当前位置： SCI文献检索 > NUCLEAR MEDICINE AND BIOLOGY期刊下所有文献 > Backbone metal-cyclization: a novel approach for simultaneous peptide cyclization and radiolabeling. Application to the combinatorial synthesis of rhenium-cyclic somatostatin analogs.

Backbone metal-cyclization: a novel approach for simultaneous peptide cyclization and radiolabeling. Application to the combinatorial synthesis of rhenium-cyclic somatostatin analogs.

Abstract：

:A novel approach for the combinatorial synthesis of backbone-derived metal-cyclic peptide libraries is presented. In this approach the metalo-cyclic peptides are prepared from their linear precursors through complexation of a metal atom via two hemi-chelating arms located on the peptide backbone. Thus, cyclization and metal labeling of the peptides are achieved simultaneously. A library, composed of 48 rhenium-cyclic somatostatin analogs, was prepared. All rhenium somatostatin complexes exhibited high to moderate in vitro binding affinities toward cloned human somatostatin receptor subtype 2 (hsstr2). Five rhenium-cyclic peptides were found to be most potent with IC50 values between 1 and 3 nM making them promising leads for further development of tumor diagnostic and therapeutic radiolabeled agents. A 99mTc somatostatin cyclic analog was successfully prepared by the same method.

journal_name

Nucl Med Biol

journal_title

Nuclear medicine and biology

authors

Fridkin G,Bonasera TA,Litman P,Gilon C

doi

10.1016/j.nucmedbio.2004.08.007

keywords:

subject

Has Abstract

pub_date

2005-01-01 00:00:00

pages

39-50

issue

1

eissn

0969-8051

issn

1872-9614

pii

S0969-8051(04)00128-3

journal_volume

32

pub_type

杂志文章

相关文献

NUCLEAR MEDICINE AND BIOLOGY文献大全
  • 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

  • Effect of the EGFR density of breast cancer cells on nuclear importation, in vitro cytotoxicity, and tumor and normal-tissue uptake of [111In]DTPA-hEGF.

    abstract：INTRODUCTION:Our objective was to evaluate the effect of epidermal growth factor receptor(s) (EGFR) density on the importation and nuclear localization of 111In-labeled diethylenetriaminepentaacetic acid human epidermal growth factor ([111In]DTPA-hEGF) in breast cancer (BC) cells in vitro and in tumor xenografts and no...

    journal_title：Nuclear medicine and biology

    pub_type： 杂志文章

    doi：10.1016/j.nucmedbio.2007.06.010

    authors： Hu M,Scollard D,Chan C,Chen P,Vallis K,Reilly RM

    更新日期：2007-11-01 00:00:00

  • Exploration of the impact of stereochemistry on the identification of the novel translocator protein PET imaging agent [(18)F]GE-180.

    abstract：INTRODUCTION:The tricyclic indole compound, [(18)F]GE-180 has been previously identified as a promising positron emission tomography (PET) imaging agent of the translocator protein (TSPO) with the potential to aid in the diagnosis, prognosis and therapy monitoring of degenerative neuroinflammatory conditions such as mu...

    journal_title：Nuclear medicine and biology

    pub_type： 杂志文章

    doi：10.1016/j.nucmedbio.2015.05.004

    authors： Chau WF,Black AM,Clarke A,Durrant C,Gausemel I,Khan I,Mantzilas D,Oulie I,Rogstad A,Trigg W,Jones PA

    更新日期：2015-09-01 00:00:00

  • Synthesis and in vivo brain distribution of carbon-11-labeled δ-opioid receptor agonists.

    abstract：:Three new radiolabeled compounds, [(11)C]SNC80 ((+)-4-[(αR)-α-{(2S,5R)-4-allyl-2,5-dimethyl-1-piperazinyl}-3-[(11)C]methoxybenzyl-N,N-diethylbenzamide), N,N-diethyl-4-[3-methoxyphenyl-1-[(11)C]methylpiperidin-4-ylidenemethyl)benzamide and N,N-diethyl-4-[(1-[(11)C]methylpiperidin-4-ylidene)phenylmethyl]benzamide, were ...

    journal_title：Nuclear medicine and biology

    pub_type： 杂志文章

    doi：10.1016/j.nucmedbio.2010.06.002

    authors： Pichika R,Jewett DM,Sherman PS,Traynor JR,Husbands SM,Woods JH,Kilbourn MR

    更新日期：2010-11-01 00:00:00

  • In vivo inhibition of neutral endopeptidase enhances the diagnostic potential of truncated gastrin (111)In-radioligands.

    abstract：INTRODUCTION:Radiolabeled gastrin analogs represent attractive candidates for diagnosis and therapy of cholecystokinin subtype-2 receptor (CCK2R)-expressing tumors. Radiolabeled des(Glu)5-gastrins show favorably low renal accumulation, but localize poorly in CCK2R-positive lesions. We introduce herein three truncated [...

    journal_title：Nuclear medicine and biology

    pub_type： 杂志文章

    doi：10.1016/j.nucmedbio.2015.07.009

    authors： Kaloudi A,Nock BA,Lymperis E,Sallegger W,Krenning EP,de Jong M,Maina T

    更新日期：2015-11-01 00:00:00

  • (E)-[125I]-5-AOIBV: a SPECT radioligand for the vesicular acetylcholine transporter.

    abstract：:The premise that, over the course of Alzheimer's disease (AD), changes in the levels of the vesicular acetylcholine transporter (VAChT) occur in parallel with changes to other cholinergic marker proteins provides the basis for the applicability of benzovesamicol derivatives as radioligands for AD studies by single pho...

    journal_title：Nuclear medicine and biology

    pub_type： 杂志文章

    doi：10.1016/j.nucmedbio.2007.07.011

    authors： Emond P,Mavel S,Zea-Ponce Y,Kassiou M,Garreau L,Bodard S,Drossard ML,Chalon S,Guilloteau D

    更新日期：2007-11-01 00:00:00

  • Evaluation of F-18-labeled 5-iodocytidine (18F-FIAC) as a new potential positron emission tomography probe for herpes simplex virus type 1 thymidine kinase imaging.

    abstract：OBJECTIVE:Herpes simplex virus type 1 thymidine kinase (HSV1-tk) gene in combination with radiolabeled nucleoside substrates is the most widely used reporter system. This study characterized 1-(2'-deoxy-2'-[(18)F]fluoro-β-D-arabinofuranosyl)-5-iodocytosine ((18)F-FIAC) as a new potential positron emission tomography (P...

    journal_title：Nuclear medicine and biology

    pub_type： 杂志文章

    doi：10.1016/j.nucmedbio.2011.04.003

    authors： Chan PC,Wu CY,Chang WY,Chang WT,Alauddin M,Liu RS,Lin WJ,Chen FD,Chen CL,Wang HE

    更新日期：2011-10-01 00:00:00

  • 65Zn uptake by liver of rats fed 3'-methyl-dimethylaminoazobenzene.

    abstract：:The uptake of 65Zn, determined by gamma-counting and also by autoradiography, significantly increased with the increasing level of metallothionein in liver 4 weeks after the start of feeding a diet containing 3'-methyl-dimethylaminoazobenzene (3'-Me-DAB), at which time the serum gamma-glutamyl transpeptidase activity ...

    journal_title：Nuclear medicine and biology

    pub_type： 杂志文章

    doi：10.1016/0969-8051(94)00102-p

    authors： Takeda A,Tamano H,Ohnuma M,Okada S

    更新日期：1995-04-01 00:00:00

  • Improved xenograft targeting of tumor-specific anti-epidermal growth factor receptor variant III antibody labeled using N-succinimidyl 4-guanidinomethyl-3-iodobenzoate.

    abstract：:Monoclonal antibodies (mAbs) such as the tumor-specific anti-epidermal growth factor receptor variant III (EGFRvIII) that are internalized and degraded after cell binding necessitate the use of radioiodination methods that minimize the loss of radioactivity from the tumor cell after intracellular processing. The purpo...

    journal_title：Nuclear medicine and biology

    pub_type： 杂志文章

    doi：10.1016/s0969-8051(01)00277-3

    authors： Vaidyanathan G,Affleck DJ,Bigner DD,Zalutsky MR

    更新日期：2002-01-01 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

  • Cellular penetration and nuclear importation properties of 111In-labeled and 123I-labeled HIV-1 tat peptide immunoconjugates in BT-474 human breast cancer cells.

    abstract：INTRODUCTION:Our objective was to compare the cell penetration and nuclear importation properties of 111In-labeled and 123I-labeled immunoconjugates (ICs) composed of 16-mer peptides (GRKKRRQRRRPPQGYG) derived from HIV-1 transactivator of transcription (tat) protein and anti-mouse IgG (mIgG) in BT-474 breast cancer (BC...

    journal_title：Nuclear medicine and biology

    pub_type： 杂志文章

    doi：10.1016/j.nucmedbio.2006.10.008

    authors： Cornelissen B,Hu M,McLarty K,Costantini D,Reilly RM

    更新日期：2007-01-01 00:00:00

  • Kinetic parameters of 3-[(123)I]iodo-L-alpha-methyl tyrosine ([(123)I]IMT) transport in human GOS3 glioma cells.

    abstract：:The radiolabelled amino acid 3-[(123)I]iodo-L-alpha-methyl tyrosine ([(123)I]IMT) is a promising tool for the diagnosis and monitoring of brain tumors using single-photon emission tomography (SPECT). However, little is known about the precise kinetics of [(123)I]IMT uptake in human glioma cells. The kinetic analysis o...

    journal_title：Nuclear medicine and biology

    pub_type： 杂志文章

    doi：10.1016/s0969-8051(01)00191-3

    authors： Riemann B,Kopka K,Stögbauer F,Halfter H,Ketteler S,Phan TQ,Franzius C,Weckesser M,Ringelstein EB,Schober O

    更新日期：2001-04-01 00:00:00

  • ScVEGF-PEG-HBED-CC and scVEGF-PEG-NOTA conjugates: comparison of easy-to-label recombinant proteins for [68Ga]PET imaging of VEGF receptors in angiogenic vasculature.

    abstract：INTRODUCTION:VEGF receptors play a key role in angiogenesis and are important targets for several approved and many experimental drugs. Imaging of VEGF receptor expression in malignant tumors would provide important information, which can influence patient management. The aim of this study was the development of an eas...

    journal_title：Nuclear medicine and biology

    pub_type： 杂志文章

    doi：10.1016/j.nucmedbio.2010.02.001

    authors： Eder M,Krivoshein AV,Backer M,Backer JM,Haberkorn U,Eisenhut M

    更新日期：2010-05-01 00:00:00

  • A change of in vivo characteristics depending on specific activity of radioiodinated (+)-2-[4-(4-iodophenyl)piperidino]cyclohexanol [(+)-pIV] as a ligand for sigma receptor imaging.

    abstract：:The radioiodinated (+)-p-iodovesamicol [(+)-pIV], which shows a high binding affinity for sigma-1 (sigma-1) receptors, is prepared by an exchange reaction. The specific activity (SA) is fairly low and therefore is insufficient for clinical use. In this study, we prepared (+)-[(125)I]pIV with a high SA from tributylsta...

    journal_title：Nuclear medicine and biology

    pub_type： 杂志文章

    doi：10.1016/j.nucmedbio.2007.09.005

    authors： Akhter N,Shiba K,Ogawa K,Tsuji S,Kinuya S,Nakajima K,Mori H

    更新日期：2008-01-01 00:00:00

  • A comprehensive study on the blockage of thyroid and gastric uptakes of 188Re-perrhenate in endovascular irradiation using liquid-filled balloon to prevent restenosis.

    abstract：:188Re-perrhenate has been reported effective in preventing restenosis after percutaneous transluminal coronary angioplasty. However, if the balloon ruptures, 188Re-perrhenate is released into the circulation, causing high radiation dosing to the thyroid and stomach. In this study, we evaluated the effects of perchlora...

    journal_title：Nuclear medicine and biology

    pub_type： 杂志文章

    doi：10.1016/s0969-8051(99)00079-7

    authors： Lin WY,Hsieh JF,Tsai SC,Yen TC,Wang SJ,Knapp FF Jr

    更新日期：2000-01-01 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

  • Biological studies of radiolabeled glucose analogues iodinated in positions 3, 4 or 6.

    abstract：:The aim of this study was to assess the biological behavior of new radiolabeled glucose analogues proposed as tracers of glucose uptake in vivo and iodinated in position 3, 4, or 6. Biological results obtained in vitro on adipocytes and erythrocytes and in vivo in mice were compared to those obtained with the gold-sta...

    journal_title：Nuclear medicine and biology

    pub_type： 杂志文章

    doi：10.1016/j.nucmedbio.2003.08.009

    authors： Perret P,Ghezzi C,Ogier L,Abbadi M,Morin C,Mathieu JP,Fagret D

    更新日期：2004-02-01 00:00:00

  • PET imaging of dopamine transporters with [(18)F]FE-PE2I: Effects of anti-Parkinsonian drugs.

    abstract：PURPOSE:This study aimed to assess the striatal [(18)F]FE-PE2I binding and the immunohistochemical stain of tyrosine hydroxylase (TH) in the striatum, and to evaluate the effects of therapeutic drugs on [(18)F]FE-PE2I binding. METHODS:Dynamic PET/CT of [(18)F]FE-PE2I was performed in Parkinson's disease (PD) rat model...

    journal_title：Nuclear medicine and biology

    pub_type： 杂志文章

    doi：10.1016/j.nucmedbio.2015.11.002

    authors： Bang JI,Jung IS,Song YS,Park HS,Moon BS,Lee BC,Kim SE

    更新日期：2016-02-01 00:00:00

  • A comparative evaluation of the chelators H4octapa and CHX-A″-DTPA with the therapeutic radiometal (90)Y.

    abstract：OBJECTIVES:To compare the radiolabeling performance, stability, and practical efficacy of the chelators CHX-A″-DTPA and H4octapa with the therapeutic radiometal (90)Y. METHODS:The bifunctional chelators p-SCN-Bn-H4octapa and p-SCN-Bn-CHX-A″-DTPA were conjugated to the HER2-targeting antibody trastuzumab. The resulting...

    journal_title：Nuclear medicine and biology

    pub_type： 杂志文章

    doi：10.1016/j.nucmedbio.2016.06.004

    authors： Price EW,Edwards KJ,Carnazza KE,Carlin SD,Zeglis BM,Adam MJ,Orvig C,Lewis JS

    更新日期：2016-09-01 00:00:00

  • Synthesis of L-2,4-diamino[4-11C]butyric acid and its use in some in vitro and in vivo tumour models.

    abstract：:L-2,4-Diamino[4-11C]butyric acid (DAB) was synthesized by an enzyme catalysed carrier added (0.1 micromol KCN) reaction of hydrogen [11C]cyanide with O-acetyl-L-serine followed by reduction. L-[11C]DAB was obtained with a radiochemical purity higher than 96% and with a decay corrected radiochemical yield of 30-40% wit...

    journal_title：Nuclear medicine and biology

    pub_type： 杂志文章

    doi：10.1016/s0969-8051(97)00032-2

    authors： Antoni G,Omura H,Bergström M,Furuya Y,Moulder R,Roberto A,Sundin A,Watanabe Y,Långström B

    更新日期：1997-08-01 00:00:00

  • Decreased kidney uptake of technetium-99m-labelled Fab' fragments in ovarian carcinoma bearing nude mice using a cleavable chelator.

    abstract：:A new 99mTc labelling method using a cleavable chelator, RP-1, was developed. In this study Balb/c mice with ovarian carcinoma xenografts received various Fab' fragments labelled with 99mTc either directly or via RP-1. Kidney uptake was significantly lower for the RP-1 linked conjugates. Tumour uptake showed no signif...

    journal_title：Nuclear medicine and biology

    pub_type： 杂志文章

    doi：10.1016/0969-8051(94)90125-2

    authors： Tibben JG,Massuger LF,Boerman OC,Claessens RA,Borm GF,Pak KY,Koenders EB,Corstens FH

    更新日期：1994-01-01 00:00:00

  • An alumina ceramic target vessel for the remote production of metallic radionuclides by in situ target dissolution.

    abstract：INTRODUCTION:As the use of metallic radionuclides increases, so does the demand for a simple production method. In this study, we demonstrated an in situ target processing concept for automated metallic radionuclide production without the use of any robotic device. METHODS:An alumina ceramic vessel for a vertical irra...

    journal_title：Nuclear medicine and biology

    pub_type： 杂志文章

    doi：10.1016/j.nucmedbio.2012.05.010

    authors： Nagatsu K,Suzuki H,Fukada M,Minegishi K,Tsuji A,Fukumura T

    更新日期：2012-11-01 00:00:00

  • Pharmacokinetics of the thymidine analog 2'-fluoro-5-methyl-1-beta-D-arabinofuranosyluracil (FMAU) in tumor-bearing rats.

    abstract：:The thymidine analog 2'-fluoro-5-methyl-1-beta-D-arabinofuranosyluracil (FMAU) is incorporated into DNA and is resistant to catabolism. We performed pharmacokinetic measurements with [(14)C]FMAU and PET studies with [(11)C]FMAU using rats bearing several different syngeneic tumors. Among normal tissues, FMAU uptake re...

    journal_title：Nuclear medicine and biology

    pub_type： 杂志文章

    doi：10.1016/j.nucmedbio.2004.01.001

    authors： Bading JR,Shahinian AH,Vail A,Bathija P,Koszalka GW,Koda RT,Alauddin MM,Fissekis JD,Conti PS

    更新日期：2004-05-01 00:00:00

  • Evaluation of [¹⁸F]PFH PET renography to predict future disease progression in a rat model of autosomal dominant polycystic kidney disease.

    abstract：INTRODUCTION:Prognostic markers for progression of polycystic kidney disease (PKD) are limited. We evaluated the potential of early para-[(18)F]fluorohippurate ([(18)F]PFH) positron emission tomography (PET) renography to predict future progression of PKD in Han:SPRD rats with slowly progressive autosomal dominant PKD....

    journal_title：Nuclear medicine and biology

    pub_type： 杂志文章

    doi：10.1016/j.nucmedbio.2015.10.002

    authors： Pathuri G,Hedrick AF,Awasthi V,Cowley BD Jr,Gali H

    更新日期：2016-01-01 00:00:00

  • Influence of different chelators on the radiochemical properties of a 68-Gallium labelled bombesin analogue.

    abstract：UNLABELLED:The radiolabelled bombesin analogue AMBA shows high potential for diagnosis and treatment of prostate and breast cancer, but the influence of different chelators, which differ in terms of radiochemical reactivity and stability, have not been explored so far. In order to find the best suitable chelator for la...

    journal_title：Nuclear medicine and biology

    pub_type： 杂志文章

    doi：10.1016/j.nucmedbio.2013.08.010

    authors： Asti M,Iori M,Capponi PC,Atti G,Rubagotti S,Martin R,Brennauer A,Müller M,Bergmann R,Erba PA,Versari A

    更新日期：2014-01-01 00:00:00

  • Preclinical and clinical evaluation of O-[11C]methyl-L-tyrosine for tumor imaging by positron emission tomography.

    abstract：:We performed preclinical and clinical studies of O-[11C]methyl-L-tyrosine, a potential tracer for imaging amino acid transport of tumors by positron emission tomography (PET). Examinations of the radiation-absorbed dose by O-[11C]methyl-L-tyrosine and the acute toxicity and mutagenicity of O-methyl-L-tyrosine showed s...

    journal_title：Nuclear medicine and biology

    pub_type： 临床试验,杂志文章

    doi：10.1016/j.nucmedbio.2004.11.005

    authors： Ishiwata K,Tsukada H,Kubota K,Nariai T,Harada N,Kawamura K,Kimura Y,Oda K,Iwata R,Ishii K

    更新日期：2005-04-01 00:00:00

  • Pharmacokinetic computer simulations of the relationship between in vivo and in vitro neuroreceptor subtype selectivity of radioligands.

    abstract：:Pharmacokinetic computer simulations reveal a discrepancy between the in vivo and in vitro neuroreceptor subtype selectivity of radioligands. For radioligands with an in vitro neuroreceptor subtype selectivity between 0.1 and 10.0, the in vivo neuroreceptor subtype selectivity appears to be constrained to be between 0...

    journal_title：Nuclear medicine and biology

    pub_type： 杂志文章

    doi：10.1016/s0969-8051(99)00061-x

    authors： Zeeberg BR

    更新日期：1999-10-01 00:00:00

  • Experimental radiation synovectomy in rabbit knee with holmium-166 ferric hydroxide macroaggregate.

    abstract：:Holmium-166 ferric hydroxide macroaggregate (Ho-166 FHMA) particles possess two important properties for radiosynovectomy; relatively short half-life of the radioisotope and appropriate carrier size. Both these minimize radioactive leakage from the treated joint. This study was conducted to assess the effects of Ho-16...

    journal_title：Nuclear medicine and biology

    pub_type： 杂志文章

    doi：10.1016/s0969-8051(02)00317-7

    authors： Mäkelä O,Penttilä P,Kolehmainen E,Sukura A,Sankari S,Tulamo RM

    更新日期：2002-07-01 00:00:00

  • N-(6-18F-fluorohexyl)-N-methylpropargylamine: a fluorine-18-labeled monoamine oxidase B inhibitor for potential use in PET studies.

    abstract：:We have synthesized N-(6-18F-fluorohexyl)-N-methylpropargylamine (18F-FHMP) as a positron emission tomography (PET) radiotracer for monoamine oxidase B (MAO-B). The radiosynthesis was carried out by a fluorine-for-bromine substitution in 30-40% radiochemical yield in specific activities of 1-2 Ci/micromol. Selectivity...

    journal_title：Nuclear medicine and biology

    pub_type： 杂志文章

    doi：10.1016/s0969-8051(98)00061-4

    authors： Mukherjee J,Yang ZY,Lew R

    更新日期：1999-01-01 00:00:00

  • Synthesis of fluorine-18-labeled ciprofloxacin for PET studies in humans.

    abstract：:Ciprofloxacin (1-cyclopropyl-6-fluoro-1,4-dihydro-4-oxo-7-(1-piperazinyl)-quinoline-3-carboxylic acid), a widely-prescribed antibiotic, was labeled with fluorine-18 with the aim to perform positron emission tomography studies in humans for pharmacokinetic measurements. Due to a lack of chemical activation of ciproflox...

    journal_title：Nuclear medicine and biology

    pub_type： 杂志文章

    doi：10.1016/s0969-8051(02)00444-4

    authors： Langer O,Mitterhauser M,Brunner M,Zeitlinger M,Wadsak W,Mayer BX,Kletter K,Müller M

    更新日期：2003-04-01 00:00:00