Modular One-Pot Strategy for the Synthesis of Heterobivalent Tracers
| dc.rights.license | open | en_US |
| dc.contributor.author | BAILLY, Thibaud | |
| hal.structure.identifier | Institut de Neurosciences cognitives et intégratives d'Aquitaine [INCIA] | |
| dc.contributor.author | BODIN, Sacha | |
| dc.contributor.author | GONCALVES, Victor | |
| dc.contributor.author | DENAT, Franck | |
| hal.structure.identifier | Institut de Neurosciences cognitives et intégratives d'Aquitaine [INCIA] | |
| dc.contributor.author | MORGAT, Clement | |
| dc.contributor.author | PRIGNON, Aurelie | |
| dc.contributor.author | VALVERDE, Ibai E | |
| dc.date.accessioned | 2023-06-28T12:08:01Z | |
| dc.date.available | 2023-06-28T12:08:01Z | |
| dc.date.issued | 2023-05-11 | |
| dc.identifier.issn | 1948-5875 | en_US |
| dc.identifier.uri | https://oskar-bordeaux.fr/handle/20.500.12278/183228 | |
| dc.description.abstractEn | Bivalent ligands, i.e., molecules having two ligands covalently connected by a linker, have been gathering attention since the first description of their pharmacological potential in the early 80s. However, their synthesis, particularly of labeled heterobivalent ligands, can still be cumbersome and time-consuming. We herein report a straightforward procedure for the modular synthesis of labeled heterobivalent ligands (HBLs) using dual reactive 3,6-dichloro-1,2,4,5-tetrazine as a starting material and suitable partners for sequential SAr and inverse electron-demand Diels-Alder (IEDDA) reactions. This assembly method conducted in a stepwise or in a sequential one-pot manner provides quick access to multiple HBLs. A conjugate combining ligands toward the prostate-specific membrane antigen (PSMA) and the gastrin-releasing peptide receptor (GRPR) was radiolabeled, and its biological activity was assessed and (receptor binding affinity, biodistribution, imaging) as an illustration that the assembly methodology preserves the tumor targeting properties of the ligands. | |
| dc.description.sponsorship | France Life Imaging - ANR-11-INBS-0006 | en_US |
| dc.language.iso | EN | en_US |
| dc.subject.en | Bioconjugation | |
| dc.subject.en | Click chemistry | |
| dc.subject.en | Drug delivery | |
| dc.subject.en | Heterobivalent ligands | |
| dc.subject.en | Radiopharmaceuticals | |
| dc.title.en | Modular One-Pot Strategy for the Synthesis of Heterobivalent Tracers | |
| dc.title.alternative | ACS Med Chem Lett | en_US |
| dc.type | Article de revue | en_US |
| dc.identifier.doi | 10.1021/acsmedchemlett.3c00057 | en_US |
| dc.subject.hal | Sciences du Vivant [q-bio]/Neurosciences [q-bio.NC] | en_US |
| dc.identifier.pubmed | 37197474 | en_US |
| bordeaux.journal | ACS Medicinal Chemistry Letters | en_US |
| bordeaux.page | 636-644 | en_US |
| bordeaux.volume | 14 | en_US |
| bordeaux.hal.laboratories | Institut de neurosciences cognitives et intégratives d'Aquitaine (INCIA) - UMR 5287 | en_US |
| bordeaux.issue | 5 | en_US |
| bordeaux.institution | Université de Bordeaux | en_US |
| bordeaux.institution | CNRS | en_US |
| bordeaux.team | Imagerie multimodale translationnelle | |
| bordeaux.peerReviewed | oui | en_US |
| bordeaux.inpress | non | en_US |
| bordeaux.import.source | pubmed | |
| hal.export | false | |
| workflow.import.source | pubmed | |
| dc.rights.cc | Pas de Licence CC | en_US |
| bordeaux.COinS | ctx_ver=Z39.88-2004&rft_val_fmt=info:ofi/fmt:kev:mtx:journal&rft.jtitle=ACS%20Medicinal%20Chemistry%20Letters&rft.date=2023-05-11&rft.volume=14&rft.issue=5&rft.spage=636-644&rft.epage=636-644&rft.eissn=1948-5875&rft.issn=1948-5875&rft.au=BAILLY,%20Thibaud&BODIN,%20Sacha&GONCALVES,%20Victor&DENAT,%20Franck&MORGAT,%20Clement&rft.genre=article |
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