دورية أكاديمية
Synthesis and preliminary in vitro evaluation of DOTA-Tenatumomab conjugates for theranostic applications in tenascin expressing tumors
| العنوان: | Synthesis and preliminary in vitro evaluation of DOTA-Tenatumomab conjugates for theranostic applications in tenascin expressing tumors |
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| المؤلفون: | Giannini G., Milazzo F. M., Battistuzzi G., Rosi A., Anastasi A. M., Petronzelli F., Albertoni C., Tei L., Leone L., Salvini L., De Santis R. |
| المساهمون: | Giannini, G., Milazzo, F. M., Battistuzzi, G., Rosi, A., Anastasi, A. M., Petronzelli, F., Albertoni, C., Tei, L., Leone, L., Salvini, L., De Santis, R. |
| سنة النشر: | 2019 |
| المجموعة: | Università degli Studi del Piemonte Orientale: CINECA IRIS |
| مصطلحات موضوعية: | Cancer, Chelating ligand, Radionuclide therapy, Tenascin, Tenatumomab, Theranostic |
| الوصف: | Tenatumomab is an anti-tenascin murine monoclonal antibody previously used in clinical trials for delivering radionuclides to tumors by both pre-targeting (biotinylated Tenatumomab within PAGRIT) and direct 131Iodine labeling approaches. Here we present the synthesis and in vitro characterization of three Tenatumomab con-jugates to bifunctional chelating agents (NHS-DOTA, NCS-DOTA and NCS-DTPA). Results indicate ST8198AA1(Tenatumomab-DOTAMA, derived by conjugation of NHS-DOTA), as the most promising candidate in terms ofconjugation rate andyield, stability,antigenimmunoreactivity andaffinity. Labeling efficiency of thedifferentchelators was investigated with a panel of cold metals indicating DOTAMA as the best chelator. Labeling ofTenatumomab-DOTAMA was then optimized with several metals and stability performed confirms suitability of this conjugate for further development. ST8198AA1 represents an improvement of the previous antibody forms because the labeling with radionuclides like177Lu or64Cu would allow theranostic applications in patientsbearing tenascin expressing tumors |
| نوع الوثيقة: | article in journal/newspaper |
| وصف الملف: | STAMPA |
| اللغة: | English |
| العلاقة: | info:eu-repo/semantics/altIdentifier/pmid/31208798; info:eu-repo/semantics/altIdentifier/wos/WOS:000476649400005; volume:27; firstpage:3248; lastpage:3253; numberofpages:6; journal:BIOORGANIC & MEDICINAL CHEMISTRY; http://hdl.handle.net/11579/104245Test; info:eu-repo/semantics/altIdentifier/scopus/2-s2.0-85067197804; http://www.journals.elsevier.com/bioorganic-and-medicinal-chemistryTest/ |
| DOI: | 10.1016/j.bmc.2019.05.047 |
| الإتاحة: | https://doi.org/10.1016/j.bmc.2019.05.047Test http://hdl.handle.net/11579/104245Test http://www.journals.elsevier.com/bioorganic-and-medicinal-chemistryTest/ |
| حقوق: | info:eu-repo/semantics/openAccess |
| رقم الانضمام: | edsbas.1EBA013C |
| قاعدة البيانات: | BASE |
| DOI: | 10.1016/j.bmc.2019.05.047 |
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