PMID: 3320566Jan 1, 1987Paper

Interactions of tamoxifen in the chicken

Journal of Steroid Biochemistry
C B Lazier

Abstract

The triphenylethylene antiestrogens are very potent antagonists of estrogen action in the chicken and manifest little agonist activity compared to their action in other species. The estrogen antagonism is most probably mediated by the estrogen receptor, to which tamoxifen binds with a Ki of 2.6 nM. Tamoxifen is readily metabolized by liver to 4-hydroxytamoxifen, which binds the liver nuclear estrogen receptor with a Ki of 0.1 nM. The Kd of the receptor is 0.7 nM. Estrogen receptor concentrations in liver from immature chickens are relatively low both in nuclear and cytosol fractions. Treatment with estradiol results in 10-fold up-regulation of the nuclear levels to give a total receptor concentration of about 2 pmol/g tissue. Tamoxifen can promote this up-regulation to a limited extent, but interpretation of experimental results is compromised by difficulties with exchange assays in the face of the very high binding affinity of 4-hydroxytamoxifen. Tamoxifen also binds with high affinity (Kd 2-4 nM) and distinctive specificity to antiestrogen binding sites (AEBS) present in a wide variety of chicken tissues and in the highest concentration in the liver (800 pmol/g tissue). Liver and serum contain ether-soluble components which c...Continue Reading

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Citations

Mar 15, 1995·Thrombosis Research·M E MillerG M Dores
Nov 6, 2003·Toxicology in Vitro : an International Journal Published in Association with BIBRA·C LuxoM T Silva
Oct 1, 1996·Toxicology in Vitro : an International Journal Published in Association with BIBRA·J B CustódioV M Madeira
May 8, 2001·British Poultry Science·D E McKeeganM A Mitchell
Oct 16, 2004·Journal of Veterinary Medicine. A, Physiology, Pathology, Clinical Medicine·A SechmanJ Rzasa
May 22, 2009·Acta Veterinaria Hungarica·Janusz RzasaAnna Hrabia

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