Estrone Sulfatase:  Probing Structural Requirements for Substrate and Inhibitor Recognition

Anderson, Cynthia M.; Freeman, Jennifer L.; Lucas, Linda H.; Farley, Michael; Dalhoumi, Habib; Widlanski, Theodore S.

doi:10.1021/bi9750089

Cited by 4 publications

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“…They also showed inhibition of the phosphatase as well as the sulfatase activities of alkaline phosphatase by inorganic phosphate (64). Anderson et al reported on steroidal and nonsteroidal phosphates that inhibited steroid sulfatase ac-tivity (43). We demonstrated inhibition of the iodothyronine sulfatase activities by inorganic phosphate and citrate.…”

Section: Discussionsupporting

confidence: 60%

“…Recently, much research has been performed to develop inhibitors of steroid sulfatase (ARSC) because of their potential for the treatment of estrogen-dependent breast cancers (43)(44)(45)(46)(47)(48)(49)(50)(51)(52)(53)(54). These studies have revealed some important structure-activity relations for compounds binding to the active site of ARSC.…”

Section: Discussionmentioning

confidence: 99%

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Characterization of Iodothyronine Sulfatase Activities in Human and Rat Liver and Placenta

et al. 2002

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In conditions associated with high serum iodothyronine sulfate concentrations, e.g. during fetal development, desulfation of these conjugates may be important in the regulation of thyroid hormone homeostasis. However, little is known about which sulfatases are involved in this process. Therefore, we investigated the hydrolysis of iodothyronine sulfates by homogenates of V79 cells expressing the human arylsulfatases A (ARSA), B (ARSB), or C (ARSC; steroid sulfatase), as well as tissue fractions of human and rat liver and placenta. We found that only the microsomal fraction from liver and placenta hydrolyzed iodothyronine sulfates. Among the recombinant enzymes only the endoplasmic reticulum-associated ARSC showed activity toward iodothyronine sulfates; the soluble lysosomal ARSA and ARSB were inactive. Recombinant ARSC as well as human placenta microsomes hydrolyzed iodothyronine sulfates with a substrate preference for 3,3'-diiodothyronine sulfate (3,3'-T(2)S) approximately T(3) sulfate (T(3)S) >> rT(3)S approximately T(4)S, whereas human and rat liver microsomes showed a preference for 3,3'-T(2)S > T(3)S >> rT(3)S approximately T(4)S. ARSC and the tissue microsomal sulfatases were all characterized by high apparent K(m) values (>50 microM) for 3,3'-T(2)S and T(3)S. Iodothyronine sulfatase activity determined using 3,3'-T(2)S as a substrate was much higher in human liver microsomes than in human placenta microsomes, although ARSC is expressed at higher levels in human placenta than in human liver. The ratio of estrone sulfate to T(2)S hydrolysis in human liver microsomes (0.2) differed largely from that in ARSC homogenate (80) and human placenta microsomes (150). These results suggest that ARSC accounts for the relatively low iodothyronine sulfatase activity of human placenta, and that additional arylsulfatase(s) contributes to the high iodothyronine sulfatase activity in human liver. Further research is needed to identify these iodothyronine sulfatases, and to study the physiological importance of the reversible sulfation of iodothyronines in thyroid hormone metabolism.

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Section: Discussionsupporting

confidence: 60%

Section: Discussionmentioning

confidence: 99%

Characterization of Iodothyronine Sulfatase Activities in Human and Rat Liver and Placenta

et al. 2002

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“…These findings are in line with previously reported results for c‐kit in aggressive fibromatosis 19 . However, some authors have reported EGFR expression in some cases of fibromatosis even though the EGFR expression level was rather low and cases of palmar fibromatosis were investigated 20 …”

Section: Discussionmentioning

confidence: 99%

Expression of β‐catenin and p53 are prognostic factors in deep aggressive fibromatosis

et al. 2007

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Hexanones

Martin¹,

Buisson²

2015

Aromatic Hydroxyketones: Preparation &Amp; Physical Properties

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Estrone Sulfatase: Probing Structural Requirements for Substrate and Inhibitor Recognition

Abstract: Lineweaver-Burk plots, secondary replots, and 31 P NMRbased titration curves (34 pages). Ordering information is given on any current masthead page.

Cited by 4 publications

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Characterization of Iodothyronine Sulfatase Activities in Human and Rat Liver and Placenta

Characterization of Iodothyronine Sulfatase Activities in Human and Rat Liver and Placenta

Expression of β‐catenin and p53 are prognostic factors in deep aggressive fibromatosis

Hexanones

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