Pub. Date : 2013 Jul
PMID : 23567241
5 Functional Relationships(s)Download |
Sentence | Compound Name | Protein Name | Organism |
| 1 | The structure-activity relationships of parabens which are widely used as preservatives for transcriptional activities mediated by human estrogen receptor alpha (hERalpha), hERbeta and androgen receptor (hAR) were investigated. | Parabens | estrogen receptor 2 | Homo sapiens |
| 2 | Fourteen of 17 parabens exhibited hERalpha and/or hERbeta agonistic activity at concentrations of <= 1 x 10(-5)M, whereas none of the 17 parabens showed AR agonistic or antagonistic activity. | Parabens | estrogen receptor 2 | Homo sapiens |
| 3 | Among 12 parabens with linear alkyl chains ranging in length from C1 to C12, heptylparaben (C7) and pentylparaben (C5) showed the most potent ERalpha and ERbeta agonistic activity in the order of 10(-7)M and 10(-8)M, respectively, and the activities decreased in a stepwise manner as the alkyl chain was shortened to C1 or lengthened to C12. | Parabens | estrogen receptor 2 | Homo sapiens |
| 4 | Most parabens showing estrogenic activity exhibited ERbeta-agonistic activity at lower concentrations than those inducing ERalpha-agonistic activity. | Parabens | estrogen receptor 2 | Homo sapiens |
| 5 | These results indicate that parabens are selective agonists for ERbeta over ERalpha; their interactions with ERalpha/beta are dependent on the size and bulkiness of the alkyl groups; and they are metabolized by carboxylesterases, leading to attenuation of their estrogenic activity. | Parabens | estrogen receptor 2 | Homo sapiens |