Expression of the Steroid and Xenobiotic Receptor and Its Possible Target Gene, Organic Anion Transporting Polypeptide-A, in Human Breast Carcinoma

Miki, Yasuhiro; Suzuki, Takashi; Kitada, Koji; Yabuki, Nami; Shibuya, Rie; Moriya, Takuya; Ishida, Toru; Ohuchi, Noriaki; Blumberg, Bruce; Sasano, Hironobu

doi:10.1158/0008-5472.can-05-1070

Cited by 127 publications

(165 citation statements)

References 43 publications

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“…The expression of OATP1A2 messenger RNA (mRNA) and protein in breast cancer was first reported by Miki et al (61). The results from reverse transcriptase-polymerase chain reaction (RT-PCR) analyses indicated that OATP1A2 is expressed in human breast cancer tissues, but not in noncancerous breast tissues, adipose tissues, or stromal cells (61).…”

Section: Oatp1a2 (Gene Symbol Slco1a2)mentioning

confidence: 99%

“…Given that OATP1A2 can mediate the transport of endogenous hormonal substrates and several anticancer drugs (Table I), several investigations have examined the expression and functional impact of OATP1A2 in cancer. OATP1A2 expression was first reported in breast cancer and subsequently in additional types of cancer including colon, prostate, and bone (Table II) (6,(61)(62)(63)65). To date, the potential functional significance of OATP1A2 has been reported in breast cancer, but not in other types of cancer.…”

Section: Oatp1a2 (Gene Symbol Slco1a2)mentioning

confidence: 99%

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Role of Organic Anion-Transporting Polypeptides (OATPs) in Cancer Therapy

Thakkar

Lockhart

Lee

2015

AAPS J

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Abstract. The superfamily of organic anion-transporting polypeptides (OATPs, gene symbol SLCO) includes important transporters handling a variety of endogenous and xenobiotic substrates. Currently, 11 human OATPs are known and their substrates include endogenous hormones and their conjugates, anticancer drugs, and imaging agents. The contribution of OATPs to the in vivo disposition of these substrates has been extensively investigated. An accumulating body of evidence also indicates that the expression of some OATPs may be up-or downregulated in several types of cancers, suggesting potential pathogenic roles during the development and progression of cancer. Given that the role of OATPs in handling cancer therapeutics has been already covered by several excellent reviews, this review will focus on the recent progresses on the topic, in particular the role of OATPs in the disposition of anticancer drugs, the impact of OATP genetic variations on the function of OATPs, and the OATPs differentially expressed in cancer and their potential roles in cancer development, progression, and treatment.

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Section: Oatp1a2 (Gene Symbol Slco1a2)mentioning

confidence: 99%

Section: Oatp1a2 (Gene Symbol Slco1a2)mentioning

confidence: 99%

Role of Organic Anion-Transporting Polypeptides (OATPs) in Cancer Therapy

Thakkar

Lockhart

Lee

2015

AAPS J

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“…It is known that E 1 -3-sulfate is an important estrogen conjugate that has a relatively long half-life in circulation. This estrogen conjugate can be readily taken up by estrogen target cells via an active transport mechanism [62,63], and the subsequent hydrolysis mediated by sulfatases to release the hormonally-active parent hormone E 1 represents an important pathway for the biosynthesis of active estrogens in the body. Therefore, it is suggested that a marked decrease of hepatic sulfatase activity may subsequently reduce the body's overall estrogenic exposure and stimulation.…”

Section: Effect Of Tcdd and Hf Diet On Hepatic Estrogen Metabolismmentioning

confidence: 99%

Effect of 2,3,7,8-tetrachlorodibenzo-p-dioxin administration and high-fat diet on the body weight and hepatic estrogen metabolism in female C3H/HeN mice

Zhu

Gallo

Burger

et al. 2008

Toxicology and Applied Pharmacology

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We studied the effect of administration of 2,3,7,8-tetrachlorodibenzo-p-dioxin (TCDD) by i.p. injection once every two weeks in combination with a high-fat (HF) diet for 8 or 16 weeks on the body and organ weight changes as well as on the hepatic enzyme activity for estrogen metabolism in C3H/HeN female mice. Administration of TCDD at 100 μg/kg b.w. once every two weeks for 8 weeks increased the body weight by 46% in the HF diet-fed animals, but not in the regular diet-fed animals. This is the first observation suggesting that TCDD, a potent Ah receptor agonist, may have an obesity-inducing effect in animals fed a HF diet. While TCDD increased liver weight and decreased thymus weight in animals, these effects were enhanced by feeding animals a HF diet. Metabolism studies showed that TCDD administration for 8 or 16 weeks increased the liver microsomal activity for the 2-and 4-hydroxylation of 17β-estradiol in animals fed a control diet, but surprisingly not in animals fed a HF diet. Treatment with TCDD dose-dependently increased the hepatic activity for the O-methylation of catechol estrogens in both control and HF diet-fed animals, and it also decreased the levels of liver microsomal sulfatase activity for hydrolysis of estrone-3-sulfate. TCDD did not significantly affect the hepatic enzyme activity for the glucuronidation or esterification of endogenous estrogens. It is suggested that enhanced metabolic inactivation of 1 This study was supported, in part, by a grant from the American Cancer Society (RSG-02-143-01-CNE to BTZ) and also by grants from the NIH (CA92391, CA97109 and ES05022). Publisher's Disclaimer: This is a PDF file of an unedited manuscript that has been accepted for publication. As a service to our customers we are providing this early version of the manuscript. The manuscript will undergo copyediting, typesetting, and review of the resulting proof before it is published in its final citable form. Please note that during the production process errors may be discovered which could affect the content, and all legal disclaimers that apply to the journal pertain. endogenous estrogens by hepatic estrogen-metabolizing enzymes in TCDD-treated, control diet-fed animals contributes importantly to the reduced incidence of estrogen-associated tumors in animals treated with TCDD. NIH Public Access

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“…Instead, they would usually only activate those target tissues or cells most in need of estrogenic stimulation. Here, it is also worth noting that several recent studies have shown that estrogen target cells can actively transport E1-3-sulfate into the cells (38,39). Moreover, these cells may selectively adjust their ability to actively transport E1-3-sulfate into the cells to release biologically active estrogens depending on their hormonal needs.…”

Section: Which Estrogens Are Ideal For Postmenopausal Hormone Replacementioning

confidence: 92%

Is it necessary to control the level of estrogen receptor α and β activation in postmenopausal hormone replacement therapy in order to achieve the optimal outcome? (Review)

Zhu

2008

Mol Med Report

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Abstract. Endogenous estrogens exert an array of biological actions on women, many of which are mediated by the estrogen receptors (ERs) α and ß. Results from our recent studies suggest that the human ERα and ERß systems are differentially activated under different physiological conditions. In non-pregnant young women, the ERα system is preferentially activated over the ERß system, mainly by estrone (E1) and its major oxidative metabolite, 2-hydroxy-E1. These two estrogens are among the quantitatively major estrogens present in young women, and have approximately 4-fold preferential activity for ERα over ERß. During pregnancy, however, there is a preponderance of activation of ERß over ERα conferred by various pregnancy estrogens such as estriol and other D-ring derivatives of 17ß-estradiol (E2). These estrogens have an up to 18-fold preference for binding to ERß than for ERα, and some of them are produced in unusually large quantities. Given this new information, it is hypothesized that the estrogens ideal for female hormone replacement therapy (HRT) would be those which produce a hormonal condition mirroring that found in non-pregnant young women rather than in pregnant women. Endogenous estrogen derivatives, such as the sulfated conjugates of E1, may be among the ideal candidates for achieving this clinical purpose. In comparison, Premarin, the most commonly-used HRT containing a mixture of conjugated estrogens isolated from pregnant mare's urine, is less suitable because several of its estrogenic components can produce a strong preferential overstimulation of the human ERß signaling system. Contents 1. Introduction 2. Differences in the composition and quantity of endogenous estrogens produced in pregnant and non-pregnant women 3. Differences in the biological activity of pregnancy and non-pregnancy estrogens 4. Biological activity of estrogens contained in Premarin 5. Which estrogens are ideal for postmenopausal hormone replacement therapy? 6. Concluding remarks IntroductionFemale hormone replacement therapy (HRT), also commonly called menopausal hormone therapy, is a hormonal treatment for peri-or post-menopausal women undertaken to reduce the discomfort and health problems associated with diminished circulating ovarian hormones (namely, estrogens and progesterone). HRT usually provides a low dose of an estrogen (or a mixture of estrogens), often in combination with a progestin. In the past few decades, the most commonly-used estrogen treatment for HRT has been Premarin, which consists of a mixture of mostly sulfated estrogens isolated from pregnant mare's urine. The hormonal activity of these conjugated estrogens in vivo results from their enzymatic hydrolysis and releases biologically active estrogens.Until a few years ago, the generally-held scientific belief was that 'an estrogen is an estrogen', i.e., that all estrogens exert similar pharmacological actions on the body. However, this dogmatic view has gradually changed over the past decade due, in large part, to the emergence of the following body of ...

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Expression of the Steroid and Xenobiotic Receptor and Its Possible Target Gene, Organic Anion Transporting Polypeptide-A, in Human Breast Carcinoma

Abstract: Steroid and xenobiotic receptor (SXR) or human pregnane X receptor (hPXR) has been shown to play an important role in

Cited by 127 publications

References 43 publications

Role of Organic Anion-Transporting Polypeptides (OATPs) in Cancer Therapy

Role of Organic Anion-Transporting Polypeptides (OATPs) in Cancer Therapy

Effect of 2,3,7,8-tetrachlorodibenzo-p-dioxin administration and high-fat diet on the body weight and hepatic estrogen metabolism in female C3H/HeN mice

Is it necessary to control the level of estrogen receptor α and β activation in postmenopausal hormone replacement therapy in order to achieve the optimal outcome? (Review)

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