Nearly all current targeting strategies rely on specific recognition of the endogenous protein receptors; one such technology that has received great success is the antibody/antigen technology. Antibody/antigen technology for cancer targeting, however, has several drawbacks such as large size of both receptor and targeting ligand, limited number of endogenous receptors, immunogenicity, high cost and difficulty of handling of antibody, and synthetic challenges of structure-specific drug-antibody conjugates for immunotherapy. In this talk, I will present the development of an unprecedented in vivo targeting technology based on exogenous introduction of azido group,<sub> </sub>an artificial “antigen”, onto the surface of the target cancer cells followed by highly efficient in vivo Click chemistry to target the introduced azido group. This new targeting technology is essentially the small molecule version of antibody/antigen targeting technology and has several obvious advantages such as much reduced size of receptor/targeting moieties, substantially increased cell-surface receptor numbers, ease of handling and synthesis of both azido-sugars and targeting substrates, low cost, and non-immunogenicity. Substantially reduced toxicity was observed with the use of this small molecule mediated targeting technology followed by chemotherapy. We also successfully demonstrated the use of this technology for nanomedicine in vivo targeting.

Selective <i>in vivo</i> cell labeling mediated cancer targeting and drug delivery

254th National Meeting (2017)

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Selective in vivo cell labeling mediated cancer targeting and drug delivery