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  1. Article ; Online: A Kinetically Controlled Bioconjugation Method for the Synthesis of Radioimmunoconjugates and the Development of a Domain Mapping MS-Workflow for Its Characterization.

    Pometti, Marco A / Di Natale, Giuseppe / Geremia, Giancarlo / Gauswami, Nileshgiri / Garufi, Gianni / Ricciardi, Giuseppina / Sciortino, Marcella / Scopelliti, Fabrizio / Russo, Giorgio / Ippolito, Massimo

    Bioconjugate chemistry

    2024  Volume 35, Issue 3, Page(s) 324–332

    Abstract: Immunoconjugates exploit the high affinity of monoclonal antibodies for a recognized antigen to selectively deliver a cytotoxic payload, such as drugs or radioactive nuclides, at the site of disease. Despite numerous techniques have been recently ... ...

    Abstract Immunoconjugates exploit the high affinity of monoclonal antibodies for a recognized antigen to selectively deliver a cytotoxic payload, such as drugs or radioactive nuclides, at the site of disease. Despite numerous techniques have been recently developed for site-selective bioconjugations of protein structures, reaction of ε-amine group of lysine residues with electrophilic reactants, such as activated esters (NHS), is the main method reported in the literature as it maintains proteins in their native conformation. Since antibodies hold a high number of lysine residues, a heterogeneous mixture of conjugates will be generated, which can result in decreased target affinity. Here, we report an intradomain regioselective bioconjugation between the monoclonal antibody Trastuzumab and the
    MeSH term(s) Immunoconjugates/chemistry ; Lysine/chemistry ; Workflow ; Antibodies, Monoclonal/chemistry ; Chelating Agents ; Esters
    Chemical Substances Immunoconjugates ; Lysine (K3Z4F929H6) ; Antibodies, Monoclonal ; Chelating Agents ; Esters
    Language English
    Publishing date 2024-02-17
    Publishing country United States
    Document type Journal Article
    ZDB-ID 1024041-x
    ISSN 1520-4812 ; 1043-1802
    ISSN (online) 1520-4812
    ISSN 1043-1802
    DOI 10.1021/acs.bioconjchem.3c00519
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  2. Article: Biodistribution Assessment of a Novel

    Pavone, Anna Maria / Benfante, Viviana / Giaccone, Paolo / Stefano, Alessandro / Torrisi, Filippo / Russo, Vincenzo / Serafini, Davide / Richiusa, Selene / Pometti, Marco / Scopelliti, Fabrizio / Ippolito, Massimo / Giannone, Antonino Giulio / Cabibi, Daniela / Asti, Mattia / Vettorato, Elisa / Morselli, Luca / Merone, Mario / Lunardon, Marcello / Andrighetto, Alberto /
    Tuttolomondo, Antonino / Cammarata, Francesco Paolo / Verona, Marco / Marzaro, Giovanni / Mastrotto, Francesca / Parenti, Rosalba / Russo, Giorgio / Comelli, Albert

    Life (Basel, Switzerland)

    2024  Volume 14, Issue 3

    Abstract: The aim of the present study consists of the evaluation of the biodistribution of a ... ...

    Abstract The aim of the present study consists of the evaluation of the biodistribution of a novel
    Language English
    Publishing date 2024-03-20
    Publishing country Switzerland
    Document type Journal Article
    ZDB-ID 2662250-6
    ISSN 2075-1729
    ISSN 2075-1729
    DOI 10.3390/life14030409
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  3. Article ; Online: Chelation of Theranostic Copper Radioisotopes with S-Rich Macrocycles: From Radiolabelling of Copper-64 to In Vivo Investigation.

    Tosato, Marianna / Verona, Marco / Favaretto, Chiara / Pometti, Marco / Zanoni, Giordano / Scopelliti, Fabrizio / Cammarata, Francesco Paolo / Morselli, Luca / Talip, Zeynep / van der Meulen, Nicholas P / Di Marco, Valerio / Asti, Mattia

    Molecules (Basel, Switzerland)

    2022  Volume 27, Issue 13

    Abstract: Copper radioisotopes are generally employed for cancer imaging and therapy when firmly coordinated via a chelating agent coupled to a tumor-seeking vector. However, the biologically triggered ... ...

    Abstract Copper radioisotopes are generally employed for cancer imaging and therapy when firmly coordinated via a chelating agent coupled to a tumor-seeking vector. However, the biologically triggered Cu
    MeSH term(s) Animals ; Chelating Agents ; Copper Radioisotopes ; Mice ; Mice, Nude ; Positron-Emission Tomography/methods ; Precision Medicine ; Radiopharmaceuticals/metabolism ; Tissue Distribution
    Chemical Substances Chelating Agents ; Copper Radioisotopes ; Radiopharmaceuticals
    Language English
    Publishing date 2022-06-28
    Publishing country Switzerland
    Document type Journal Article
    ZDB-ID 1413402-0
    ISSN 1420-3049 ; 1431-5165 ; 1420-3049
    ISSN (online) 1420-3049
    ISSN 1431-5165 ; 1420-3049
    DOI 10.3390/molecules27134158
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  4. Article ; Online: A New Preclinical Decision Support System Based on PET Radiomics: A Preliminary Study on the Evaluation of an Innovative

    Benfante, Viviana / Stefano, Alessandro / Comelli, Albert / Giaccone, Paolo / Cammarata, Francesco Paolo / Richiusa, Selene / Scopelliti, Fabrizio / Pometti, Marco / Ficarra, Milene / Cosentino, Sebastiano / Lunardon, Marcello / Mastrotto, Francesca / Andrighetto, Alberto / Tuttolomondo, Antonino / Parenti, Rosalba / Ippolito, Massimo / Russo, Giorgio

    Journal of imaging

    2022  Volume 8, Issue 4

    Abstract: The 64Cu-labeled chelator was analyzed in vivo by positron emission tomography (PET) imaging to evaluate its biodistribution in a murine model at different acquisition times. For this purpose, nine 6-week-old female Balb/C nude strain mice underwent ... ...

    Abstract The 64Cu-labeled chelator was analyzed in vivo by positron emission tomography (PET) imaging to evaluate its biodistribution in a murine model at different acquisition times. For this purpose, nine 6-week-old female Balb/C nude strain mice underwent micro-PET imaging at three different time points after 64Cu-labeled chelator injection. Specifically, the mice were divided into group 1 (acquisition 1 h after [64Cu] chelator administration, n = 3 mice), group 2 (acquisition 4 h after [64Cu]chelator administration, n = 3 mice), and group 3 (acquisition 24 h after [64Cu] chelator administration, n = 3 mice). Successively, all PET studies were segmented by means of registration with a standard template space (3D whole-body Digimouse atlas), and 108 radiomics features were extracted from seven organs (namely, heart, bladder, stomach, liver, spleen, kidney, and lung) to investigate possible changes over time in [64Cu]chelator biodistribution. The one-way analysis of variance and post hoc Tukey Honestly Significant Difference test revealed that, while heart, stomach, spleen, kidney, and lung districts showed a very low percentage of radiomics features with significant variations (p-value < 0.05) among the three groups of mice, a large number of features (greater than 60% and 50%, respectively) that varied significantly between groups were observed in bladder and liver, indicating a different in vivo uptake of the 64Cu-labeled chelator over time. The proposed methodology may improve the method of calculating the [64Cu]chelator biodistribution and open the way towards a decision support system in the field of new radiopharmaceuticals used in preclinical imaging trials.
    Language English
    Publishing date 2022-03-30
    Publishing country Switzerland
    Document type Journal Article
    ZDB-ID 2824270-1
    ISSN 2313-433X ; 2313-433X
    ISSN (online) 2313-433X
    ISSN 2313-433X
    DOI 10.3390/jimaging8040092
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  5. Article ; Online: Proton boron capture therapy (PBCT) induces cell death and mitophagy in a heterotopic glioblastoma model.

    Cammarata, Francesco Paolo / Torrisi, Filippo / Vicario, Nunzio / Bravatà, Valentina / Stefano, Alessandro / Salvatorelli, Lucia / D'Aprile, Simona / Giustetto, Pierangela / Forte, Giusi Irma / Minafra, Luigi / Calvaruso, Marco / Richiusa, Selene / Cirrone, Giuseppe Antonio Pablo / Petringa, Giada / Broggi, Giuseppe / Cosentino, Sebastiano / Scopelliti, Fabrizio / Magro, Gaetano / Porro, Danilo /
    Libra, Massimo / Ippolito, Massimo / Russo, Giorgio / Parenti, Rosalba / Cuttone, Giacomo

    Communications biology

    2023  Volume 6, Issue 1, Page(s) 388

    Abstract: Despite aggressive therapeutic regimens, glioblastoma (GBM) represents a deadly brain tumor with significant aggressiveness, radioresistance and chemoresistance, leading to dismal prognosis. Hypoxic microenvironment, which characterizes GBM, is ... ...

    Abstract Despite aggressive therapeutic regimens, glioblastoma (GBM) represents a deadly brain tumor with significant aggressiveness, radioresistance and chemoresistance, leading to dismal prognosis. Hypoxic microenvironment, which characterizes GBM, is associated with reduced therapeutic effectiveness. Moreover, current irradiation approaches are limited by uncertain tumor delineation and severe side effects that comprehensively lead to unsuccessful treatment and to a worsening of the quality of life of GBM patients. Proton beam offers the opportunity of reduced side effects and a depth-dose profile, which, unfortunately, are coupled with low relative biological effectiveness (RBE). The use of radiosensitizing agents, such as boron-containing molecules, enhances proton RBE and increases the effectiveness on proton beam-hit targets. We report a first preclinical evaluation of proton boron capture therapy (PBCT) in a preclinical model of GBM analyzed via μ-positron emission tomography/computed tomography (μPET-CT) assisted live imaging, finding a significant increased therapeutic effectiveness of PBCT versus proton coupled with an increased cell death and mitophagy. Our work supports PBCT and radiosensitizing agents as a scalable strategy to treat GBM exploiting ballistic advances of proton beam and increasing therapeutic effectiveness and quality of life in GBM patients.
    MeSH term(s) Humans ; Glioblastoma/drug therapy ; Glioblastoma/radiotherapy ; Glioblastoma/pathology ; Protons ; Boron ; Mitophagy ; Quality of Life ; Radiation-Sensitizing Agents/pharmacology ; Cell Death ; Tumor Microenvironment
    Chemical Substances Protons ; Boron (N9E3X5056Q) ; Radiation-Sensitizing Agents
    Language English
    Publishing date 2023-04-08
    Publishing country England
    Document type Journal Article ; Research Support, Non-U.S. Gov't
    ISSN 2399-3642
    ISSN (online) 2399-3642
    DOI 10.1038/s42003-023-04770-w
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  6. Article ; Online: Evaluation of proton beam radiation-induced skin injury in a murine model using a clinical SOBP.

    Pisciotta, Pietro / Costantino, Angelita / Cammarata, Francesco Paolo / Torrisi, Filippo / Calabrese, Giovanna / Marchese, Valentina / Cirrone, Giuseppe Antonio Pablo / Petringa, Giada / Forte, Giusi Irma / Minafra, Luigi / Bravatà, Valentina / Gulisano, Massimo / Scopelliti, Fabrizio / Tommasino, Francesco / Scifoni, Emanuele / Cuttone, Giacomo / Ippolito, Massimo / Parenti, Rosalba / Russo, Giorgio

    PloS one

    2020  Volume 15, Issue 5, Page(s) e0233258

    Abstract: The purpose of this paper is to characterize the skin deterministic damage due to the effect of proton beam irradiation in mice occurred during a long-term observational experiment. This study was initially defined to evaluate the insurgence of ... ...

    Abstract The purpose of this paper is to characterize the skin deterministic damage due to the effect of proton beam irradiation in mice occurred during a long-term observational experiment. This study was initially defined to evaluate the insurgence of myelopathy irradiating spinal cords with the distal part of a Spread-out Bragg peak (SOBP). To the best of our knowledge, no study has been conducted highlighting high grades of skin injury at the dose used in this paper. Nevertheless these effects occurred. In this regard, the experimental evidence of significant insurgence of skin injury induced by protons using a SOBP configuration will be shown. Skin damages were classified into six scores (from 0 to 5) according to the severity of the injuries and correlated to ED50 (i.e. the radiation dose at which 50% of animals show a specific score) at 40 days post-irradiation (d.p.i.). The effects of radiation on the overall animal wellbeing have been also monitored and the severity of radiation-induced skin injuries was observed and quantified up to 40 d.p.i.
    MeSH term(s) Animals ; Disease Models, Animal ; Dose-Response Relationship, Radiation ; Injury Severity Score ; Mice ; Proton Therapy/adverse effects ; Radiation Injuries/pathology ; Skin/radiation effects
    Language English
    Publishing date 2020-05-22
    Publishing country United States
    Document type Journal Article ; Research Support, Non-U.S. Gov't
    ISSN 1932-6203
    ISSN (online) 1932-6203
    DOI 10.1371/journal.pone.0233258
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