Antiestrogenic activity

Navas JM, Segner H. 1998. Antiestrogenic activity of anthropogenic and natural chemicals. Environ Sci Pollut Res 5(2) 75-82. 

McDonnell DP, Clemm DL, Imhof MO (1994) RU486 exerts antiestrogenic activities through a novel progesterone receptor A form-mediated mechanism. J Biol Chem 269 11945... 

Dick GM, Hunter AC, Sanders KM (2002) Ethylbromide tamoxifen, a membrane-impermeant antiestrogen, activates smooth muscle calcium-activated large-conductance potassium channels from the extracellular side. Mol Pharmacol 61 (5) 1105—1113... 

The main compounds that have demonstrated a pure antiestrogenic activity in the laboratory are the following (Fig. 6.1) ... 

Other compounds, such as ZK-703 and ZK-253, are currently under preclinical testing, and preliminary data show a pure antiestrogen activity in xenograft breast cancer models (Hoffmann et al. 2004). 

Finally, it has been suggested that fulvestrant, in addition to its antiestrogenic activity, has also significant antiprogestin activity, comparable to the activity of the antiprogestin RU-486 (Nawaz et al. 1999). 

McKim JM, Wilga PC, Breslin WJ, Plotzke KP, Gallavan RH, Meeks RG (2001) Potential estrogenic and antiestrogenic activity of the cyclic siloxane octamethylcyclotetrasiloxane (D4) and the linear siloxane hexamethyldisiloxane (HMDS) in immature rats using the uterotrophic assay. Toxicol Sci 63 37-46... 

Okubo T, Suzuki T, Yokoyama Y, Kano K, Kano I (2003) Estimation of estrogenic and antiestrogenic activities of some phthalate diesters and monoesters by MCF-7 cell proliferation assay in vitro. Biol Pharm Bull 26 1219-1224... 

Lubrano, et al. Evidence that Serenoa repens extract displays an antiestrogenic activity in prostatic tissue of benign prostatic hypertrophy patients. Eur Urol... 

Flammia, et al. Antiestrogenic activity of Serenoa repens in patients with BPH. Acta Urol Ital 1992 1992(4) 271-272. 

The estrogenic and antiestrogenic activities of several PBDE congeners and three hydroxylated PBDEs were tested in vitro using human breast cell line assays based on estrogen receptor (ER)-dependent luciferase reporter gene expression (Mccrts et al. 2001). The hydroxylated PBDEs,... 

Polybrominated Biphenyls. PBBs have the potential to interact with the endocrine system based on effects that mainly include changes in levels of thyroid and female reproductive hormones. No studies were located that investigated the estrogenic and antiestrogenic activity of PBBs in vitro or in vivo at the level of the estrogen receptor. 

The antiestrogenic activity of 47a motivated structural studies of gem-dichloro compounds 479. The orientations of the m-diaryl rings in 47 and in the well-known... 

Chlorotrianisene does not bind in vitro to the uterine estrogen receptor but has potent estrogenic and antiestrogenic actions in vivo, suggesting that it is a prodrug. Its antiestrogenic activity has been proposed to be due to a reactive intermediate (1). 

Idoxifene is another of the newer selective estrogen receptor modulators (SERMs), and preclinical data show that it has greater antiestrogenic activity than tamoxifen but lower estrogenic activity. It is not yet clear whether this affects its degree of usefulness or safety when it is used, for example, in cases of metastatic breast cancer. In comparisons of the two drugs in such patients the desired effects were similar and the incidence of adverse effects was essentially the same (14). 

Oh SM, Chung KH. 2006. Antiestrogenic activities of Ginkgo biloba extracts. J Steroid Biochem Mol Biol 100 167-176. 

Lu R, Serrero G. 1999. Resveratrol, a natural product derived from grape, exhibits antiestrogenic activity and inhibits the growth of human breast cancer cells. J. Cell Physiol 179 297-304. 

Gupta, M., McDougal, A., and Safe, S. 1998. Estrogenic and antiestrogenic activities of 16a- and 2-hydroxy metabolites of 17b-estradiol in MCF-7 and T47D human breast cancer cells. J. Steroid. Biochem. Mol. Biol. 67, 413 419. 

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