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Issue 36, 2019
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Synthesis and application of light-switchable arylazopyrazole rapamycin analogs

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Abstract

Rapamycin-induced dimerization of FKBP and FRB has been utilized as a tool for co-localizing two proteins of interest in numerous applications. Due to the tight binding interaction of rapamycin with FKBP and FRB, the ternary complex formation is essentially irreversible. Since biological processes occur in a highly dynamic fashion with cycles of protein association and dissociation to generate a cellular response, it is useful to have chemical tools that function in a similar manner. We have developed arylazopyrazole-modified rapamycin analogs which undergo a configurational change upon light exposure and we observed enhanced ternary complex formation for the cis-isomer over the trans-isomer for one of the analogs.

Graphical abstract: Synthesis and application of light-switchable arylazopyrazole rapamycin analogs

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Publication details

The article was received on 04 Aug 2019, accepted on 27 Aug 2019 and first published on 30 Aug 2019


Article type: Communication
DOI: 10.1039/C9OB01719D
Org. Biomol. Chem., 2019,17, 8348-8353

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    Synthesis and application of light-switchable arylazopyrazole rapamycin analogs

    T. M. Courtney, T. J. Horst, C. P. Hankinson and A. Deiters, Org. Biomol. Chem., 2019, 17, 8348
    DOI: 10.1039/C9OB01719D

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