.

    abstract:INTRODUCTION:The alpha-7 nicotinic acetylcholine receptor (α7 nAChR) is key in brain communication and has been implicated in the pathophysiology of diseases of the central nervous system. A positron-emitting radioligand targeting the α7 nAChR would enable better understanding of a variety of neuropsychiatric illnesses...

    journal_title:Nuclear medicine and biology

    pub_type: 杂志文章

    doi:10.1016/j.nucmedbio.2013.04.005

    authors: Ravert HT,Dorff P,Foss CA,Mease RC,Fan H,Holmquist CR,Phillips E,McCarthy DJ,Heys JR,Holt DP,Wang Y,Endres CJ,Dannals RF,Pomper MG

    更新日期:2013-08-01 00:00:00