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Discovery of a near-IR photorelease technique for targeted drug delivery

Wednesday, September 24, 2014 — Poster Session IV

10:00 a.m. –12:00 p.m.

FAES Academic Center



* FARE Award Winner


  • A.P. Gorka
  • R.R. Nani
  • M.J. Schnermann


The development of near-IR light-activated photocaging strategies would offer new tools for basic research and enable spatial and temporal control of drug delivery without the limitations of UV-based approaches. We have developed a near-IR light-promoted uncaging strategy that releases phenol- or amine-containing small molecules. The approach uses previously unexploited photodecomposition chemistry of heptamethine cyanine fluorophores. The reaction sequence is initiated by low intensity 690 nm light and is equally effective in simple aqueous buffer and in complex biological mixtures. The broader utility of this approach is demonstrated through a caged version of the estrogen receptor antagonist, 4-hydroxycyclofen. Utilizing this construct in concert with CreER/LoxP reporter recombination in transgenic MEF cells, we effect near-IR light-controlled gene expression. We also demonstrate near-IR light-dependent cytotoxicity of a tamoxifen-sensitive tumor cell line, with similar potency to the native drug. Importantly, these effects are absent upon release of inactive small molecules. Efforts to apply this approach towards the targeted delivery of potent cytotoxic small molecules are ongoing.

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