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Cycloheximide
Chemical Name:4-[2-(3,5-Dimethyl-2-oxo-cyclohexyl)-2-hydroxyethyl]-2,
6-piperidinedione
Biological Activity:
Selective inhibitor of eukaryotic
(over prokaryotic) protein synthesis, blocking tRNA binding and release from
ribosomes. Induces apoptosis in a variety of transformed and normal cell lines,
including T-cells. Competitively inhibits the PPIase hFKBP12 (Ki =
3.4 μM). Antifungal antibiotic.
Obrig et al (1971) The mechanism by which cycloheximide and
related glutarimide antibiotics inhibit peptide synthesis on reticulocyte
ribosomes. J.Biol.Chem. 246 174. Tanget al (1999)
Cycloheximide-induced T-cell death is mediated by a Fas-associated death
domain-dependent mechanism. J.Biol.Chem. 274 7245. Christneret al (1999) Synthesis and cytotoxic evaluation of cycloheximide
derivatives as potential inhibitors of FKBP12 with neuroregenerative
properties. J.Med.Chem. 42 3615.
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