Inherently Emissive Puromycin Analogues for Live Cell Labelling |
| |
| Authors: | Kaivin Hadidi Kfir B Steinbuch Lara E Dozier Prof Dr Gentry N Patrick Prof Dr Yitzhak Tor |
| |
| Institution: | 1. Department of Chemistry and Biochemistry, University of California, San Diego, La Jolla, CA, 92093-0358 USA;2. Section of Neurobiology, Division of Biological Sciences, University of California, San Diego, La Jolla, CA, 92093-0347 USA |
| |
| Abstract: | Puromycin derivatives containing an emissive thieno3,4-d]-pyrimidine core, modified with azetidine and 3,3-difluoroazetidine as Me2N surrogates, exhibit translation inhibition and bactericidal activity similar to the natural antibiotic. The analogues are capable of cellular puromycylation of nascent peptides, generating emissive products without any follow-up chemistry. The 3,3-difluoroazetidine-containing analogue is shown to fluorescently label newly translated peptides and be visualized in both live and fixed HEK293T cells and rat hippocampal neurons. |
| |
| Keywords: | Antibiotics Fluorescence Heterocycles Labelling Modified Nucleosides |
|
|
