The Influence of Glycans-Specific Bioconjugation on the FcγRI Binding and <i>In vivo</i> Performance of <sup>89</sup>Zr-DFO-Pertuzumab

Vivier, Delphine; Fung, Kimberly; Rodriguez, Cindy; Adumeau, Pierre; Ulaner, Gary A.; Lewis, Jason S.; Sharma, Sai Kiran; Zeglis, Brian M.

doi:10.7150/thno.39089

Cited by 38 publications

(47 citation statements)

References 40 publications

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“…PET imaging and biodistribution experiments in athymic nude mice bearing BT474 xenografts yielded no significant differences in the behavior of the non-site-specific and site-specific 89 Zr-tagged mAbs. Nevertheless, experiments in tumor-bearing huNSG mice revealed that site-specific RICs produces higher tumor uptake and lower activity concentrations in non-target tissues (e.g., liver and spleen) than the non-site-specifically labeled counterpart, a phenomenon that may be due to the altered binding of the formers to huFcγRI [145]. Notably, 89 Zr-DFO-ss pertuzumab-EndoS was the best performing adduct.…”

Section: Galactosyltransferase-mediated Conjugation In MImentioning

confidence: 97%

“…Furthermore, site-specific 89 Zr-DFO-trastuzumab exhibited superior tumortargeting properties in the SK-OV-3 model. Likewise, Vivier et al also explored in a comparative study the effects of the above chemo-enzymatic approach of site-specific bioconjugation on the in vivo performance of selected RICs (Table 7 panel E) [145]. The truncation of the heavy chain glycans of the RIC was expected to reduce its off-target uptake and increase the tumor accumulation [146].…”

Section: Galactosyltransferase-mediated Conjugation In MImentioning

confidence: 99%

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Enzymatic Methods for the Site-Specific Radiolabeling of Targeting Proteins

Bolzati

Spolaore

2021

Molecules

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Site-specific conjugation of proteins is currently required to produce homogenous derivatives for medicine applications. Proteins derivatized at specific positions of the polypeptide chain can actually show higher stability, superior pharmacokinetics, and activity in vivo, as compared with conjugates modified at heterogeneous sites. Moreover, they can be better characterized regarding the composition of the derivatization sites as well as the conformational and activity properties. To this aim, several site-specific derivatization approaches have been developed. Among these, enzymes are powerful tools that efficiently allow the generation of homogenous protein–drug conjugates under physiological conditions, thus preserving their native structure and activity. This review will summarize the progress made over the last decade on the use of enzymatic-based methodologies for the production of site-specific labeled immunoconjugates of interest for nuclear medicine. Enzymes used in this field, including microbial transglutaminase, sortase, galactosyltransferase, and lipoic acid ligase, will be overviewed and their recent applications in the radiopharmaceutical field will be described. Since nuclear medicine can benefit greatly from the production of homogenous derivatives, we hope that this review will aid the use of enzymes for the development of better radio-conjugates for diagnostic and therapeutic purposes.

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Section: Galactosyltransferase-mediated Conjugation In MImentioning

confidence: 97%

Section: Galactosyltransferase-mediated Conjugation In MImentioning

confidence: 99%

Enzymatic Methods for the Site-Specific Radiolabeling of Targeting Proteins

Bolzati

Spolaore

2021

Molecules

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“…Indium-111 is the second most-used radionuclide, followed by radioisotopes of iodine [59] . More recently, positron-emitting radionuclides such as Flour-18, Manganez-52, Zirconium-89 [60] have been increasingly used, reflecting the growing interest in positron emission tomography (PET) imaging and the increasing availability of preclinical and clinical PET scanners in radiopharmacy and nuclear medicine applications [54] . Another important parameter for the selection of radiation types are the energy levels of the emitters.…”

Section: The Application Of Imaging Modalities In Nanomedicine Fieldmentioning

confidence: 99%

Current update on nanoplatforms as therapeutic and diagnostic tools: A review for the materials used as nanotheranostics and imaging modalities

Sıafaka

Okur

Karantas

et al. 2021

Asian Journal of Pharmaceutical Sciences

121

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In the last decade, the use of nanotheranostics as emerging diagnostic and therapeutic tools for various diseases, especially cancer, is held great attention. Up to date, several approaches have been employed in order to develop smart nanotheranostics, which combine bioactive targeting on specific tissues as well as diagnostic properties. The nanotheranostics can deliver therapeutic agents by concomitantly monitor the therapy response in real-time. Consequently, the possibility of over- or under-dosing is decreased. Various non-invasive imaging techniques have been used to quantitatively monitor the drug delivery processes. Radiolabeling of nanomaterials is widely used as powerful diagnostic approach on nuclear medicine imaging. In fact, various radiolabeled nanomaterials have been designed and developed for imaging tumors and other lesions due to their efficient characteristics. Inorganic nanoparticles as gold, silver, silica based nanomaterials or organic nanoparticles as polymers, carbon based nanomaterials, liposomes have been reported as multifunctional nanotheranostics. In this review, the imaging modalities according to their use in various diseases are summarized, providing special details for radiolabeling. In further, the most current nanotheranostics categorized via the used nanomaterials are also summed up. To conclude, this review can be beneficial for medical and pharmaceutical society as well as material scientists who work in the field of nanotheranostics since they can use this research as guide for producing newer and more efficient nanotheranostics.

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“…Ex vivo biodistribution data confirmed similar radiotracer tumor uptake of site-specifically glycan modified and randomly bioconjugated [ 89 Zr]Zr-DFO-pertuzumab at 144 h p.i in athymic nude mice. On the other hand, in humanized NOD-SCID animals a significant difference was observed using an identical experimental set-up [ 47 ]. This study confirms the importance of site-specific biomodifications in immuno-PET/SPECT and also shows the added benefit of glycan modification in avoiding Fc-FcγR binding, promoting retention in the vascular space and allowing more time for immune interactions.…”

Section: Radiolabeling and Bioconjugation Strategies Of Monoclonalmentioning

confidence: 99%

Development of Antibody Immuno-PET/SPECT Radiopharmaceuticals for Imaging of Oncological Disorders—An Update

Dewulf

Adhikari

Vangestel

et al. 2020

Cancers

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Positron emission tomography (PET) and single-photon emission computed tomography (SPECT) are molecular imaging strategies that typically use radioactively labeled ligands to selectively visualize molecular targets. The nanomolar sensitivity of PET and SPECT combined with the high specificity and affinity of monoclonal antibodies have shown great potential in oncology imaging. Over the past decades a wide range of radio-isotopes have been developed into immuno-SPECT/PET imaging agents, made possible by novel conjugation strategies (e.g., site-specific labeling, click chemistry) and optimization and development of novel radiochemistry procedures. In addition, new strategies such as pretargeting and the use of antibody fragments have entered the field of immuno-PET/SPECT expanding the range of imaging applications. Non-invasive imaging techniques revealing tumor antigen biodistribution, expression and heterogeneity have the potential to contribute to disease diagnosis, therapy selection, patient stratification and therapy response prediction achieving personalized treatments for each patient and therefore assisting in clinical decision making.

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The Influence of Glycans-Specific Bioconjugation on the FcγRI Binding and In vivo Performance of ⁸⁹Zr-DFO-Pertuzumab

Cited by 38 publications

References 40 publications

Enzymatic Methods for the Site-Specific Radiolabeling of Targeting Proteins

Enzymatic Methods for the Site-Specific Radiolabeling of Targeting Proteins

Current update on nanoplatforms as therapeutic and diagnostic tools: A review for the materials used as nanotheranostics and imaging modalities

Development of Antibody Immuno-PET/SPECT Radiopharmaceuticals for Imaging of Oncological Disorders—An Update

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The Influence of Glycans-Specific Bioconjugation on the FcγRI Binding and In vivo Performance of 89Zr-DFO-Pertuzumab

Cited by 38 publications

References 40 publications

Enzymatic Methods for the Site-Specific Radiolabeling of Targeting Proteins

Enzymatic Methods for the Site-Specific Radiolabeling of Targeting Proteins

Current update on nanoplatforms as therapeutic and diagnostic tools: A review for the materials used as nanotheranostics and imaging modalities

Development of Antibody Immuno-PET/SPECT Radiopharmaceuticals for Imaging of Oncological Disorders—An Update

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The Influence of Glycans-Specific Bioconjugation on the FcγRI Binding and In vivo Performance of ⁸⁹Zr-DFO-Pertuzumab