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Full-Text Articles in Physical Sciences and Mathematics
A Pretargeted Spect Imaging Strategy Employing Technetium-99m Based On Bioorthogonal Diels-Alder Click Chemistry, Justin H. Walsh
A Pretargeted Spect Imaging Strategy Employing Technetium-99m Based On Bioorthogonal Diels-Alder Click Chemistry, Justin H. Walsh
Dissertations, Theses, and Capstone Projects
A series of related N3S 99mTc-peptide complexes were synthesized and tested for use in pretargeting SPECT imaging that utilizes the bioorthogonal Diels-Alder click reaction between tetrazine (Tz) and transcyclooctene (TCO). The objective was to optimize the excretory pathways of the 99mTc-peptide complexes for maximum tumor targeting with the in vivo “click” and minimum non-target uptake. The 99mTc–tetrazine constructs were prepared by reaction of 99mTc-peptide complexes (99mTc-FKC, 99mTc-FKCR, 99mTc-DKC, and 99mTc-SKC) with Tz-NHS or Tz-PEG5-NHS to form 99mTc FK(Tz)C, 99mTc-FK(PEG5-Tz)CR, 99mTc-DK(PEG5-Tz)C, …
Pretargeted Radioimmunotherapy Utilizing The Inverse Electron Demand Diels-Alder Reaction, Rosemery Membreno
Pretargeted Radioimmunotherapy Utilizing The Inverse Electron Demand Diels-Alder Reaction, Rosemery Membreno
Dissertations, Theses, and Capstone Projects
Radioimmunotherapy capitalizes on the specificity and affinity of antibodies for their antigens to localize radioactivity at the tumor site. One limitation in using antibodies is their long circulation time, which can take days to weeks to fully clear from blood circulation. When a radioisotope is directly conjugated to this immunoglobulin vector, the red marrow and other healthy organs are receiving a constant radiation dose while it is in blood circulation. This not only harms healthy organs, but limits the dose of radioactivity that can be administered thus prolonging treatment. A promising alternative to limit the radiation dose to non-tumor tissue …