Affiliation:
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
AbstractPuromycin derivatives containing an emissive thieno[3,4‐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.
Funder
National Institute of General Medical Sciences