Binding characteristics of aromatase inhibitors and phytoestrogens to human aromatase

Passiflora: a review update

“…Since, benzoflavone moieties are the strongest inhibitors (Aldrich Catalog, 1996) of the enzyme aromatase (a member of cytochrome P-450 family), they are very significant in the metabolism of sex-steroids (Kao et al, 1998;Kellis and Vickery, 1984). It is postulated that BZF inhibit the metabolic conversion of androgens (testosterone) to estrogens, thereby increaseing free teststerone and decreasing free estrogen (Chen et al, 1997). The free teststerone accounts for the non-appearence of withdrawal effects of substances like morphine, nicotine, cannabinoids, ethanol and even benzodiazepines.…”

1,2,4-Triazoles: Synthetic approaches and pharmacological importance. (Review)

“…In addition, it was reported that compounds having triazole moieties, such as vorozole 12, letrozole 13, and anastrozole 14, appeared to be very effective aromatase inhibitors, which in turn prevented breast cancer [40][41][42]. It is known that 1,2,4-triazole moieties interact strongly with heme iron, and aromatic substituents on the triazoles are very effective for interacting with the active site of aromatase [43]. Other laboratories reported the same biological activity of the triazole family [44][45][46].…”

Screening of herbal constituents for aromatase inhibitory activity

“…For each ligand, various initial poses were considered, but all in the vicinity of residues previously identified (on the basis of the model building studies) as lining the enzyme active site pocket [14]. These residues -many of which have also been demonstrated to be key determinants in ligand binding through site-directed mutagenesis experiments [18,[27][28][29][30] -include Glu 302, Thr 310, Ser 478 and His 480.…”