Journal
CHEMISTRYOPEN
Volume 3, Issue 2, Pages 48-53Publisher
WILEY-V C H VERLAG GMBH
DOI: 10.1002/open.201402000
Keywords
bioorthogonal chemistry; click chemistry; positron emission tomography (PET); solid-phase peptide synthesis; zirconium-89
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Funding
- US National Institute of Health (NIH) [R01A138468, K25EB016673]
- Brain Tumor Center of Memorial Sloan-Kettering Cancer Center
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The need for post-synthetic modifications and reactive prosthetic groups has long been a limiting factor in the synthesis and study of peptidic and peptidomimetic imaging agents. In this regard, the application of biologically and chemically orthogonal reactions to the design and development of novel radiotracers has the potential to have far-reaching implications in both the laboratory and the clinic. Herein, we report the synthesis and development of a series of modular and versatile building blocks for inverse electron-demand Diels-Alder copper-free click chemistry: tetrazine-functionalized artificial amino acids. Following the development of a novel peptide coupling protocol for peptide synthesis in the presence of tetrazines, we successfully demonstrated its effectiveness and applicability. This versatile methodology has the potential to have a transformational impact, opening the door for the rapid, facile, and modular synthesis of bioorthogonally reactive peptide probes.
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