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  1. Article ; Online: Fundamental evaluation regarding the relationship between albumin-binding and tumor accumulation of PSMA-targeting radioligands.

    Kazuta, Nobuki / Tsuchihashi, Shohei / Watanabe, Hiroyuki / Ono, Masahiro

    Annals of nuclear medicine

    2024  

    Abstract: Objective: The marked success of prostate-specific membrane antigen (PSMA)-targeting radioligands with albumin binder (ALB) is attributed to the improvement of blood retention and tumor accumulation. [: Method: The [: Results: The [: Conclusions! ...

    Abstract Objective: The marked success of prostate-specific membrane antigen (PSMA)-targeting radioligands with albumin binder (ALB) is attributed to the improvement of blood retention and tumor accumulation. [
    Method: The [
    Results: The [
    Conclusions: These results indicate that the moderate reversible binding of ALB with albumin, not covalent binding, may play a critical role in enhancing the tumor accumulation of PSMA-targeting radioligands.
    Language English
    Publishing date 2024-04-27
    Publishing country Japan
    Document type Journal Article
    ZDB-ID 1146984-5
    ISSN 1864-6433 ; 0914-7187
    ISSN (online) 1864-6433
    ISSN 0914-7187
    DOI 10.1007/s12149-024-01930-8
    Database MEDical Literature Analysis and Retrieval System OnLINE

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    In stock of ZB MED Cologne/Königswinter

    Zs.A 3657: Show issues Location:
    Je nach Verfügbarkeit (siehe Angabe bei Bestand)
    bis Jg. 1994: Bestellungen von Artikeln über das Online-Bestellformular
    Jg. 1995 - 2021: Lesesall (2.OG)
    ab Jg. 2022: Lesesaal (EG)

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  2. Article ; Online: Synthesis and evaluation of novel trifunctional chelating agents for pretargeting approach using albumin binder to improve tumor accumulation.

    Tsuchihashi, Shohei / Nakashima, Kazuma / Watanabe, Hiroyuki / Ono, Masahiro

    Nuclear medicine and biology

    2024  Volume 132-133, Page(s) 108911

    Abstract: Introduction: The pretargeting approach consists of in vivo ligation between pre-injected antibodies and low-molecular-weight radiolabeled effectors. The advantage of the pretargeting approach is to improve a tumor-to-background ratio, but the ... ...

    Abstract Introduction: The pretargeting approach consists of in vivo ligation between pre-injected antibodies and low-molecular-weight radiolabeled effectors. The advantage of the pretargeting approach is to improve a tumor-to-background ratio, but the disadvantage is to compromise tumor accumulation. In this study, we applied albumin binder (ALB) to the pretargeting approach to overcome low tumor accumulation.
    Methods: We synthesized two novel trifunctional effectors containing an ALB moiety, a chelator, and a different tetrazine and two corresponding effectors without an ALB moiety. Albumin-binding assays and stability assays were performed using
    Results: In albumin-binding assays, ALB-containing effectors exhibited a marked binding to albumin. Two ALB-containing effectors showed the difference in the reactivity and the slight difference in the stability. In biodistribution studies without the pretargeting approach, two ALB-containing effectors showed different pharmacokinetics in blood retention. With the pretargeting approach, the tumor accumulation was improved by the introduction of ALB and the highest tumor accumulation was observed in using the ALB-containing effector with higher blood retention.
    Conclusion: These results suggest that the application of ALB to the pretargeting approach is effective to improve tumor accumulation, and the structure of tetrazine influences the utility of ALB-containing effectors.
    Language English
    Publishing date 2024-04-05
    Publishing country United States
    Document type Journal Article
    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.2024.108911
    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:
    Je nach Verfügbarkeit (siehe Angabe bei Bestand)
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    Jg. 1995 - 2021: Lesesall (1.OG)
    ab Jg. 2022: Lesesaal (EG)

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  3. Article ; Online: Development of Novel

    Tsuchihashi, Shohei / Nakashima, Kazuma / Tarumizu, Yuta / Ichikawa, Hiroaki / Jinda, Hiroki / Watanabe, Hiroyuki / Ono, Masahiro

    Journal of medicinal chemistry

    2023  Volume 66, Issue 12, Page(s) 8043–8053

    Abstract: Prostate-specific membrane antigen (PSMA) is a promising target for metastatic castration-resistant prostate cancer. We previously reported the effectiveness of PSMA-DA1 as a PSMA-targeting radiotheranostic agent containing an albumin binder moiety. To ... ...

    Abstract Prostate-specific membrane antigen (PSMA) is a promising target for metastatic castration-resistant prostate cancer. We previously reported the effectiveness of PSMA-DA1 as a PSMA-targeting radiotheranostic agent containing an albumin binder moiety. To further enhance tumor uptake, we newly designed PSMA-NAT-DA1 (PNT-DA1) by the introduction of a lipophilic linker into PSMA-DA1. The PSMA affinity of [
    MeSH term(s) Humans ; Male ; Albumins ; Antigens, Surface ; Cell Line, Tumor ; Glutamate Carboxypeptidase II ; Indium/chemistry ; Prostatic Neoplasms/pathology ; Radiopharmaceuticals/therapeutic use ; Single Photon Emission Computed Tomography Computed Tomography ; Indium Radioisotopes/chemistry ; Indium Radioisotopes/therapeutic use
    Chemical Substances Albumins ; Antigens, Surface ; Glutamate Carboxypeptidase II (EC 3.4.17.21) ; Indium (045A6V3VFX) ; Radiopharmaceuticals ; Indium Radioisotopes
    Language English
    Publishing date 2023-06-07
    Publishing country United States
    Document type Journal Article ; Research Support, Non-U.S. Gov't
    ZDB-ID 218133-2
    ISSN 1520-4804 ; 0022-2623
    ISSN (online) 1520-4804
    ISSN 0022-2623
    DOI 10.1021/acs.jmedchem.3c00346
    Database MEDical Literature Analysis and Retrieval System OnLINE

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    In stock of ZB MED Cologne/Königswinter

    Zs.B 151: Show issues Location:
    Je nach Verfügbarkeit (siehe Angabe bei Bestand)
    bis Jg. 2021: Bestellungen von Artikeln über das Online-Bestellformular
    ab Jg. 2022: Lesesaal (EG)
    Zs.MB 1: Show issues

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  4. Article ; Online: Synthesis and Evaluation of Novel

    Iikuni, Shimpei / Tarumizu, Yuta / Tsuchihashi, Shohei / Ohara, Takaki / Watanabe, Hiroyuki / Ono, Masahiro

    Molecular pharmaceutics

    2022  Volume 19, Issue 8, Page(s) 2725–2736

    Abstract: Picolinic acid-based metallic chelators, e.g., neunpa and octapa, have attracted much attention as promising scaffolds for radiotheranostic agents, particularly those containing larger α-emitting radiometals. Furthermore, albumin binder (ALB) moieties, ... ...

    Abstract Picolinic acid-based metallic chelators, e.g., neunpa and octapa, have attracted much attention as promising scaffolds for radiotheranostic agents, particularly those containing larger α-emitting radiometals. Furthermore, albumin binder (ALB) moieties, which noncovalently bind to albumin, have been utilized to improve the pharmacokinetics of radioligands targeting various biomolecules. In this study, we designed and synthesized novel neunpa and octapa derivatives (Neunpa-2 and Octapa-2, respectively), which contained a prostate-specific membrane antigen (PSMA)-binding moiety (model targeting vector) and an ALB moiety. We evaluated the fundamental properties of these derivatives as radiotheranostic agents using
    MeSH term(s) Albumins/chemistry ; Animals ; Antigens, Surface/metabolism ; Cell Line, Tumor ; Glutamate Carboxypeptidase II/metabolism ; Humans ; Indium ; Male ; Mice ; Picolinic Acids ; Prostatic Neoplasms/diagnostic imaging ; Prostatic Neoplasms/drug therapy ; Prostatic Neoplasms/metabolism ; Radiopharmaceuticals/chemistry ; Tissue Distribution
    Chemical Substances Albumins ; Antigens, Surface ; Picolinic Acids ; Radiopharmaceuticals ; Indium (045A6V3VFX) ; Glutamate Carboxypeptidase II (EC 3.4.17.21) ; picolinic acid (QZV2W997JQ)
    Language English
    Publishing date 2022-06-25
    Publishing country United States
    Document type Journal Article
    ZDB-ID 2138405-8
    ISSN 1543-8392 ; 1543-8384
    ISSN (online) 1543-8392
    ISSN 1543-8384
    DOI 10.1021/acs.molpharmaceut.2c00071
    Database MEDical Literature Analysis and Retrieval System OnLINE

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    In stock of ZB MED Cologne/Königswinter

    Zs.A 6250: Show issues Location:
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