Inhibition of steroid sulphatase activity in endometriotic implants by 667 COUMATE: a potential new therapy

A Purohit, Luca Fusi, L Fusi, J Brosens, Jan J. Brosens, L. W. Lawrence Woo, L W L Woo, B V L Potter, M J Reed, Michael Reed
Human Reproduction · 2007 · vol. 23(2) , pp. 290–297 · doi:10.1093/humrep/dem308 · PMID:18056119 · W2163359570
article OA: bronze CC0 ⤵ 28 in-corpus citations
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This study found high steroid sulphatase (STS) activity in endometriotic implants that correlates with disease severity, and demonstrated that the inhibitor 667 COUMATE effectively blocks this activity.

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Abstract

BACKGROUND: Local biosynthesis of estrogens is thought to be important for the maintenance and growth of endometriotic implants. In addition to the formation of estrogen via the aromatase pathway, steroid sulphatase (STS), which is responsible for the hydrolysis of estrogen sulphates, may be an important source of estrogens in endometriosis. METHODS: Eutopic and ectopic endometrial samples from 14 women with minimal or mild (MM) endometriosis and from 13 women with moderate to severe (MS) endometriosis were analysed for aromatase and STS activities. RESULTS: Aromatase and STS activity were detected in all samples. STS enzyme activity in both eutopic and ectopic endometrium was considerably higher and less variable than aromatase activity. Moreover, STS, but not aromatase, activity in endometriotic implants correlated with the severity of the disease (mean +/- SEM: 203 +/- 38 nmol/4 h/g wet weight tissue in MM disease versus 423 +/- 44 nmol/4 h/g wet weight tissue in MS endometriosis, P 99%) in both eutopic and ectopic tissues. CONCLUSIONS: The high levels of STS activity detected in ectopic endometrium and the correlation with severity of disease suggest that STS inhibitors could be useful for the treatment of endometriosis.

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Condition tags

mesh:D004715endometriosis

MeSH descriptors

Coumarins Endometriosis Enzyme Inhibitors Steryl-Sulfatase Sulfonamides Adult Aromatase Aromatase Coumarins Endometriosis Endometriosis Endometrium Endometrium Enzyme Inhibitors Female Humans In Vitro Techniques Middle Aged Severity of Illness Index Steryl-Sulfatase

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Papers in the corpus that this work cites (lower rings, blue) and that cite this one (upper rings, green). Dot size scales with the paper's in-corpus citation count — bigger dot = more influential within the endo/adeno field. Click a dot to open that paper. [ expand to 2 hops ] — adds papers reached through this work's immediate citers/citees. Heavier; up to 60 extra dots.

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Cited by (28)

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