Through a concept we refer to as "Therapeutic In Vivo Synthetic Chemistry", we aim to develop an adaptable system where a cascade of organic transformations can be directly executed at target regions within the body during predefined times to generate a bioactive molecule that elicits a localized biological effect. Towards this goal, we are analyzing, with the use of molecular imaging, the complex pattern recognition mechanisms of natural glycans in vivo and applying the glycan-based interactions to direct various linked biomolecules to desired organs and tissues. Our research has introduced various glycan structures onto proteins, dendrons, and live cells, through the 6π-azaelectrocyclization protocols [1-4], as a means to investigate glycan dependence on in vivo dynamics. Through the use of molecular imaging, results have shown that glycan composition on these templates can directly control accumulation towards specific organ and cancer cells, as well as affect their excretion profiles. We are ultimately challenging to develop a model system where bioactive compounds can be synthesized within living animals, i.e., "Therapeutic In Vivo Synthetic Chemistry". Our preliminary challenge will be discussed in this symposium. [1] K. Tanaka, T. Masuyama, K. Hasegawa, T. Tahara, H. Mizuma, Y. Wada, Y. Watanabe, K. Fukase, Angew. Chem. Int. Ed., 2008, 47, 102-105. [2] K. Tanaka, E. R. O. Siwu, K. Minami, K. Hasegawa, S. Nozaki, Y. Kanayama, K. Koyama, C. W. Chen, J. C. Paulson, Y. Watanabe, K. Fukase, Angew. Chem. Int. Ed., 2010, 49, 8195. [3] K. Fukase, K. Tanaka, Curr. Opin. Chem. Biol., 2012, 16, 614-621. [4] A. Ogura, K. Tanaka, to be submitted.

Therapeutic in vivo synthesis by glycocarriers

249th National Meeting (2015)

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