The anti-oestrogen drug tamoxifen is an elongation inhibitor of eukaryotic protein biosynthesis.
The drug tamoxifen is widely used in the chemotherapy of breast cancer but its action is not explained completely by its anti-oestrogen properties. We now present evidence indicating that it is also a potent inhibitor of eukaryotic protein synthesis as demonstrated in Xenopus oocytes, intact reticulocytes and reticulocyte lysates. The inhibition affects general protein synthesis, is transient in oocytes and not reversed by oestrogen. The drug appears to act by inhibiting polypeptide chain elongation. This action of tamoxifen is independent of oestrogen receptors and may explain its therapeutic effectiveness in oestrogen-independent tumours.
D000818:Animals; D004305:Dose-Response Relationship, Drug; D009865:Oocytes / Q000378:metabolism; D010441:Peptide Chain Elongation, Translational / Q000187:drug effects*; D011132:Polyribosomes / Q000187:drug effects; D014176:Protein Biosynthesis; D011817:Rabbits; D012156:Reticulocytes / Q000378:metabolism; D013629:Tamoxifen / Q000494:pharmacology*
D013629:Tamoxifen