A novel 18F-labelled tetrazine ester prosthetic group for improved radiolabelling and in vivo stability of proteins and peptides [PDF]
Background Monoclonal antibodies, engineered protein scaffolds, and peptides are increasingly important in therapy and diagnostics owing to their high specificity and affinity.
Francesco Lechi +5 more
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Efficient Approaches to the Design of Six-Membered Polyazacyclic Compounds—Part 1: Aromatic Frameworks [PDF]
This review summarises the possible applications and basic methodologies for the synthesis of six-membered polyazo heterocycles, namely, diazines, triazines, and tetrazines.
Elena A. Gyrgenova +2 more
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Click-to-Release for Controlled Immune Cell Activation: Tumor-Targeted Unmasking of an IL12 Prodrug [PDF]
Objectives: Immunotherapy utilizing immune-stimulating cytokines such as IL12 holds great promise for the treatment of cancer. However, clinical use of IL12 is hampered due to severe toxicity following systemic administration.
Martijn H. den Brok +8 more
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MODIFICATION OF [18F]FDG BY THE FORMATION OF A HYDRAZONE BOND [PDF]
Purpose: The [18F]-fluorodeoxyglucose ([18F]-FDG) is known to be one of the most used radio-pharmaceuticals for positron emission tomography. [18F]-FDG allows the assessment of glycolytic activity, which is more enhanced in tumor cells than in normal ...
Gergana Simeonova, Boyan Todorov
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Overview of Syntheses and Molecular-Design Strategies for Tetrazine-Based Fluorogenic Probes
Various bioorthogonal chemistries have been used for fluorescent imaging owing to the advantageous reactions they employ. Recent advances in bioorthogonal chemistry have revolutionized labeling strategies for fluorescence imaging, with inverse electron ...
Sang-Kee Choi, Jonghoon Kim, Eunha Kim
doaj +1 more source
Herein, we tune the redox potential of 3,6-diphenyl-1,2,4,5-tetrazine (DPT) by introducing various electron-donating/withdrawing groups (methoxy, t-butyl, H, F, and trifluoromethyl) into its two peripheral benzene rings for use as electrode material in a
Dong Joo Min +4 more
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A 99mTc-Labelled Tetrazine for Bioorthogonal Chemistry. Synthesis and Biodistribution Studies with Small Molecule trans-Cyclooctene Derivatives. [PDF]
A convenient strategy to radiolabel a hydrazinonicotonic acid (HYNIC)-derived tetrazine with 99mTc was developed, and its utility for creating probes to image bone metabolism and bacterial infection using both active and pretargeting strategies was ...
Alyssa Vito +13 more
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Pretargeted nuclear imaging for the diagnosis of various cancers is an emerging and fast developing field. The tetrazine ligation is currently considered the most promising reaction in this respect. Monoclonal antibodies are often the preferred choice as
Christian B. M. Poulie +6 more
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IEDDA: An Attractive Bioorthogonal Reaction for Biomedical Applications
The pretargeting strategy has recently emerged in order to overcome the limitations of direct targeting, mainly in the field of radioimmunotherapy (RIT).
Maryana Handula +2 more
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Tetrazine-Containing Amino Acid for Peptide Modification and Live Cell Labeling. [PDF]
A novel amino acid derivative 3-(4-(1, 2, 4, 5-tetrazine-3-yl) phenyl)-2-aminopropanoic acid was synthesized in this study. The compound possessed better water-solubility and was synthesized more easily compared with the well-known and commercially ...
Zhongqiu Ni +4 more
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