scholarly journals Sex steroids regulate skin pigmentation through nonclassical membrane-bound receptors

eLife ◽  
2016 ◽  
Vol 5 ◽  
Author(s):  
Christopher A Natale ◽  
Elizabeth K Duperret ◽  
Junqian Zhang ◽  
Rochelle Sadeghi ◽  
Ankit Dahal ◽  
...  
Keyword(s):  
Hormone Receptors ◽  
Treatment Options ◽  
Skin Pigmentation ◽  
Progesterone Receptors ◽  
Steroid Hormone Receptors ◽  
Pigment Synthesis ◽  
17Β Estradiol ◽  
Membrane Bound ◽  
Epidermal Melanocyte ◽  
G Protein Coupled

The association between pregnancy and altered cutaneous pigmentation has been documented for over two millennia, suggesting that sex hormones play a role in regulating epidermal melanocyte (MC) homeostasis. Here we show that physiologic estrogen (17β-estradiol) and progesterone reciprocally regulate melanin synthesis. This is intriguing given that we also show that normal primary human MCs lack classical estrogen or progesterone receptors (ER or PR). Utilizing both genetic and pharmacologic approaches, we establish that sex steroid effects on human pigment synthesis are mediated by the membrane-bound, steroid hormone receptors G protein-coupled estrogen receptor (GPER), and progestin and adipoQ receptor 7 (PAQR7). Activity of these receptors was activated or inhibited by synthetic estrogen or progesterone analogs that do not bind to ER or PR. As safe and effective treatment options for skin pigmentation disorders are limited, these specific GPER and PAQR7 ligands may represent a novel class of therapeutics.

scholarly journals 3C. 3-Ketosteroid receptors in GtoPdb v.2021.3

2021 ◽  
Vol 2021 (3) ◽  
Author(s):  
Derek Cain ◽  
John Cidlowski ◽  
Dean P. Edwards ◽  
Peter Fuller ◽  
Sandra L. Grimm ◽  
...  
Keyword(s):  
Hormone Receptors ◽  
Steroid Hormone ◽  
Steroid Hormone Receptors ◽  
Nuclear Hormone Receptors ◽  
17Β Estradiol

Steroid hormone receptors (nomenclature as agreed by the NC-IUPHAR Subcommittee on Nuclear Hormone Receptors [74, 215, 3]) are nuclear hormone receptors of the NR3 class, with endogenous agonists that may be divided into 3-hydroxysteroids (estrone and 17β-estradiol) and 3-ketosteroids (dihydrotestosterone [DHT], aldosterone, cortisol, corticosterone, progesterone and testosterone). For rodent GR and MR, the physiological ligand is corticosterone rather than cortisol.

Proliferative diseases of the uterus: clinical, immunological, and molecular aspects

2020 ◽  
Vol 19 (5) ◽  
pp. 13-21
Author(s):  
S.V. Shramko ◽  
◽  
L.F. Gulyaeva ◽  
V.N. Zorina ◽  
T.V. Tretyakova ◽  
...  
Keyword(s):  
Estrogen Receptors ◽  
Hormone Receptors ◽  
Acute Phase Proteins ◽  
Uterine Fibroids ◽  
Progesterone Receptors ◽  
Serum Levels ◽  
Steroid Hormone Receptors ◽  
Sex Steroid Hormone ◽  
Expression Of Genes ◽  
Genes Encoding

Objective. To perform comparative analysis of clinical data, serum levels of acute-phase proteins, cytokines, steroid hormones, and expression of genes encoding sex hormone receptors in tissues of patients with proliferative diseases of the uterus. Patients and methods. We analyzed clinical data of 349 patients with various proliferative diseases of the uterus. We also evaluated their serum levels of α2-macroglobulin, pregnancy-associated α2-glycoprotein, their immunocomplexes with IgG, lactoferrin, VEGF, IL-6, TNFa, IL-8, and sex hormones. Uterine tissue samples were tested for the expression of genes encoding estrogen receptors α and β (ЕRα, ЕRβ) and progesterone receptors (PGR). Data analysis was performed using the statistical packages of SAS 9.4, STATISTICA12, and IBM-SPSS Statistics 22. Results. The changes in the level of acute-phase proteins indicated inflammation. In isolated uterine fibroids, expression of genes encoding progesterone receptors prevailed, whereas in isolated adenomyosis, expression of genes encoding estrogen receptors prevailed. Patients with both uterine fibroids and adenomyosis demonstrated similar levels of expression of genes encoding sex steroid hormone receptors. Tissues of uterine leiomyosarcoma were characterized by downregulated expression of genes encoding sex steroid hormone receptors. Conclusion. Upregulation of genes encoding progesterone receptors in isolated uterine fibroids confirms that therapy with progesterone receptor blockers is appropriate in this case. The predominance of expression of genes encoding estrogen receptors in isolated adenomyosis indicates local hyperestrogenism, justifying the use of progestogens and antiestrogens. Equal expression of genes encoding estrogen and progesterone receptors in patients with combined disease, as wells as high frequency of inflammatory changes in tissues and increased serum levels of inflammatory markers, proves the need for antiinflammatory therapy. Key words: adenomyosis, inflammation, steroid receptor genes, leiomyosarcoma, uterine fibroids, gene expression

scholarly journals Minireview: G Protein-Coupled Estrogen Receptor-1, GPER-1: Its Mechanism of Action and Role in Female Reproductive Cancer, Renal and Vascular Physiology

Endocrinology ◽  
2012 ◽  
Vol 153 (7) ◽  
pp. 2953-2962 ◽  
Author(s):  
Edward J. Filardo ◽  
Peter Thomas
Keyword(s):  
Estrogen Receptor ◽  
G Protein ◽  
Mechanism Of Action ◽  
Knockout Mice ◽  
Mammalian Cells ◽  
Hormone Receptors ◽  
Bone Growth ◽  
Steroid Hormone Receptors ◽  
Vascular Physiology ◽  
G Protein Coupled

Using cDNA cloning strategies commonly employed for G protein-coupled receptors (GPCR), GPCR-30 (GPR30), was isolated from mammalian cells before knowledge of its cognate ligand. GPR30 is evolutionarily conserved throughout the vertebrates. A broad literature suggests that GPR30 is a Gs-coupled heptahelical transmembrane receptor that promotes specific binding of naturally occurring and man-made estrogens but not cortisol, progesterone, or testosterone. Its “pregenomic” signaling actions are manifested by plasma membrane-associated actions familiar to GPCR, namely, stimulation of adenylyl cyclase and Gβγ-subunit protein-dependent release of membrane-tethered heparan bound epidermal growth factor. These facts regarding its mechanism of action have led to the formal renaming of this receptor to its current functional designate, G protein-coupled estrogen receptor (ER) (GPER)-1. Further insight regarding its biochemical action and physiological functions in vertebrates is derived from receptor knockdown studies and the use of selective agonists/antagonists that discriminate GPER-1 from the nuclear steroid hormone receptors, ERα and ERβ. GPER-1-selective agents have linked GPER-1 to physiological and pathological events regulated by estrogen action, including, but not limited to, the central nervous, immune, renal, reproductive, and cardiovascular systems. Moreover, immunohistochemical studies have shown a positive association between GPER-1 expression and progression of female reproductive cancer, a relationship that is diametrically opposed from ER. Unlike ER knockout mice, GPER-1 knockout mice are fertile and show no overt reproductive anomalies. However, they do exhibit thymic atrophy, impaired glucose tolerance, and altered bone growth. Here, we discuss the role of GPER-1 in female reproductive cancers as well as renal and vascular physiology.

Immunohistochemical localization of intracellular progesterone and glucocorticoid receptors in the rabbit lung

1994 ◽  
Vol 142 (2) ◽  
pp. 311-316 ◽  
Author(s):  
I Camacho-Arroyo ◽  
A Ruiz ◽  
A Gamboa-Domínguez ◽  
G Pérez-Palacios ◽  
M A Cerbón
Keyword(s):  
Glucocorticoid Receptors ◽  
Hormone Receptors ◽  
Progesterone Receptors ◽  
Cell Types ◽  
Immunohistochemical Localization ◽  
Alveolar Epithelial Cells ◽  
Steroid Hormone Receptors ◽  
Polymorphonuclear Leucocytes ◽  
Rabbit Lung ◽  
Oestradiol Treatment

Abstract We have determined the presence and distribution of intracellular progesterone receptors (PRs) and glucocorticoid receptors (GRs) in the lung of adult female rabbits using immunohistochemistry. The effects of ovariectomy and administration of oestradiol benzoate (10 μg for 3 consecutive days) upon PR and GR immunoreactivity were also studied. The results demonstrated the presence of both steroid hormone receptors in the female rabbit lung. PR and GR immunoreactivity was predominantly nuclear and located in alveolar epithelial cells and various interstitial cells such as polymorphonuclear leucocytes. Tissue distribution of both receptors was similar in all cases. Oestradiol treatment induced a marked increase in the number of PR immunoreactive cells compared with intact and ovariectomized female animals. Neither ovariectomy nor oestradiol treatment modified the number of GR immunoreactive cells. The presence and localization of intracellular PRs and GRs in several lung cell types suggest that they may play an important role in mediating the effects of progesterone and glucocorticoids in various physiological processes in the rabbit lung. The data also indicated an oestrogen regulation of PRs in the rabbit lung. Journal of Endocrinology (1994) 142, 311–316

Fibromatosis of the Breast

2000 ◽  
Vol 124 (2) ◽  
pp. 276-280 ◽  
Author(s):  
Mojgan Devouassoux-Shisheboran ◽  
David P. Schammel ◽  
Yan-Gao Man ◽  
Fattaneh A. Tavassoli
Keyword(s):  
Estrogen Receptor ◽  
Androgen Receptor ◽  
Hormone Receptors ◽  
Spindle Cell ◽  
Immunohistochemical Study ◽  
Progesterone Receptors ◽  
Steroid Hormone Receptors ◽  
Childbearing Age ◽  
Sex Steroid Hormone ◽  
Receptor Profile

Abstract Objective.—To predict if antiestrogenic agents are useful in the treatment of breast fibromatoses, we undertook an immunohistochemical study of sex steroid hormone receptors (estrogen receptor, progesterone receptor, and androgen receptor) and protein pS2 in 33 cases. Methods.—The morphologic and immunohistochemical findings were correlated to patient menstrual status, which was categorized as childbearing age (n = 15), perimenopausal (n = 8), and postmenopausal (n = 10). Results.—Fibromatoses in women of childbearing age were more cellular, more mitotically active, and displayed a larger proportion of cells with mild atypia than those in perimenopausal and postmenopausal women. The hormonal status of these 3 groups does not explain the morphologic variations observed in these groups, inasmuch as no immunostaining for any of the hormone receptors was detected in the tumors. Conclusions.—The absence of estrogen receptor and pS2 in breast fibromatoses suggests that antiestrogenic agents are unlikely to be beneficial in the management of these tumors. Assessment of the hormone receptor profile is a useful adjunct in the diagnosis of spindle cell lesions of the breast. Although most spindle cell carcinomas as well as fibromatoses of the breast do not express estrogen or progesterone receptors, the absence of androgen receptor reactivity would favor a diagnosis of fibromatosis over that of myofibroblastoma.

Immunohistochemical assessment of progesterone, oestrogen and glucocorticoid receptors in bovine placentomes during pregnancy, induced parturition, and after birth with or without retention of fetal membranes

Reproduction ◽  
2000 ◽  
pp. 351-360 ◽  
Author(s):  
A Boos ◽  
J Kohtes ◽  
A Stelljes ◽  
H Zerbe ◽  
HH Thole
Keyword(s):  
Caesarean Section ◽  
Connective Tissue ◽  
Glucocorticoid Receptors ◽  
Hormone Receptors ◽  
Post Partum ◽  
Progesterone Receptors ◽  
Steroid Hormone Receptors ◽  
Fetal Membranes ◽  
Oestrogen Receptors ◽  
Tissue Cells

Steroid hormones play an important role in placental development. However, the exact cellular site of hormone action has not been evaluated in bovine placentomes. Thus, the present immunohistochemical study was designed to assess the distribution of progesterone receptors, oestrogen receptors and glucocorticoid receptors in bovine placentomes. Tissue specimens were obtained from cows at slaughter and from cattle during pre-term Caesarean section 27 h after prostaglandin administration, immediately after spontaneous parturition and from cattle that had retained the fetal membranes. Specific antibodies were used for receptor demonstration in tissue sections. Progesterone receptors were only detected in maternal connective tissue cells, whereas oestrogen receptors were also present in maternal crypt epithelium. At specific sites, both receptor immunoreactivities remained constant or changed significantly during pregnancy, were generally higher during Caesarean section and decreased post partum, but were less pronounced in cattle that released the fetal membranes than in those that retained the fetal membranes. Glucocorticoid receptors were evident in fetal connective tissue cells as well as in fetal and maternal blood vessels. Maternal crypt epithelial cells showed increasing immunoreactivities for glucocorticoid receptors during pregnancy. Receptor immunoreactivities tended to be lower after spontaneous parturition than during Caesarean section; these results were significant for progesterone and oestrogen receptors in animals that released the fetal membranes but not for those that retained the fetal membranes. The results indicate that in bovine placentome steroid hormone receptors are distributed in patterns that are specific to the type of cell, the stage of pregnancy and the tissue location, implying highly specific modulation of placental metabolism. Retention of the fetal membranes is reflected by altered placental receptor states at parturition.

Steroid Hormone Receptors in Meningiomas of Chinese Patients

Neurosurgery ◽  
1989 ◽  
Vol 25 (4) ◽  
pp. 541-545 ◽  
Author(s):  
Liang-Shong Lee ◽  
Chin-Wen Chi ◽  
Tai-Jay Chang ◽  
Min-Deh Chou ◽  
Hsiu-Chih Liu ◽  
...  
Keyword(s):  
Malignant Lymphoma ◽  
Glucocorticoid Receptors ◽  
Hormone Receptors ◽  
Steroid Hormone ◽  
Progesterone Receptors ◽  
Tyrosine Aminotransferase ◽  
Intracranial Tumor ◽  
Steroid Hormone Receptors ◽  
Chinese Patients ◽  
Anaplastic Ependymoma

Abstract Meningioma is a hormone-related intracranial tumor. Brain tumor samples were collected from 32 Chinese patients, 20 of whom had meningiomas. Estrogen receptors were present in 6 of 17 meningiomas, 1 hemangioblastoma, 1 gemistocytic astrocytoma, and 1 neurilemoma. Of the 26 samples assayed for progesterone receptors, measurable bindings were found in 14 of 17 meningiomas, 1 of 2 astrocytomas, 1 malignant lymphoma, 1 hemangioblastoma, 1 ganglioglioma, 1 glioblastoma multiforme, 1 anaplastic ependymoma, 1 small cell sarcoma, and 1 neurilemoma. Androgen receptors were found in 8 of 19 meningiomas, but not in the 11 other brain tumors examined. Measurable glucocorticoid receptors were found in 15 of 19 meningiomas, 1 malignant lymphoma, 1 hemangioblastoma, 2 craniopharyngiomas, 1 neurilemoma, 1 of 2 glioblastomas, and 1 of 2 astrocytomas. Of the 10 samples examined for tyrosine aminotransferase activity, measurable enzyme activity was found in 7 of the 8 meningiomas, but not in the single hemangioblastoma nor in the single craniopharyngioma. In accordance with other published studies, the results from this study also suggest that the growth of meningiomas may be regulated by hormones, and that the role steroid hormones and their receptors play in the meningioma is worthy of further investigation.

scholarly journals Interaction of oestrogen and progesterone receptors with specific subfractions of laying-hen oviduct chromatin

1984 ◽  
Vol 217 (1) ◽  
pp. 309-316 ◽  
Author(s):  
N Massol ◽  
M C Lebeau ◽  
E E Baulieu
Keyword(s):  
Progesterone Receptor ◽  
Oestrogen Receptor ◽  
Hormone Receptors ◽  
Steroid Hormone ◽  
Progesterone Receptors ◽  
Steroid Hormone Receptors ◽  
Target Tissue ◽  
Low Salt ◽  
High Concentrations

Salt (NaCl)-extracted nuclear oestrogen receptor from hen oviduct was incubated with salt-depleted oviduct chromatin and dialysed to low salt. The oestrogen receptor (re)associated with chromatin to form a 13-14S-sedimenting fraction, as found in ‘native’ chromatin, and saturation of this interaction was obtained for very low receptor concentrations (approx. 0.04 nM). Similarly, purified progesterone receptor from chick oviduct cytosol associated with depleted chromatin to form an 11-12S-sedimenting fraction, as in ‘native’ chromatin; this interaction tended towards saturation for much higher concentrations of progesterone receptor (approx. 8 nM) than that observed for oestrogen receptor. When the two receptors were incubated with depleted chromatin from hen kidney or erythrocytes, their s values were as for oviduct chromatin. However, no saturation of these interactions was seen, even for high concentrations of receptor. Steroid-hormone receptors can therefore bind in vitro to particular subfractions of non-target-tissue chromatin, but with a much lower affinity than to target-tissue chromatin.

GnRH agonist (buserelin) up regulates estrogen receptor α mRNA but not estrogen receptor β and progesterone receptor mRNA in bovine endometrium in vitro

2009 ◽  
Vol 89 (4) ◽  
pp. 467-473 ◽  
Author(s):  
R Singh ◽  
T Pretheeban ◽  
R Rajamahendran
Keyword(s):  
Estrogen Receptor ◽  
Estrogen Receptors ◽  
Gnrh Agonist ◽  
Luteal Phase ◽  
Hormone Receptors ◽  
Steroid Hormone ◽  
Progesterone Receptors ◽  
Gonadotropin Releasing Hormone ◽  
Steroid Hormone Receptors ◽  
Releasing Hormone

The local modulatory role of gonadotropin releasing hormone (GnRH), gonadotropin releasing hormone receptor (GnRH-R) system in regulating steroid hormone receptors at the endometrial level is still not known. Estrogen and progesterone maintain uterine functions by acting through their corresponding receptors; estrogen receptors (ERα and ERβ) and progesterone receptors (PR). We recently demonstrated GnRH-R in bovine endometrium and find the co-existence of GnRH and steroid hormone receptors in endometrium as interesting. Our objective was to determine the effect of a GnRH agonist (buserelin), on the expression of ERα, ERβ, and PR messenger RNA (mRNA) in bovine endometrium. Reproductive tracts were collected from slaughtered cows at a local abattoir, and endometrial explants were treated with buserelin (0, 200, 500, 1000 ng mL-1 respectively), GnRH antagonist-antide (500 ng mL-1) and antide + buserelin (500+200 ng mL-1) for 6 h and stored at -80°C for RNA extraction. Two micrograms of total RNA was subjected to reverse transcription polymerase chain reaction, PCR products electrophoresed (2% agrose gel); visualized and statistically analyzed. The results showed that buserelin (200 ng mL-1) increased the expression of ERα in the luteal phase endometrium. In addition, the expression of endometrial ERα was greater during the follicular than luteal phase. This up regulation of ERα mRNA in luteal phase endometrium suggests that GnRH administration may influence pregnancy in bovines. Key words: GnRH, bovine, endometrium, estrogen receptors, progesterone receptors

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