PubMed Health⌕ Search
Home/Archive/PubMed

PubMed · 15892637

Non-steroidal subtype selective estrogens.

Gerrit H Veeneman
View original source ↗Export metadata ↓

Abstract

The biological effects of estrogens are thought to be mediated by two receptors referred to as ERalpha and ERbeta. In recent years significant efforts have been devoted to the design of subtype selective ligands. These ligands are valuable tools to establish the precise biological role of each of the subtypes and to develop new generations of therapeutics. The first part of this review briefly summarizes the biology behind the estrogen receptors. The second part addresses the structure-activity relationship of the subtype selective ER ligands that were reported up to now. In the third part, the current insights in the therapeutic prospects of the subtype selective estrogens will be discussed.

Explore related subjects

Estrogens, Non-SteroidalHumansLigandsReceptors, EstrogenJournal ArticleReview

Keep this discovery

Explore connections, maps & timelines

BibTeXRIS

Gerrit H Veeneman. 2005. Non-steroidal subtype selective estrogens.. https://doi.org/10.2174/0929867053764662

Cite the original work for its findings. Save a collection to share your selection of sources.

KEEP EXPLORING

Related citations

PubMed2004

Ring nitrogen-substituted non-steroidal estrogens: pyridine and pyrimidine analogs of the phenol in deoxyhexestrol experience resonance constraints on preferred ligand conformation.

To develop compounds selective for estrogen receptor beta (ERbeta), we substituted hydroxypyridine and pyrimidine heteroaryl groups for the characteristic phenol ring of non-steroidal estrogens. The unexpectedly low affinity showed by some of these compounds is ascribed, in part, to a resonance-enforced conformational constraint that prevents their optimal accommodation in the ER ligand binding pocket.

Estrogens, Non-Steroidal↗
PubMed2004

Preliminary results of monitoring research on zearalenone presence in blood of women with neoplastic lesions in reproductive system.

The aim of the monitoring of zearalenone presence in the blood plasma of women with neoplastic lesions in the reproductive tract was to asses whether the phytosteride is noted in the patients blood and whether the correlation exists between its presence and the incidence of particular neoplasm. The presence of zearalenone or its metabolite--alpha-zearalenole, was noted in 13.51% of the examined women. In 60% of the patients with the confirmed presence of the xenobiotic it was noted in the lowest concentrations. These patients had neoplastic lesions of Carcinoma corpus uteri type.

Estrogens, Non-Steroidal↗
PubMed2003

Occurrence and removal of estrogenic short-chain ethoxy nonylphenolic compounds and their halogenated derivatives during drinking water production.

The elimination of nonylphenol (NP), nonylphenol mono- and diethoxylates (NP1EO and NP2EO), nonylphenol carboxylates (NP1EC and NP2EC) and their brominated and chlorinated derivatives during drinking water treatment process in Sant Joan Despf waterworks in Barcelona was investigated utilizing a recently developed, highly sensitive LC-MS-MS method. The concentration of these potentially estrogenic compounds in raw water entering waterworks (taken from the Llobregat River, NE Spain) ranged from 8.3 to 22 microg/L, with NP2EC being the most abundant compound. Prechlorination reduced the concentration of short-chain ethoxy NPECs and NPEOs by about 25-35% and of NP by almost 90%. However, this reduction of concentrations was partially due to their transformation to halogenated derivatives. After prechlorination, halogenated nonylphenolic compounds represented approximately 13% of the total metabolite pool, of which 97% were in the form of brominated acidic metabolites. The efficiency of further treatment steps to eliminate nonylphenolic compounds (calculated for the sum of all short-chain ethoxy metabolites including halogenated derivatives) was as follows: settling and flocculation followed by rapid sand filtration (7%), ozonation (87%), GAC filtration (73%), and final disinfection with chlorine (43%), resulting in overall elimination ranging from 96 to 99% (mean 98% for four sampling dates). A few of the nonylphenolic compounds (NP, NP1EC, and NP2EC) were also identified in drinking water; however, the residues detected were generally below 100 ng/L, with one exception for NP2EC in November 2001 when a concentration of 215 ng/L was detected.

Estrogens, Non-Steroidal↗