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  1. Article: Correction: [

    Marner, Lisbeth / Korsholm, Kirsten / Anderberg, Lasse / Lonsdale, Markus N / Jensen, Mads Radmer / Brødsgaard, Eva / Denholt, Charlotte L / Gillings, Nic / Law, Ian / Friberg, Lars

    EJNMMI research

    2023  Volume 13, Issue 1, Page(s) 19

    Language English
    Publishing date 2023-03-01
    Publishing country Germany
    Document type Published Erratum
    ZDB-ID 2619892-7
    ISSN 2191-219X
    ISSN 2191-219X
    DOI 10.1186/s13550-023-00970-x
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  2. Article ; Online: (99m)Tc-aprotinin - optimisation and validation of radiolabelling kits for routine preparation for diagnostic imaging of amyloidosis.

    Denholt, Charlotte / Gillings, Nic

    Journal of labelled compounds & radiopharmaceuticals

    2016  Volume 59, Issue 4, Page(s) 171–174

    Abstract: Technetium-99m aprotinin was prepared from an optimised radiolabelling kit formulation containing aprotinin, alkaline buffer and stannous chloride (reducing agent) and radiolabelled using (99m) Tc-pertechnetate. The labelling was achieved within 25 min, ... ...

    Abstract Technetium-99m aprotinin was prepared from an optimised radiolabelling kit formulation containing aprotinin, alkaline buffer and stannous chloride (reducing agent) and radiolabelled using (99m) Tc-pertechnetate. The labelling was achieved within 25 min, with radiochemical purities of >98%.
    MeSH term(s) Amyloidosis/diagnostic imaging ; Aprotinin/chemistry ; Diagnostic Imaging ; Isotope Labeling/methods ; Radiochemistry ; Technetium/chemistry
    Chemical Substances Technetium (7440-26-8) ; Aprotinin (9087-70-1)
    Language English
    Publishing date 2016-02-28
    Publishing country England
    Document type Journal Article
    ZDB-ID 196095-7
    ISSN 1099-1344 ; 0362-4803 ; 0022-2135
    ISSN (online) 1099-1344
    ISSN 0362-4803 ; 0022-2135
    DOI 10.1002/jlcr.3381
    Database MEDical Literature Analysis and Retrieval System OnLINE

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    In stock of ZB MED Cologne/Königswinter

    Zs.A 1332: Show issues Location:
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  3. Article: Fully Automated GMP-Compliant Synthesis of [

    Bratteby, Klas / Denholt, Charlotte Lund / Lehel, Szabolcs / Petersen, Ida Nymann / Madsen, Jacob / Erlandsson, Maria / Ohlsson, Tomas / Herth, Matthias Manfred / Gillings, Nic

    Pharmaceuticals (Basel, Switzerland)

    2021  Volume 14, Issue 7

    Abstract: In the struggle to understand and accurately diagnose Parkinson's disease, radiopharmaceuticals and medical imaging techniques have played a major role. By being able to image and quantify the dopamine transporter density, noninvasive diagnostic imaging ... ...

    Abstract In the struggle to understand and accurately diagnose Parkinson's disease, radiopharmaceuticals and medical imaging techniques have played a major role. By being able to image and quantify the dopamine transporter density, noninvasive diagnostic imaging has become the gold standard. In the shift from the first generation of SPECT tracers, the fluorine-18-labeled tracer [
    Language English
    Publishing date 2021-06-22
    Publishing country Switzerland
    Document type Journal Article
    ZDB-ID 2193542-7
    ISSN 1424-8247
    ISSN 1424-8247
    DOI 10.3390/ph14070601
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  4. Article: [

    Marner, Lisbeth / Korsholm, Kirsten / Anderberg, Lasse / Lonsdale, Markus N / Jensen, Mads Radmer / Brødsgaard, Eva / Denholt, Charlotte L / Gillings, Nic / Law, Ian / Friberg, Lars

    EJNMMI research

    2022  Volume 12, Issue 1, Page(s) 56

    Abstract: Background: Dopamine transporter (DAT) imaging of striatum is clinically used in Parkinson's disease (PD) and neurodegenerative parkinsonian syndromes (PS) especially in the early disease stages. The aim of the present study was to evaluate the ... ...

    Abstract Background: Dopamine transporter (DAT) imaging of striatum is clinically used in Parkinson's disease (PD) and neurodegenerative parkinsonian syndromes (PS) especially in the early disease stages. The aim of the present study was to evaluate the diagnostic performance of the recently developed tracer for DAT imaging [
    Methods: Ninety-eight unselected patients referred for DAT imaging were included prospectively and consecutively and evaluated with [
    Results: Fifty-six of the [
    Conclusions: The high correspondence of [
    Language English
    Publishing date 2022-09-07
    Publishing country Germany
    Document type Journal Article
    ZDB-ID 2619892-7
    ISSN 2191-219X
    ISSN 2191-219X
    DOI 10.1186/s13550-022-00930-x
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  5. Article ; Online: Fully Automated GMP-Compliant Synthesis of [ 18 F]FE-PE2I

    Klas Bratteby / Charlotte Lund Denholt / Szabolcs Lehel / Ida Nymann Petersen / Jacob Madsen / Maria Erlandsson / Tomas Ohlsson / Matthias Manfred Herth / Nic Gillings

    Pharmaceuticals, Vol 14, Iss 601, p

    2021  Volume 601

    Abstract: In the struggle to understand and accurately diagnose Parkinson′s disease, radiopharmaceuticals and medical imaging techniques have played a major role. By being able to image and quantify the dopamine transporter density, noninvasive diagnostic imaging ... ...

    Abstract In the struggle to understand and accurately diagnose Parkinson′s disease, radiopharmaceuticals and medical imaging techniques have played a major role. By being able to image and quantify the dopamine transporter density, noninvasive diagnostic imaging has become the gold standard. In the shift from the first generation of SPECT tracers, the fluorine-18-labeled tracer [ 18 F]FE-PE2I has emerged as the agent of choice for many physicians. However, implementing suitable synthesis for the production of [ 18 F]FE-PE2I has proved more challenging than expected. Through a thorough analysis of the relevant factors affecting the final radiochemical yield, we were able to implement high-yielding fully automated GMP-compliant synthesis of [ 18 F]FE-PE2I on a Synthera ® + platform. By reaching RCYs up to 62%, it allowed us to isolate 25 GBq of the formulated product, and an optimized formulation resulted in the shelf life of 6 h, satisfying the increased demand for this radiopharmaceutical.
    Keywords [ 18 F]FE-PE2I ; radiochemistry ; fluorine-18 ; automation ; GMP ; Medicine ; R ; Pharmacy and materia medica ; RS1-441
    Subject code 333
    Language English
    Publishing date 2021-06-01T00:00:00Z
    Publisher MDPI AG
    Document type Article ; Online
    Database BASE - Bielefeld Academic Search Engine (life sciences selection)

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  6. Article: Identification of novel peptide ligands for the cancer-specific receptor mutation EFGRvIII using a mixture-based synthetic combinatorial library.

    Denholt, Charlotte Lund / Hansen, Paul Robert / Pedersen, Nina / Poulsen, Hans Skovgaard / Gillings, Nic / Kjaer, Andreas

    Biopolymers

    2009  Volume 91, Issue 3, Page(s) 201–206

    Abstract: We report here, the design and synthesis of a positional scanning synthetic combinatorial library for the identification of novel peptide ligands targeted against the cancer-specific epidermal growth factor tyrosine kinase receptor mutation variant III ( ... ...

    Abstract We report here, the design and synthesis of a positional scanning synthetic combinatorial library for the identification of novel peptide ligands targeted against the cancer-specific epidermal growth factor tyrosine kinase receptor mutation variant III (EGFRvIII). This receptor is expressed in several kinds of cancer, in particular, ovarian, glioblastomas, and breast cancer, but not in normal tissue. The library consisted of six individual positional sublibraries in the format, H-O(1-6)XXXXX-NH(2), O being one of the 19 proteinogenic amino acids (cysteine omitted) and X an equimolar mixture of these. The library consisted of 114 mixtures in total. Using a biotin-streptavidin assay, the binding of each sublibrary to NR6M, NR6W-A, and NR6 cells was tested. These cells express EGFRvIII, EGFR, and neither of the receptors, respectively. The result from each sublibrary was examined to identify the most active amino acid residue at each position. On the basis of this knowledge, eight peptides were synthesized and tested for binding to EGFRvIII. We identified one peptide, H-FALGEA-NH(2), that showed more selective binding to the mutated receptor than the EGFRvIII specific peptide PEPHC1. This study demonstrates the value of using mixture-based combinatorial positional scanning libraries for the identification of novel peptide ligands targeted against the cancer-specific EGFRvIII. Our best candidate H-FALGEA-NH(2) will be radioactively labeled and evaluated as an imaging agent for positron emission tomography investigation for diagnosis, staging, and monitoring of therapy of various types of cancer.
    MeSH term(s) Animals ; Cell Line ; Combinatorial Chemistry Techniques/methods ; Ligands ; Mice ; Mutant Proteins/genetics ; Mutant Proteins/metabolism ; Mutation/genetics ; Neoplasms/enzymology ; Neoplasms/genetics ; Peptides/analysis ; Peptides/metabolism ; Protein Binding ; Receptor, Epidermal Growth Factor/genetics ; Receptor, Epidermal Growth Factor/metabolism
    Chemical Substances Ligands ; Mutant Proteins ; Peptides ; epidermal growth factor receptor VIII ; Receptor, Epidermal Growth Factor (EC 2.7.10.1)
    Language English
    Publishing date 2009-03
    Publishing country United States
    Document type Journal Article ; Research Support, Non-U.S. Gov't
    ZDB-ID 1123-x
    ISSN 1097-0282 ; 0006-3525
    ISSN (online) 1097-0282
    ISSN 0006-3525
    DOI 10.1002/bip.21117
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    In stock of ZB MED Cologne/Königswinter

    Zs.A 77: Show issues Location:
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    Jg. 1995 - 2021: Lesesall (1.OG)
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  7. Article ; Online: Evaluation of 4-[18F]fluorobenzoyl-FALGEA-NH2 as a positron emission tomography tracer for epidermal growth factor receptor mutation variant III imaging in cancer.

    Denholt, Charlotte Lund / Binderup, Tina / Stockhausen, Marie-Thérése / Poulsen, Hans Skovgaard / Spang-Thomsen, Mogens / Hansen, Paul Robert / Gillings, Nic / Kjær, Andreas

    Nuclear medicine and biology

    2011  Volume 38, Issue 4, Page(s) 509–515

    Abstract: Introduction: This study describes the radiosynthesis, in vitro and in vivo evaluation of the novel small peptide radioligand, 4-[(18)F]fluorobenzoyl-Phe-Ala-Leu-Gly-Glu-Ala-NH(2,) ([(18)F]FBA-FALGEA-NH(2)) as a positron emission tomography (PET) tracer ...

    Abstract Introduction: This study describes the radiosynthesis, in vitro and in vivo evaluation of the novel small peptide radioligand, 4-[(18)F]fluorobenzoyl-Phe-Ala-Leu-Gly-Glu-Ala-NH(2,) ([(18)F]FBA-FALGEA-NH(2)) as a positron emission tomography (PET) tracer for imaging of the cancer specific epidermal growth factor receptor (EGFR) variant III mutation, EGFRvIII.
    Methods: For affinity, stability and PET measurements, H-FALGEA-NH(2) was radiolabelled using 4-[(18)F]fluorobenzoic acid ([(18)F]FBA). The binding affinity of ([(18)F]FBA)-FALGEA-NH(2) was measured on EGFRvIII expressing cells, NR6M. Stability studies in vitro and in vivo were carried out in blood plasma from nude mice. PET investigations of [(18)F]FBA-FALGEA-NH(2) were performed on a MicroPET scanner, using seven nude mice xenografted subcutaneously with human glioblastoma multiforme (GBM) tumours, expressing the EGFRvIII in its native form, and five nude mice xenografted subcutaneously with GBM tumours lacking EGFRvIII expression. Images of [(18)F]FDG were also obtained for comparison. The mice were injected with 5-10 MBq of the radiolabelled peptide or [(18)F]FDG. Furthermore, the gene expression of EGFRvIII in the tumours was determined using quantitative real-time PCR.
    Results: Radiolabelling and purification was achieved within 180 min, with overall radiochemical yields of 2.6-9.8% (decay-corrected) and an average specific radioactivity of 6.4 GBq/μmol. The binding affinity (K(d)) of [(18)F]FBA-FALGEA-NH(2) to EGFRvIII expressing cells was determined to be 23 nM. The radiolabelled peptide was moderately stable in the plasma from nude mice where 53% of the peptide was intact after 60 min of incubation in plasma but rapidly degraded in vivo, where no intact peptide was observed in plasma 5 min post-injection. The PET imaging showed that [(18)F]FBA-FALGEA-NH(2) accumulated preferentially in the human GBM xenografts which expressed high amounts of the mutated receptor. The average tumour-to-muscle ratio (T/M) in the EGFRvIII tumours was 7.8 at 60 min post-injection, compared with 4.6 in the wild-type EGFR tumours. Furthermore, there was a strong correlation (R=0.86, P=.007) between the expression of EGFRvIII in the tumours and the tracer uptake expressed as T/M.
    Conclusion: Our results indicate that, despite its rapid metabolism, [(18)F]FBA-FALGEA-NH(2) binds preferentially to EGFRvIII in the tumours in vivo and is a promising lead for further development of EGFRvIII specific peptide radiopharmaceuticals.
    MeSH term(s) Animals ; Benzoates/chemistry ; Biological Transport ; Cell Transformation, Neoplastic ; Drug Stability ; Fluorodeoxyglucose F18 ; Gene Expression Regulation, Neoplastic ; Glioblastoma/diagnostic imaging ; Glioblastoma/genetics ; Glioblastoma/metabolism ; Glioblastoma/pathology ; Humans ; Mice ; Mutation ; Oligopeptides/chemical synthesis ; Oligopeptides/metabolism ; Positron-Emission Tomography/methods ; Radioactive Tracers ; Receptor, Epidermal Growth Factor/genetics ; Receptor, Epidermal Growth Factor/metabolism
    Chemical Substances 4-fluorobenzoyl-phenylalanyl-alanyl-leucyl-glycyl-glutamyl-alaninamide ; Benzoates ; Oligopeptides ; Radioactive Tracers ; epidermal growth factor receptor VIII ; Fluorodeoxyglucose F18 (0Z5B2CJX4D) ; Receptor, Epidermal Growth Factor (EC 2.7.10.1) ; 4-fluorobenzoic acid (V5ROO2HOU4)
    Language English
    Publishing date 2011-05
    Publishing country United States
    Document type Journal Article ; Research Support, Non-U.S. Gov't
    ZDB-ID 1138098-6
    ISSN 1872-9614 ; 0883-2897 ; 0969-8051
    ISSN (online) 1872-9614
    ISSN 0883-2897 ; 0969-8051
    DOI 10.1016/j.nucmedbio.2010.11.003
    Database MEDical Literature Analysis and Retrieval System OnLINE

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    In stock of ZB MED Cologne/Königswinter

    Zs.A 1090: Show issues Location:
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