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  1. Article: The Development of a Smart Magnetic Resonance Imaging and Chemical Exchange Saturation Transfer Contrast Agent for the Imaging of Sulfatase Activity.

    Welleman, Ilse M / Reeβing, Friederike / Boersma, Hendrikus H / Dierckx, Rudi A J O / Feringa, Ben L / Szymanski, Wiktor

    Pharmaceuticals (Basel, Switzerland)

    2023  Volume 16, Issue 10

    Abstract: The molecular imaging of biomarkers plays an increasing role in medical diagnostics. In particular, the imaging of enzyme activity is a promising approach, as it enables the use of its inherent catalytic activity for the amplification of an imaging ... ...

    Abstract The molecular imaging of biomarkers plays an increasing role in medical diagnostics. In particular, the imaging of enzyme activity is a promising approach, as it enables the use of its inherent catalytic activity for the amplification of an imaging signal. The increased activity of a sulfatase enzyme has been observed in several types of cancers. We describe the development and in vitro evaluation of molecular imaging agents that allow for the detection of sulfatase activity using the whole-body, non-invasive MRI and CEST imaging methods. This approach relies on a responsive ligand that features a sulfate ester moiety, which upon sulfatase-catalyzed hydrolysis undergoes an elimination process that changes the functional group, coordinating with the metal ion. When Gd
    Language English
    Publishing date 2023-10-11
    Publishing country Switzerland
    Document type Journal Article
    ZDB-ID 2193542-7
    ISSN 1424-8247
    ISSN 1424-8247
    DOI 10.3390/ph16101439
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  2. Article ; Online: Preclinical evaluation of 2-[

    Braams, Lisanne M / Sijbesma, Jürgen W A / Boersma, Hendrikus H / van Dijl, Jan Maarten / Elsinga, Philip H / Glaudemans, Andor W J M / Slart, Riemer H J A / van Oosten, Marleen

    International journal of medical microbiology : IJMM

    2023  Volume 313, Issue 3, Page(s) 151581

    Abstract: Fluorine-18-fluorodeoxyglucose ([ ...

    Abstract Fluorine-18-fluorodeoxyglucose ([
    MeSH term(s) Animals ; Humans ; Fluorodeoxyglucose F18 ; Positron-Emission Tomography/methods ; Bacterial Infections ; Sorbitol ; Bacteria ; Mammals
    Chemical Substances Fluorodeoxyglucose F18 (0Z5B2CJX4D) ; Sorbitol (506T60A25R)
    Language English
    Publishing date 2023-05-16
    Publishing country Germany
    Document type Journal Article
    ZDB-ID 2006518-8
    ISSN 1618-0607 ; 1438-4221
    ISSN (online) 1618-0607
    ISSN 1438-4221
    DOI 10.1016/j.ijmm.2023.151581
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  3. Article: Characterization of a novel model for atherosclerosis imaging: the apolipoprotein E-deficient rat.

    Sijbesma, Jürgen W A / van Waarde, Aren / Kristensen, Sebastiaan / Kion, Ilse / Tietge, Uwe J F / Hillebrands, Jan-Luuk / Bulthuis, Marian L C / Buikema, Hendrik / Nakladal, Dalibor / Westerterp, Marit / Liu, Fan / Boersma, Hendrikus H / Dierckx, Rudi A J O / Slart, Riemer H J A

    EJNMMI research

    2023  Volume 13, Issue 1, Page(s) 106

    Abstract: Background: The apolipoprotein E-deficient (apoE: Results: ApoE: Conclusion: These data demonstrate early signs of hypercholesterolemia, high levels of bile acids, the development of atherosclerotic lesions, and macrophage accumulation in ... ...

    Abstract Background: The apolipoprotein E-deficient (apoE
    Results: ApoE
    Conclusion: These data demonstrate early signs of hypercholesterolemia, high levels of bile acids, the development of atherosclerotic lesions, and macrophage accumulation in apoE
    Language English
    Publishing date 2023-12-11
    Publishing country Germany
    Document type Journal Article
    ZDB-ID 2619892-7
    ISSN 2191-219X
    ISSN 2191-219X
    DOI 10.1186/s13550-023-01055-5
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  4. Article ; Online: Oral administration of PET tracers: Current status.

    Salvi de Souza, Giordana / Mantovani, Dimitri B A / Mossel, Pascalle / Haarman, Bartholomeus C M / Marques da Silva, Ana Maria / Boersma, Hendrikus H / Furini, Cristiane R G / Lammertsma, Adriaan A / Tsoumpas, Charalampos / Luurtsema, Gert

    Journal of controlled release : official journal of the Controlled Release Society

    2023  Volume 357, Page(s) 591–605

    Abstract: The oral route is the most widely used and preferable way of drug administration. Several pharmacokinetic processes play a role in the distribution of administered drugs. Therefore, accurate quantification of absorption, distribution, metabolism, ... ...

    Abstract The oral route is the most widely used and preferable way of drug administration. Several pharmacokinetic processes play a role in the distribution of administered drugs. Therefore, accurate quantification of absorption, distribution, metabolism, excretion, and characterisation of drug kinetics after oral administration is extremely important for developing new human drugs. In vivo methods, such as gamma-scintigraphy, magnetic resonance imaging (MRI), and positron emission tomography (PET), have been used to analyse gastrointestinal tract (GIT) absorption behaviour. This scoping review provides an overview of PET studies that used oral tracer administration. A systematic literature search was performed using PubMed, EMBASE, Scopus, Science Direct, and Web of Science databases. Extensive variation between these studies was seen concerning acquisition protocols, quantification methods, and pharmacokinetic outcome parameters. Studies in humans indicate that it takes 10 to 30 min for the tracer to be in the intestine and about 100 min to reach its maximum concentration in the brain. In rodent studies, different pharmacokinetic parameters for the brain, blood, and GIT were estimated, showing the potential of PET to measure the absorption and distribution of drugs and pharmaceuticals non-invasively. Finally, regarding radiation protection, oral administration has a higher absorbed dose in GIT and, consequently, a higher effective dose. However, with the recent introduction of Long Axial Field of View (LAFOV) PET scanners, it is possible to reduce the administered dose, making oral administration feasible for routine clinical studies.
    MeSH term(s) Humans ; Positron-Emission Tomography ; Brain/diagnostic imaging ; Administration, Oral ; Gastrointestinal Tract/diagnostic imaging
    Language English
    Publishing date 2023-04-23
    Publishing country Netherlands
    Document type Journal Article ; Review ; Research Support, Non-U.S. Gov't
    ZDB-ID 632533-6
    ISSN 1873-4995 ; 0168-3659
    ISSN (online) 1873-4995
    ISSN 0168-3659
    DOI 10.1016/j.jconrel.2023.04.008
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  5. Article ; Online: PET/CT Imaging and Physiology of Mice on High Protein Diet.

    Sijbesma, Jürgen W A / van Waarde, Aren / Stegger, Lars / Dierckx, Rudi A J O / Boersma, Hendrikus H / Slart, Riemer H J A

    International journal of molecular sciences

    2021  Volume 22, Issue 6

    Abstract: Background: High protein (HP) diets have been proposed to reduce body weight in humans. The diets are known to alter energy metabolism, which can affect the quality of [: Methods: C57BL/6J (Black six (Bl6)) and apolipoprotein E-deficient (: Results! ...

    Abstract Background: High protein (HP) diets have been proposed to reduce body weight in humans. The diets are known to alter energy metabolism, which can affect the quality of [
    Methods: C57BL/6J (Black six (Bl6)) and apolipoprotein E-deficient (
    Results: Myocardial [
    Conclusions: Myocardial uptake of [
    MeSH term(s) Animals ; Blood Glucose ; Body Composition ; Body Weight ; Diet, High-Protein ; Fluorodeoxyglucose F18 ; Heart/diagnostic imaging ; Mice ; Myocardium/metabolism ; Organ Size ; Positron Emission Tomography Computed Tomography
    Chemical Substances Blood Glucose ; Fluorodeoxyglucose F18 (0Z5B2CJX4D)
    Language English
    Publishing date 2021-03-22
    Publishing country Switzerland
    Document type Journal Article
    ZDB-ID 2019364-6
    ISSN 1422-0067 ; 1422-0067 ; 1661-6596
    ISSN (online) 1422-0067
    ISSN 1422-0067 ; 1661-6596
    DOI 10.3390/ijms22063236
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  6. Article ; Online: Preclinical evaluation of 2-[18F]fluorodeoxysorbitol as a tracer for targeted imaging of Enterobacterales infection

    Lisanne M. Braams / Jürgen W.A. Sijbesma / Hendrikus H. Boersma / Jan Maarten van Dijl / Philip H. Elsinga / Andor W.J.M. Glaudemans / Riemer H.J.A. Slart / Marleen van Oosten

    International Journal of Medical Microbiology, Vol 313, Iss 3, Pp 151581- (2023)

    2023  

    Abstract: Fluorine-18-fluorodeoxyglucose ([18F]FDG) positron emission tomography (18F-FDG-PET) is widely used for the detection of inflammatory and infectious diseases. Although this modality has proven to be a useful diagnostic tool, reliable distinction of ... ...

    Abstract Fluorine-18-fluorodeoxyglucose ([18F]FDG) positron emission tomography (18F-FDG-PET) is widely used for the detection of inflammatory and infectious diseases. Although this modality has proven to be a useful diagnostic tool, reliable distinction of bacterial infection from sterile inflammation or even from a malignancy remains challenging. Therefore, there is a need for bacteria-specific tracers for PET imaging that facilitate a reliable distinction of bacterial infection from other pathology. The present study was aimed at exploring the potential of 2-[18F]-fluorodeoxysorbitol ([18F]FDS) as a tracer for detection of Enterobacterales infections. Sorbitol is a sugar alcohol that is commonly metabolized by bacteria of the Enterobacterales order, but not by mammalian cells, which makes it an attractive candidate for targeted bacterial imaging. The latter is important in view of the serious clinical implications of infections caused by Enterobacterales. Here we demonstrate that sorbitol-based PET can be applied to detect a broad range of clinical bacterial isolates not only in vitro, but also in blood and ascites samples from patients suffering from Enterobacterales infections. Notably, the possible application of [18F]FDS is not limited to Enterobacterales since Pseudomonas aeruginosa and Corynebacterium jeikeium also showed substantial uptake of this tracer. We conclude that [18F]FDS is a promising tracer for PET-imaging of infections caused by a group of bacteria that can cause serious invasive disease.
    Keywords Enterobacterales ; Gram-negative ; Sorbitol ; Infection imaging ; Clinical isolates ; Blood ; Microbiology ; QR1-502 ; Other systems of medicine ; RZ201-999
    Subject code 610
    Language English
    Publishing date 2023-05-01T00:00:00Z
    Publisher Elsevier
    Document type Article ; Online
    Database BASE - Bielefeld Academic Search Engine (life sciences selection)

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  7. Article: Photoresponsive molecular tools for emerging applications of light in medicine.

    Welleman, Ilse M / Hoorens, Mark W H / Feringa, Ben L / Boersma, Hendrikus H / Szymański, Wiktor

    Chemical science

    2020  Volume 11, Issue 43, Page(s) 11672–11691

    Abstract: Light-based therapeutic and imaging modalities, which emerge in clinical applications, rely on molecular tools, such as photocleavable protecting groups and photoswitches that respond to photonic stimulus and translate it into a biological effect. ... ...

    Abstract Light-based therapeutic and imaging modalities, which emerge in clinical applications, rely on molecular tools, such as photocleavable protecting groups and photoswitches that respond to photonic stimulus and translate it into a biological effect. However, optimisation of their key parameters (activation wavelength, band separation, fatigue resistance and half-life) is necessary to enable application in the medical field. In this perspective, we describe the applications scenarios that can be envisioned in clinical practice and then we use those scenarios to explain the necessary properties that the photoresponsive tools used to control biological function should possess, highlighted by examples from medical imaging, drug delivery and photopharmacology. We then present how the (photo)chemical parameters are currently being optimized and an outlook is given on pharmacological aspects (toxicity, solubility, and stability) of light-responsive molecules. With these interdisciplinary insights, we aim to inspire the future directions for the development of photocontrolled tools that will empower clinical applications of light.
    Language English
    Publishing date 2020-10-15
    Publishing country England
    Document type Journal Article ; Review
    ZDB-ID 2559110-1
    ISSN 2041-6539 ; 2041-6520
    ISSN (online) 2041-6539
    ISSN 2041-6520
    DOI 10.1039/d0sc04187d
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  8. Article ; Online: [

    Slart, Riemer H J A / Martinez-Lucio, T Samara / Boersma, Hendrikus H / Borra, Ronald H / Cornelissen, Bart / Dierckx, Rudi A J O / Dobrolinska, Magdalena / Doorduin, Janine / Erba, Paola A / Glaudemans, Andor W J M / Giacobbo, Bruno Lima / Luurtsema, Gert / Noordzij, Walter / van Sluis, Joyce / Tsoumpas, Charalampos / Lammertsma, Adriaan A

    Seminars in nuclear medicine

    2023  

    Abstract: Imaging water pathways in the human body provides an excellent way of measuring accurately the blood flow directed to different organs. This makes it a powerful diagnostic tool for a wide range of diseases that are related to perfusion and oxygenation. ... ...

    Abstract Imaging water pathways in the human body provides an excellent way of measuring accurately the blood flow directed to different organs. This makes it a powerful diagnostic tool for a wide range of diseases that are related to perfusion and oxygenation. Although water PET has a long history, its true potential has not made it into regular clinical practice. The article highlights the potential of water PET in molecular imaging and suggests its prospective role in becoming an essential tool for the 21st century precision medicine in different domains ranging from preclinical to clinical research and practice. The recent technical advances in high-sensitivity PET imaging can play a key accelerating role in empowering this technique, though there are still several challenges to overcome.
    Language English
    Publishing date 2023-08-26
    Publishing country United States
    Document type Journal Article ; Review
    ZDB-ID 120248-0
    ISSN 1558-4623 ; 0001-2998
    ISSN (online) 1558-4623
    ISSN 0001-2998
    DOI 10.1053/j.semnuclmed.2023.08.002
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  9. Article ; Online: Immunogenicity phase II study evaluating booster capacity of nonadjuvanted AKS-452 SARS-Cov-2 RBD Fc vaccine.

    Alleva, David G / Feitsma, Eline A / Janssen, Yester F / Boersma, Hendrikus H / Lancaster, Thomas M / Sathiyaseelan, Thillainaygam / Murikipudi, Sylaja / Delpero, Andrea R / Scully, Melanie M / Ragupathy, Ramya / Kotha, Sravya / Haworth, Jeffrey R / Shah, Nishit J / Rao, Vidhya / Nagre, Shashikant / Ronca, Shannon E / Green, Freedom M / Shaw, Stephen A / Aminetzah, Ari /
    Kruijff, Schelto / Brom, Maarten / van Dam, Gooitzen M / Zion, Todd C

    NPJ vaccines

    2024  Volume 9, Issue 1, Page(s) 40

    Abstract: AKS-452, a subunit vaccine comprising an Fc fusion of the ancestral wild-type (WT) SARS-CoV-2 virus spike protein receptor binding domain (SP/RBD), was evaluated without adjuvant in a single cohort, non-randomized, open-labelled phase II study ( ... ...

    Abstract AKS-452, a subunit vaccine comprising an Fc fusion of the ancestral wild-type (WT) SARS-CoV-2 virus spike protein receptor binding domain (SP/RBD), was evaluated without adjuvant in a single cohort, non-randomized, open-labelled phase II study (NCT05124483) at a single site in The Netherlands for safety and immunogenicity. A single 90 µg subcutaneous booster dose of AKS-452 was administered to 71 adults previously primed with a registered mRNA- or adenovirus-based vaccine and evaluated for 273 days. All AEs were mild and no SAEs were attributable to AKS-452. While all subjects showed pre-existing SP/RBD binding and ACE2-inhibitory IgG titers, 60-68% responded to AKS-452 via ≥2-fold increase from days 28 to 90 and progressively decreased back to baseline by day 180 (days 28 and 90 mean fold-increases, 14.7 ± 6.3 and 8.0 ± 2.2). Similar response kinetics against RBD mutant proteins (including omicrons) were observed but with slightly reduced titers relative to WT. There was an expected strong inverse correlation between day-0 titers and the fold-increase in titers at day 28. AKS-452 enhanced neutralization potency against live virus, consistent with IgG titers. Nucleocapsid protein (Np) titers suggested infection occurred in 66% (46 of 70) of subjects, in which only 20 reported mild symptomatic COVID-19. These favorable safety and immunogenicity profiles support booster evaluation in a planned phase III universal booster study of this room-temperature stable vaccine that can be rapidly and inexpensively manufactured to serve vaccination at a global scale without the need of a complex distribution or cold chain.
    Language English
    Publishing date 2024-02-21
    Publishing country England
    Document type Journal Article
    ISSN 2059-0105
    ISSN (online) 2059-0105
    DOI 10.1038/s41541-024-00830-2
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  10. Article ; Online: Quantification of P-glycoprotein function at the human blood-brain barrier using [

    Mossel, Pascalle / Arif, Wejdan M / De Souza, Giordana Salvi / Varela, Lara Garcia / van der Weijden, Chris W J / Boersma, Hendrikus H / Willemsen, Antoon T M / Boellaard, Ronald / Elsinga, Philip H / Borra, Ronald J H / Dierckx, Rudi A J O / Lammertsma, Adriaan A / Bartels, Anna L / Luurtsema, Gert

    European journal of nuclear medicine and molecular imaging

    2023  Volume 50, Issue 13, Page(s) 3917–3927

    Abstract: Introduction: P-glycoprotein (P-gp) is one of the most studied efflux transporters at the blood-brain barrier. It plays an important role in brain homeostasis by protecting the brain from a variety of endogenous and exogeneous substances. Changes in P- ... ...

    Abstract Introduction: P-glycoprotein (P-gp) is one of the most studied efflux transporters at the blood-brain barrier. It plays an important role in brain homeostasis by protecting the brain from a variety of endogenous and exogeneous substances. Changes in P-gp function are associated both with the onset of neuropsychiatric diseases, including Alzheimer's disease and Parkinson's disease, and with drug-resistance, for example in treatment-resistant depression. The most widely used approach to measure P-gp function in vivo is (R)-[
    Aim: The aim of this study was (1) to identify the pharmacokinetic model that best describes [
    Methods: Five (2 male, 3 female) of fourteen healthy subjects (8 male, 6 female, age 67 ± 5 years) were scanned twice (injected dose 201 ± 47 MBq) with a minimum interval of 2 weeks between scans. Each scanning session consisted of a 60-min dynamic [
    Results: Sixty minutes post-injection, the parent fraction was 63.8 ± 4.0%. The reversible two tissue compartment model corrected for plasma metabolites with an estimated blood volume (V
    Conclusion: [
    Trial registration: EudraCT 2020-001564-28 . Registered 25 May 2020.
    MeSH term(s) Humans ; Male ; Female ; Middle Aged ; Aged ; Blood-Brain Barrier/diagnostic imaging ; Blood-Brain Barrier/metabolism ; ATP Binding Cassette Transporter, Subfamily B, Member 1/metabolism ; Reproducibility of Results ; Brain/diagnostic imaging ; Brain/metabolism ; ATP Binding Cassette Transporter, Subfamily B/metabolism ; Positron-Emission Tomography ; Verapamil ; Radiopharmaceuticals/pharmacokinetics
    Chemical Substances ATP Binding Cassette Transporter, Subfamily B, Member 1 ; ATP Binding Cassette Transporter, Subfamily B ; Verapamil (CJ0O37KU29) ; Radiopharmaceuticals
    Language English
    Publishing date 2023-08-08
    Publishing country Germany
    Document type Journal Article
    ZDB-ID 8236-3
    ISSN 1619-7089 ; 0340-6997 ; 1619-7070
    ISSN (online) 1619-7089
    ISSN 0340-6997 ; 1619-7070
    DOI 10.1007/s00259-023-06363-5
    Database MEDical Literature Analysis and Retrieval System OnLINE

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