Cycloheximide is an inhibitor of protein biosynthesis in eukaryotic organisms, produced by the bacterium Streptomyces griseus. Cycloheximide exerts its effect by interfering with the translocation step in protein synthesis (movement of two tRNA molecules and mRNA in relation to the ribosome) thus blocking translational elongation. Cycloheximide is widely used in biomedical research to inhibit protein synthesis in eukaryotic cells studied in vitro (i.e. outside of organisms). It is inexpensive and works rapidly. Its effects are rapidly reversed by simply removing it from the culture medium.
Cycloheximide is a highly effective antibiotic with activity against mold, yeast, and phytopathogenic fungi, with lower activity against bacteria. It has been reported to inhibit the synthesis of both proteins and macromolecules, as well as affect apoptosis in eukaryotes. Inhibition of protein synthesis is believed to be mediated through DNA translation arrest, as demonstrated in rat thymocytes. Although cycloheximide has been reported to induce apoptosis in various cells, it has also been shown to inhibit or delay induced apoptosis. These observations suggest that cycloheximide's effect on apoptosis may not be solely through protein translation arrest and that other mechanisms may be involved. Cycloheximide has also been reported to inhibit FKBP12 (peptidylprolylisomerase hFKBP12, PPIase hFKBP12) via competitive inhibition.
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