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Bioconjugation of a Fibroblast Activation Protein Targeted Interleukin-4

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    Bioconjugation of a Fibroblast Activation Protein Targeted Interleukin-4
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    • Matthias Ruopp
      Matthias Ruopp
      Institute of Pharmacy and Food Chemistry, University of Würzburg, Am Hubland, 97074 Würzburg, Germany
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    • Sha Zhu
      Sha Zhu
      Department of Nuclear Medicine, Translational Research Center, Friedrich-Alexander University (FAU), Schwabachanlage 12, 91054 Erlangen, Germany
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    • Rafael Worschech
      Rafael Worschech
      Institute of Pharmacy and Food Chemistry, University of Würzburg, Am Hubland, 97074 Würzburg, Germany
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    • Dorothee Haas
      Dorothee Haas
      Institute of Pharmacy and Food Chemistry, University of Würzburg, Am Hubland, 97074 Würzburg, Germany
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    • Simone Maschauer
      Simone Maschauer
      Department of Nuclear Medicine, Translational Research Center, Friedrich-Alexander University (FAU), Schwabachanlage 12, 91054 Erlangen, Germany
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      Orcidhttps://orcid.org/0000-0002-6550-933X
    • Olaf Prante
      Olaf Prante
      Department of Nuclear Medicine, Translational Research Center, Friedrich-Alexander University (FAU), Schwabachanlage 12, 91054 Erlangen, Germany
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      Orcidhttps://orcid.org/0000-0003-0247-3656
    • Lorenz Meinel
      Lorenz Meinel
      Institute of Pharmacy and Food Chemistry, University of Würzburg, Am Hubland, 97074 Würzburg, Germany
      Helmholtz Institute for RNA-Based Infection Research (HIRI), Helmholtz Center for Infection Research (HZI), 97080 Würzburg, Germany
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      Orcidhttps://orcid.org/0000-0002-7549-7627
    • Tessa Lühmann*
      Tessa Lühmann
      Institute of Pharmacy and Food Chemistry, University of Würzburg, Am Hubland, 97074 Würzburg, Germany
      *[email protected]
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      Orcidhttps://orcid.org/0000-0001-7552-6435
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    ACS Biomaterials Science & Engineering

    Cite this: ACS Biomater. Sci. Eng. 2023, 9, 10, 5580–5588
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    https://doi.org/10.1021/acsbiomaterials.3c00879
    Published September 18, 2023
    Copyright © 2023 The Authors. Published by American Chemical Society
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    Abstract

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    Interleukin-4 (IL-4) is an immune-modulating therapeutic with growing potential for the treatment of inflammatory diseases. Current challenges of IL-4 therapy include a low serum half-life and pleiotropic activity, suggesting effective targeting of IL-4. To develop an interleukin-4 bioconjugate with rapid targeting to inflammatory disease sites, we report the chemical synthesis, bioconjugation, and in vitro characterization of a murine interleukin-4 (mIL-4) conjugate decorated with a fibroblast activation protein inhibitor (FAPI). The FAPI targeting moiety features 2,2′,2″,2‴-(1,4,7,10-tetraazacyclododecane-1,4,7,10-tetrayl)tetraacetic acid (DOTA) to allow future biodistribution and imaging studies of the FAPI-mIL-4 bioconjugate. We demonstrated site-specific coupling of mIL-4 and FAPI-DOTA deploying chemo-enzyme and enzyme chemistries with a high purity exceeding 95%. The FAPI-DOTA modified mIL-4 was bioactive with polarization of murine macrophages into the M2 state while maintaining specific binding to FAP on fibroblast cells. Together, these results point to future in vivo use of the FAPI-mIL-4 bioconjugate to assess biodistribution and biological effects in animal models of inflammatory joint disease.

    Copyright © 2023 The Authors. Published by American Chemical Society

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    The Supporting Information is available free of charge at https://pubs.acs.org/doi/10.1021/acsbiomaterials.3c00879.

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    This article is cited by 1 publications.

    1. Hongyan Qian, Chaoqiong Deng, Shiju Chen, Xinwei Zhang, Yan He, Jingying Lan, Aodi Wang, Guixiu Shi, Yuan Liu. Targeting pathogenic fibroblast-like synoviocyte subsets in rheumatoid arthritis. Arthritis Research & Therapy 2024, 26 (1) https://doi.org/10.1186/s13075-024-03343-4
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    ACS Biomaterials Science & Engineering

    Cite this: ACS Biomater. Sci. Eng. 2023, 9, 10, 5580–5588
    Click to copy citationCitation copied!
    https://doi.org/10.1021/acsbiomaterials.3c00879
    Published September 18, 2023
    Copyright © 2023 The Authors. Published by American Chemical Society
    Request reuse permissions

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