Aromatase inhibition by 15-deoxy-prostaglandin J2 (15-dPGJ2) and N-(4-hydroxyphenyl)-retinamide (4HPR) is associated with enhanced ceramide production

Andrews, W. J.; Winnett, Georgia; Rehman, Farah L.; Shanmugasundaram, Pradeep; Hagen, Daphne van; Schrey, M.P.

doi:10.1016/j.jsbmb.2005.01.014

Cited by 15 publications

(14 citation statements)

References 24 publications

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“…Proteasome-dependent degradation of cyclin D1 and estrogen receptor a (ERa) in a breast cancer cell line induced by PPARg agonists also has been reported (49). In addition, the activation of PPARg and/or RXR has been shown to inhibit aromatase transcription in vitro (50)(51)(52)(53)(54). Moreover, the activation of PPARg and/or RXR has been shown to inhibit COX-2 expression (55) and reduce inflammation (56,57).…”

Section: Discussionmentioning

confidence: 99%

Peroxisome proliferator-activated receptor-gamma and retinoid X receptor agonists synergistically suppress proliferation of immortalized endometrial stromal cells

Wu¹,

Guo

2009

Fertility and Sterility

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Section: Discussionmentioning

confidence: 99%

Peroxisome proliferator-activated receptor-gamma and retinoid X receptor agonists synergistically suppress proliferation of immortalized endometrial stromal cells

Wu¹,

Guo

2009

Fertility and Sterility

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“…We [31] and others [32,33] previously demonstrated that the synthetic retinoid 4-hydroxyphenylretinamide (4-HPR) inhibits the activity of aromatase in vitro. However, despite the established chemopreventive effect of retinoids towards breast cancer, and the crucial role of aromatase in the growth of estrogen-dependent tumors, the effects of ROH and other naturally occurring retinoids on aromatase activity have not, to the best of our knowledge, been investigated.…”

Section: Discussionmentioning

confidence: 99%

“…The model systems used in this study, JEG-3 human placental cells used as a source of microsomal aromatase and the estrogen-receptorpositive MCF-7 human mammary cancer cell line, have been used extensively in aromatase research [30][31][32][33]37,38] and thus are appropriate in vitro models. Plasma concentrations of ROH reach 2-3 μM in humans [2,39].…”

Section: Discussionmentioning

confidence: 99%

Retinol inhibits aromatase activity and expression in vitro

Ciolino¹,

Nair²

2011

The Journal of Nutritional Biochemistry

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“…It inhibits mitochondrial electron flow, modulating operation of Coenzyme Q activity (ubiquinone, a double allylic ketone). It also inhibits aromatase [Andrews et al, 2005], the enzyme that converts androgens to estrogens and thereby stimulates the conversion of Cer to glucosylCer (an antiapoptotic sphingolipid) [Shukla et al, 1992].…”

Section: Introductionmentioning

confidence: 99%

Drug design: hiding in full view

Radin

2008

Drug Development Research

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Compounds that can produce potent biological effects in cells encompass a variety of structural motifs. Many of these compounds share a structural feature that has rarely been noted. It is an allylic cluster of atoms, a 3-carbon chain with a double bond between two of the atoms and an oxygen atom at the other end. The oxygen can be in a hydroxyl group, or in an ether or ketal or ester linkage, or simply a carbonyl form. In the latter case, the linkage is an allylic ketone (ene-one) structure. Nitrogen is often seen in equivalent forms. Inclusion of at least one allylic moiety appears to be able to turn a modestly active or inert compound into an effective drug or toxin. Some compounds lack the allylic moiety but develop one by enzymatic action, usually via cytochrome P-450 enzymes. These metabolites probably represent the active drug forms. The above concepts seem to be radically simplistic and improbable, but the evidence supporting them and the explanations for the biological activities are hidden ''in plain view.'' Comparisons with the pleiotropic activities of the allylic sphingolipid, ceramide, indicate that many allylic drugs operate by controlling the state of protein phosphorylation, by activating proteases, by generating reactive oxygen species, by slowing mitochondrial electron transport, or by lowering cellular glutathione concentrations. Drug Dev Res 69: [15][16][17][18][19][20][21][22][23][24][25] 2008 r2008 Wiley-Liss, Inc.

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Aromatase inhibition by 15-deoxy-prostaglandin J2 (15-dPGJ2) and N-(4-hydroxyphenyl)-retinamide (4HPR) is associated with enhanced ceramide production

Cited by 15 publications

References 24 publications

Peroxisome proliferator-activated receptor-gamma and retinoid X receptor agonists synergistically suppress proliferation of immortalized endometrial stromal cells

Peroxisome proliferator-activated receptor-gamma and retinoid X receptor agonists synergistically suppress proliferation of immortalized endometrial stromal cells

Retinol inhibits aromatase activity and expression in vitro

Drug design: hiding in full view

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