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| Title: | Application of metal-free triazole formation in the synthesis of cyclic RGD-DTPA conjugates. |
| Author(s): | Berkel, S.S. van (298201674)
Dirks, A.T.
Meeuwissen, S.A.
Pingen, D.L.L.
Boerman, O.C. (074891006)
Laverman, P. (204254523)
Delft, F.L. van (148050832)
Cornelissen, J.J.
Rutjes, F.P.J.T. (107543486) |
| Publication year: | 2008 |
| Document type: | Article / Letter to editor |
| Journal: | Chembiochem |
| ISSN: | 1439-4227 |
| Volume: | vol. 9 |
| Issue: | iss. 11 |
| Start page: | p. 1805 |
| End page: | p. 1815 |
| Abstract: | The tandem 1,3-dipolar cycloaddition-retro-Diels-Alder (tandem crDA) reaction is presented as a versatile method for metal-free chemoselective conjugation of a DTPA radiolabel to N-delta-azido-cyclo(-Arg-Gly-Asp-d-Phe-Orn-) via oxanorbornadiene derivatives. To this end, the behavior of several trifluoromethyl-substituted oxanorbornadiene derivatives in the 1,3-dipolar cycloaddition was studied and optimized to give a clean and efficient method for bio-orthogonal ligation in an aqueous environment. After radioisotope treatment, the resulting 111In-labeled c(RGD)-CF3-triazole-DTPA conjugate was subjected to preliminary biological evaluation and showed high affinity for alpha(v)beta(3) (IC(50)=192 nM) and favorable pharmacokinetics. |
| Subject: | UMCN 1.1: Functional Imaging
UMCN 1.4: Immunotherapy, gene therapy and transplantation |
| Organization: | Nuclear Medicine
Synthetic Organic Chemistry |
| Appears in Collections: | Academic bibliography
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Please use this identifier to cite or link to this item:
http://hdl.handle.net/2066/69882
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