| pubmed-article:11557270 | rdf:type | pubmed:Citation | lld:pubmed |
| pubmed-article:11557270 | lifeskim:mentions | umls-concept:C0031809 | lld:lifeskim |
| pubmed-article:11557270 | lifeskim:mentions | umls-concept:C0033306 | lld:lifeskim |
| pubmed-article:11557270 | lifeskim:mentions | umls-concept:C0023566 | lld:lifeskim |
| pubmed-article:11557270 | lifeskim:mentions | umls-concept:C0441655 | lld:lifeskim |
| pubmed-article:11557270 | lifeskim:mentions | umls-concept:C2364326 | lld:lifeskim |
| pubmed-article:11557270 | lifeskim:mentions | umls-concept:C0870883 | lld:lifeskim |
| pubmed-article:11557270 | pubmed:issue | 2 | lld:pubmed |
| pubmed-article:11557270 | pubmed:dateCreated | 2001-9-14 | lld:pubmed |
| pubmed-article:11557270 | pubmed:abstractText | Levonorgestrel (13beta-ethyl-17alpha-ethynyl-17beta-hydroxy-4-gonen-3-one), a potent contraceptive progestin stimulates growth and proliferation of cultured breast cancer cells through a receptor-mediated mechanism, even though levonorgestrel does not bind to the oestrogen receptor (ER). To assess whether the oestrogen-like effects induced by this synthetic progestin are exerted via its metabolic conversion products, we studied the binding affinity of three A-ring levonorgestrel derivatives to the ER and their capability to transactivate an oestrogen-dependent yeast system co-transfected with the human ER gene and oestrogen responsive elements fused to a beta-galactosidase reporter vector. The results demonstrated that the 3beta,5alpha reduced levonorgestrel derivative and to a lesser extent its 3alpha isomer interact with the oestrogen receptor, with a significantly lower relative binding affinity (2.4% and 0.4%, respectively) than that of oestradiol (100%), while levonorgestrel does not. Both levonorgestrel metabolites were able to activate, in a dose-dependent manner, the beta-galactosidase reporter gene in the yeast expression system, an effect that was precluded by a steroidal antioestrogen. The oestrogenic potency of levonorgestrel metabolites was significantly lower (750-fold) than that of oestradiol. Furthermore, high doses of 3beta,5alpha levonorgestrel (2.5 mg/day/6 days) induced an increase of oestrogen-dependent progestin receptor in the anterior pituitary of castrated rats. The overall data offer a plausible explanation for the weak oestrogenic effects induced by high, non-pharmacological doses of levonorgestrel. | lld:pubmed |
| pubmed-article:11557270 | pubmed:language | eng | lld:pubmed |
| pubmed-article:11557270 | pubmed:journal | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:11557270 | pubmed:citationSubset | IM | lld:pubmed |
| pubmed-article:11557270 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:11557270 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:11557270 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:11557270 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:11557270 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:11557270 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:11557270 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:11557270 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:11557270 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:11557270 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:11557270 | pubmed:status | MEDLINE | lld:pubmed |
| pubmed-article:11557270 | pubmed:month | Sep | lld:pubmed |
| pubmed-article:11557270 | pubmed:issn | 0014-2999 | lld:pubmed |
| pubmed-article:11557270 | pubmed:author | pubmed-author:Pérez-Palacio... | lld:pubmed |
| pubmed-article:11557270 | pubmed:author | pubmed-author:ReyesMM | lld:pubmed |
| pubmed-article:11557270 | pubmed:author | pubmed-author:Damián-Matsum... | lld:pubmed |
| pubmed-article:11557270 | pubmed:author | pubmed-author:LemusA EAE | lld:pubmed |
| pubmed-article:11557270 | pubmed:author | pubmed-author:GarcíaG AGA | lld:pubmed |
| pubmed-article:11557270 | pubmed:author | pubmed-author:GrillascaII | lld:pubmed |
| pubmed-article:11557270 | pubmed:author | pubmed-author:SantillánRR | lld:pubmed |
| pubmed-article:11557270 | pubmed:issnType | Print | lld:pubmed |
| pubmed-article:11557270 | pubmed:day | 14 | lld:pubmed |
| pubmed-article:11557270 | pubmed:volume | 427 | lld:pubmed |
| pubmed-article:11557270 | pubmed:owner | NLM | lld:pubmed |
| pubmed-article:11557270 | pubmed:authorsComplete | Y | lld:pubmed |
| pubmed-article:11557270 | pubmed:pagination | 167-74 | lld:pubmed |
| pubmed-article:11557270 | pubmed:dateRevised | 2006-11-15 | lld:pubmed |
| pubmed-article:11557270 | pubmed:meshHeading | pubmed-meshheading:11557270... | lld:pubmed |
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| pubmed-article:11557270 | pubmed:meshHeading | pubmed-meshheading:11557270... | lld:pubmed |
| pubmed-article:11557270 | pubmed:meshHeading | pubmed-meshheading:11557270... | lld:pubmed |
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| pubmed-article:11557270 | pubmed:meshHeading | pubmed-meshheading:11557270... | lld:pubmed |
| pubmed-article:11557270 | pubmed:year | 2001 | lld:pubmed |
| pubmed-article:11557270 | pubmed:articleTitle | Assessment of the oestrogenic activity of the contraceptive progestin levonorgestrel and its non-phenolic metabolites. | lld:pubmed |
| pubmed-article:11557270 | pubmed:affiliation | Department of Reproductive Biology, National Institute of Medical Sciences and Nutrition S. Zubirán, Vasco de Quiroga 15, Mexico City, C.P. 14000, Mexico. | lld:pubmed |
| pubmed-article:11557270 | pubmed:publicationType | Journal Article | lld:pubmed |
| pubmed-article:11557270 | pubmed:publicationType | Research Support, Non-U.S. Gov't | lld:pubmed |
