1α,25-Dihydroxyvitamin D3 exerts tissue-specific effects on estrogen and androgen metabolism

Lundqvist, Johan; Norlin, Maria; Wikvall, Kjell

doi:10.1016/j.bbalip.2011.01.004

Cited by 44 publications

(30 citation statements)

References 36 publications

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“…Numerous studies have also used cultured mammalian cells to examine the biological responses of breast cell lines to exogenous 1,25D. Data collected to date examining the effects of vitamin D on malignant and non-malignant cell lines in vitro have shown vitamin D to induce cell cycle arrest at the G 0 /G 1 stage, apoptosis, inhibition of aromatase expression and a number of other antitumourigenic cellular processes (Kemmis et al, 2006;Lundqvist et al, 2011;Nagpal et al, 2005), reviewed by (Welsh, 2011).…”

Section: Introductionmentioning

confidence: 98%

A comparison of vitamin D activity in paired non-malignant and malignant human breast tissues

Suetani¹,

Ho²,

Jindal³

et al. 2012

Molecular and Cellular Endocrinology

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Section: Introductionmentioning

confidence: 98%

A comparison of vitamin D activity in paired non-malignant and malignant human breast tissues

Suetani¹,

Ho²,

Jindal³

et al. 2012

Molecular and Cellular Endocrinology

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“…Bar corresponds to 10 mm. Vitamin D and male reproduction breast and prostate but caused an opposite effect in adrenal cells (Lundqvist et al 2011).…”

Section: Vd Regulates Biosynthesis Of Estradiol and Testosteronementioning

confidence: 99%

“…Numerous studies investigated the putative physiological relationship between circulating levels of 25OHD 3 /1,25(OH) 2 D, the activity of VDR and VD metabolizing enzymes, and serum testosterone and estradiol levels in both animals and humans (Tanaka et al 1976, Hyldstrup et al 1984, Small et al 1984, Hochberg et al 1985, Krabbe et al 1986, Sonnenberg et al 1986, Hagenfeldt et al 1992, Morley et al 1993, Inpanbutr et al 1996, Otremski et al 1997, Rapado et al 1999, Kinuta et al 2000, van Abel et al 2002, Braga et al 2002, Van Cromphaut et al 2003, Echchgadda et al 2004, Valimaki et al 2004, Kastelan et al 2009, Fleet & Schoch 2010, Krishnan et al 2010a, 2010b, Meng et al 2010, Pilz et al 2011, Ramlau-Hansen et al 2010, Wehr et al 2010, Ceglia et al 2011, Foresta et al 2011, Lundqvist et al 2011, Lee et al 2012. It has been shown that estrogen promotes the two-step activation of cholecalciferol to 1,25(OH) 2 D 3 and reinforces a positive effect on calcium homeostasis through a direct stimulatory effect on intestinal calcium absorption.…”

Section: Vd Regulates Biosynthesis Of Estradiol and Testosteronementioning

confidence: 99%

Vitamin D metabolism, sex hormones, and male reproductive function

Jensen¹

2012

Reproduction

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The spectrum of vitamin D (VD)-mediated effects has expanded in recent years, and VD is now recognized as a versatile signaling molecule rather than being solely a regulator of bone health and calcium homeostasis. One of the recently identified target areas of VD is male reproductive function. The VD receptor (VDR) and the VD metabolizing enzyme expression studies documented the presence of this system in the testes, mature spermatozoa, and ejaculatory tract, suggesting that both systemic and local VD metabolism may influence male reproductive function. However, it is still debated which cell is the main VD target in the testis and to what extent VD is important for sex hormone production and function of spermatozoa. This review summarizes descriptive studies on testicular VD metabolism and spatial distribution of VDR and the VD metabolizing enzymes in the mammalian testes and discusses mechanistic and association studies conducted in animals and humans. The reviewed evidence suggests some effects of VD on estrogen and testosterone biosynthesis and implicates involvement of both systemic and local VD metabolism in the regulation of male fertility potential.

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“…In respect to cancer, TEI9647 reversed the down-regulation of CYP21A2 in the presence of 1,25-(OH) 2 D 3 in a reporter assay using mouse and human adrenocortical carcinoma cells (90). In MCF-7 cells, TEI-9647 reversed the 1,25-(OH) 2 D 3 -induced inhibition of aromatase enzyme, which is responsible for the conversion of testosterone to estradiol (91). In primary ERα-negative breast cancer cells, TEI-9647 reduced the induction of mRNA levels of ERα in the presence of 1,25-(OH) 2 D 3 (92).…”

Section: Vdr Antagonists or Allosteric Inhibition Of The Vdr–coregmentioning

confidence: 99%

Inhibitors for the Vitamin D Receptor–Coregulator Interaction

Teske

2016

Vitamin D Hormone

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The vitamin D receptor (VDR) belongs to the superfamily of nuclear receptors and is activated by the endogenous ligand 1,25-dihydroxyvitamin D3. The genomic effects mediated by VDR consist of the activation and repression of gene transcription, which includes the formation of multi-protein complexes with coregulator proteins. Coregulators bind many nuclear receptors and can be categorized according their role as coactivators (gene activation) or corepressors (gene repression). Herein, different approaches to develop compounds that modulate the interaction between VDR and coregulators are summarized. This include coregulator peptides that were identified by creating phage display libraries. Subsequent modification of these peptides including the introduction of a tether or non-hydrolysable bonds resulted in the first direct VDR–coregulator inhibitors. Later, small molecules that inhibit VDR–coregulator inhibitors were identified using rational drug design and high throughput screening. Early on, allosteric inhibition of VDR–coregulator interactions was achieved with VDR antagonists that change the conformation of VDR and modulate the interactions with coregulators. A detailed discussion of their dual agonist/antagonist effects is given as well as a summary of their biological effects in cell-based assays and in vivo studies.

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1α,25-Dihydroxyvitamin D3 exerts tissue-specific effects on estrogen and androgen metabolism

Cited by 44 publications

References 36 publications

A comparison of vitamin D activity in paired non-malignant and malignant human breast tissues

A comparison of vitamin D activity in paired non-malignant and malignant human breast tissues

Vitamin D metabolism, sex hormones, and male reproductive function

Inhibitors for the Vitamin D Receptor–Coregulator Interaction

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