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Journal articles on the topic 'Estrogen Molecular structures'

Author: Grafiati

Published: 4 June 2021

Last updated: 13 February 2022

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1

Nilsson, Stefan, Sari Mäkelä, Eckardt Treuter, et al. "Mechanisms of Estrogen Action." Physiological Reviews 81, no. 4 (2001): 1535–65. http://dx.doi.org/10.1152/physrev.2001.81.4.1535.

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Our appreciation of the physiological functions of estrogens and the mechanisms through which estrogens bring about these functions has changed during the past decade. Just as transgenic mice were produced in which estrogen receptors had been inactivated and we thought that we were about to understand the role of estrogen receptors in physiology and pathology, it was found that there was not one but two distinct and functional estrogen receptors, now called ERα and ERβ. Transgenic mice in which each of the receptors or both the receptors are inactive have revealed a much broader role for estro

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TERENTIEV, ALEXANDER A., NURBUBU T. MOLDOGAZIEVA, OLGA V. LEVTSOVA, DMITRY M. MAXIMENKO, DENIS A. BOROZDENKO, and KONSTANTIN V. SHAITAN. "MODELING OF THREE DIMENSIONAL STRUCTURE OF HUMAN ALPHA-FETOPROTEIN COMPLEXED WITH DIETHYLSTILBESTROL: DOCKING AND MOLECULAR DYNAMICS SIMULATION STUDY." Journal of Bioinformatics and Computational Biology 10, no. 02 (2012): 1241012. http://dx.doi.org/10.1142/s0219720012410120.

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It has been long experimentally demonstrated that human alpha-fetoprotein (HAFP) has an ability to bind immobilized estrogens with the most efficiency for synthetic estrogen analog — diethylstilbestrol (DES). However, the question remains why the human AFP (HAFP), unlike rodent AFP, cannot bind free estrogens. Moreover, despite the fact that AFP was first discovered more than 50 years ago and is presently recognized as a "golden standard" among onco-biomarkers, its three-dimensional (3D) structure has not been experimentally solved yet. In this work using MODELLER program, we generated 3D mode

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3

Ellmann, Stephan, Heinrich Sticht, Falk Thiel, Matthias W. Beckmann, Reiner Strick, and Pamela L. Strissel. "Estrogen and progesterone receptors: from molecular structures to clinical targets." Cellular and Molecular Life Sciences 66, no. 15 (2009): 2405–26. http://dx.doi.org/10.1007/s00018-009-0017-3.

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Kerdivel, Gwenneg, Denis Habauzit, and Farzad Pakdel. "Assessment and Molecular Actions of Endocrine-Disrupting Chemicals That Interfere with Estrogen Receptor Pathways." International Journal of Endocrinology 2013 (2013): 1–14. http://dx.doi.org/10.1155/2013/501851.

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In all vertebrate species, estrogens play a crucial role in the development, growth, and function of reproductive and nonreproductive tissues. A large number of natural or synthetic chemicals present in the environment and diet can interfere with estrogen signaling; these chemicals are called endocrine disrupting chemicals (EDCs) or xenoestrogens. Some of these compounds have been shown to induce adverse effects on human and animal health, and some compounds are suspected to contribute to diverse disease development. Because xenoestrogens have varying sources and structures and could act in ad

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Charitidi, Konstantina, Inna Meltser, and Barbara Canlon. "Estradiol Treatment and Hormonal Fluctuations During the Estrous Cycle Modulate the Expression of Estrogen Receptors in the Auditory System and the Prepulse Inhibition of Acoustic Startle Response." Endocrinology 153, no. 9 (2012): 4412–21. http://dx.doi.org/10.1210/en.2012-1416.

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Estrogens' effects on hearing are documented across species, but the responsible molecular mechanisms remain unknown. The presence of estrogen receptors (ER) throughout the auditory system offers a potential pathway of direct estrogenic effects on auditory function, but little is known about how each ER's expression is regulated by the overall hormonal status of the body. In the present study, we determined the effects of ovariectomy and chronic 17β-estradiol treatment on mRNA and protein expression of ERα and ERβ in peripheral (cochlea) and central (inferior colliculus) auditory structures of

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6

Makar, Subhajit, Abhrajyoti Ghosh, Ashok Kumar, and Sushil K. Singh. "Recent Studies on Aromatase and Sulfatase Involved in Breast Cancer and their Inhibitors." Current Enzyme Inhibition 16, no. 1 (2020): 20–44. http://dx.doi.org/10.2174/1573408016666200325120248.

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Enzyme aromatase uses several androgen substrates for the biosynthesis of estrogen, i.e. conversion of androstenedione to estrone and testosterone to biologically potent estradiol. Aromatase inhibitors (AIs) such as anastrozole, letrozole and exemestane have been established in standard endocrine therapy of breast cancer, by interfering with estrogen signaling cascade. Steroid sulphatase (STS) regulates the level of active oestrogens and androgens in human target organs and steroidogenic tissues, which have a key role in hormone dependent breast cancers (HDBC). Sulfatase is still under the exp

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Tamura, Fumiya, Shintaro Sugimoto, Mana Sugimoto, et al. "The Effect of a Synthetic Estrogen, Ethinylestradiol, on the hERG Block by E-4031." Biomolecules 11, no. 9 (2021): 1385. http://dx.doi.org/10.3390/biom11091385.

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Inhibition of K+-conductance through the human ether-a-go-go related gene (hERG) channel leads to QT prolongation and is associated with cardiac arrhythmias. We previously reported that physiological concentrations of some estrogens partially suppress the hERG channel currents by interacting with the S6 residue F656 and increase the sensitivity of hERG blockade by E-4031. Although these studies suggested that clinically used synthetic estrogens with similar structures have the marked potential to alter hERG functions, the hERG interactions with synthetic estrogens have not been assessed. We th

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8

Lephart, Edwin D. "Modulation of Aromatase by Phytoestrogens." Enzyme Research 2015 (December 21, 2015): 1–11. http://dx.doi.org/10.1155/2015/594656.

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The aromatase enzyme catalyzes the conversion of androgens to estrogens in many human tissues. Estrogens are known to stimulate cellular proliferation associated with certain cancers and protect against adverse symptoms during the peri- and postmenopausal intervals. Phytoestrogens are a group of plant derived naturally occurring compounds that have chemical structures similar to estrogen. Since phytoestrogens are known to be constituents of animal/human food sources, these compounds have received increased research attention. Phytoestrogens may contribute to decreased cancer risk by the inhibi

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9

Amr, Abd, Elsayed Elsayed, Mohamed Al-Omar, Hanan Badr Eldin, Eman Nossier, and Mohamed Abdallah. "Design, Synthesis, Anticancer Evaluation and Molecular Modeling of Novel Estrogen Derivatives." Molecules 24, no. 3 (2019): 416. http://dx.doi.org/10.3390/molecules24030416.

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A series of estrone derivatives 3–8 was designed and synthesized using estrone arylmethylenes 2a,b as starting materials and their structures were confirmed by different spectral data and elemental analyses. All the newly synthesized compounds exhibited potent in vitro and in vivo cytotoxic activities against breast cancer cell lines. In addition, all compounds were subjected to in vitro and in vivo inhibition assays for EGFR and VEGFR-2 kinases as well as p53 ubiquitination activity to obtain more details about their mechanism of action. Based on the promising results, a molecular docking stu

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Padron, Adrian, Li Li, Eric M. Kofoed та Fred Schaufele. "Ligand-Selective Interdomain Conformations of Estrogen Receptor-α". Molecular Endocrinology 21, № 1 (2007): 49–61. http://dx.doi.org/10.1210/me.2006-0075.

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Abstract Selective estrogen receptor modulators (SERMs) inhibit estrogen activation of the estrogen receptor (ER) in some tissues but activate ER in other tissues. These tissue-selective actions suggest that SERMs may be identified with tissue specificities that would improve the safety of breast cancer and hormone replacement therapies. The identification of an improved SERM would be aided by understanding the effects of each SERM on the structure and interactions of ER. To date, the inability to obtain structures of the full-length ER has limited our structural characterization of SERM actio

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11

Ohta, Kiminori, Takumi Ogawa, Asako Kaise, and Yasuyuki Endo. "Novel estrogen receptor (ER) modulators containing various hydrophobic bent-core structures." Bioorganic & Medicinal Chemistry 22, no. 13 (2014): 3508–14. http://dx.doi.org/10.1016/j.bmc.2014.04.022.

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12

Lin, Valerie C. L., Eng Hen Ng, Swee Eng Aw, Michelle G. K. Tan, Esther H. L. Ng, and Boon Huat Bay. "Progesterone Induces Focal Adhesion in Breast Cancer Cells MDA-MB-231 Transfected with Progesterone Receptor Complementary DNA." Molecular Endocrinology 14, no. 3 (2000): 348–58. http://dx.doi.org/10.1210/mend.14.3.0426.

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Abstract Since the effects of progesterone are mediated mainly via estrogen-dependent progesterone receptor (PR), the expression of the effects of progesterone may be masked or overridden by the influence of estrogen under conditions in which priming with estrogens is required. We have established a PR-positive but estrogen receptor-α (ER-α) negative breast cancer cell model by transfecting PR cDNA into ER-α- and PR-negative MDA-MB-231 cells in order that the functions of progesterone can be studied independently of estrogens. We have demonstrated using this model that progesterone markedly in

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13

Mandal, Suman Kumar, and Parthapratim Munshi. "Predicting Accurate Lead Structures for Screening Molecular Libraries: A Quantum Crystallographic Approach." Molecules 26, no. 9 (2021): 2605. http://dx.doi.org/10.3390/molecules26092605.

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Optimization of lead structures is crucial for drug discovery. However, the accuracy of such a prediction using the traditional molecular docking approach remains a major concern. Our study demonstrates that the employment of quantum crystallographic approach-counterpoise corrected kernel energy method (KEM-CP) can improve the accuracy by and large. We select human aldose reductase at 0.66 Å, cyclin dependent kinase 2 at 2.0 Å and estrogen receptor β at 2.7 Å resolutions with active site environment ranging from highly hydrophilic to moderate to highly hydrophobic and several of their known li

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14

Rossini, Gian Paolo, and Lorenzo Camellini. "Oligomeric structures of cytosoluble estrogen-receptor complexes as studied by anti-estrogen receptor antibodies and chemical crosslinking of intact cells." Journal of Steroid Biochemistry and Molecular Biology 50, no. 5-6 (1994): 241–52. http://dx.doi.org/10.1016/0960-0760(94)90128-7.

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15

Kartika, I. Gusti Agung Ayu, In Jae Bang, Catur Riani, et al. "Isolation and Characterization of Phenylpropanoid and Lignan Compounds from Peperomia pellucida [L.] Kunth with Estrogenic Activities." Molecules 25, no. 21 (2020): 4914. http://dx.doi.org/10.3390/molecules25214914.

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Extracts of Peperomia pellucida [L.] Kunth have previously been demonstrated to have in vivo estrogenic-like effects, thereby functioning as an anti-osteoporotic agent. However, the compounds responsible for these effects have not yet been determined. Therefore, the aim of this study is to isolate and elucidate potential compounds with estrogenic activity. The structures of the isolated compounds were identified using 1D 1H and 13C-NMR and confirmed by 2D FT-NMR. The estrogenic activity was evaluated using the E-SCREEN assay, and a molecular docking study was performed to predict the binding a

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16

Shi, Bin, Jing Liang, Xiaohan Yang, et al. "Integration of Estrogen and Wnt Signaling Circuits by the Polycomb Group Protein EZH2 in Breast Cancer Cells." Molecular and Cellular Biology 27, no. 14 (2007): 5105–19. http://dx.doi.org/10.1128/mcb.00162-07.

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ABSTRACT Essential for embryonic development, the polycomb group protein enhancer of zeste homolog 2 (EZH2) is overexpressed in breast and prostate cancers and is implicated in the growth and aggression of the tumors. The tumorigenic mechanism underlying EZH2 overexpression is largely unknown. It is believed that EZH2 exerts its biological activity as a transcription repressor. However, we report here that EZH2 functions in gene transcriptional activation in breast cancer cells. We show that EZH2 transactivates genes that are commonly targeted by estrogen and Wnt signaling pathways. We demonst

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17

Dermawan, Doni, Riyadi Sumirtanurdin, and Deti Dewantisari. "Molecular Dynamics Simulation Estrogen Receptor Alpha againts Andrographolide as Anti Breast Cancer." Indonesian Journal of Pharmaceutical Science and Technology 6, no. 2 (2019): 65. http://dx.doi.org/10.24198/ijpst.v6i2.18168.

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Breast cancer is the most common cancer suffered by women with 1.67 million new cases in the world by 2012 with a mortality rate of 12.9%. Tamoxifen is a standard therapy for breast cancer but can cause endometrial and thromboembolic cancer. Andrografolid is an active compound from Andrographis paniculata which has antiproliferation activity of MCF-7 breast cancer cells with IC50 was 61.11 μM. The purpose of this study was to design andrographolide modification structures as human estrogen receptor alpha (hER-α) antagonists. Molecular docking simulation results showed that the andrographolide

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18

Pashay Ahi, Ehsan, Benjamin S. Walker, Christopher S. Lassiter, and Zophonías O. Jónsson. "Investigation of the effects of estrogen on skeletal gene expression during zebrafish larval head development." PeerJ 4 (March 31, 2016): e1878. http://dx.doi.org/10.7717/peerj.1878.

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The development of craniofacial skeletal structures requires well-orchestrated tissue interactions controlled by distinct molecular signals. Disruptions in normal function of these molecular signals have been associated with a wide range of craniofacial malformations. A pathway mediated by estrogens is one of those molecular signals that plays role in formation of bone and cartilage including craniofacial skeletogenesis. Studies in zebrafish have shown that while higher concentrations of 17-βestradiol (E2) cause severe craniofacial defects, treatment with lower concentrations result in subtle

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19

Dat, Vu Van, Le Kim Long, Nguyen Hoang Trang, Doan Van Phuc, Nguyen Van Trang, and Nguyen Thi Thu Ha. "PREDICTING ESTROGEN ACTIVITIES OF BISPHENOL A AND ITS ANALOGS USING QUANTUM CHEMISTRY CALCULATIONS AND ARTIFICIAL NEURAL NETWORKS." IZVESTIYA VYSSHIKH UCHEBNYKH ZAVEDENII KHIMIYA KHIMICHESKAYA TEKHNOLOGIYA 62, no. 5 (2019): 31–37. http://dx.doi.org/10.6060/ivkkt.20196205.5933.

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This article presents the results of the quantitative structure – activity relationship (QSAR) study of bisphenol A (BPA) and its analogs using quantum chemistry calculations and method of artificial neural networks (ANN). Molecular structural analysis is performed using Density Functional Theory (DFT) at the B3LYP/6-31+G(d) level. The quantum calculations focus on finding the optimized molecular structures, vibrational frequencies, the molecular orbital energies with reasonable accuracy. The study of electron density distribution was carried out in the framework of the natural bond orbital (N

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20

Branowska, Danuta, Zbigniew Karczmarzyk, Ewa Wolińska, et al. "1,2,4-Triazine Sulfonamides: Synthesis by Sulfenamide Intermediates, In Vitro Anticancer Screening, Structural Characterization, and Molecular Docking Study." Molecules 25, no. 10 (2020): 2324. http://dx.doi.org/10.3390/molecules25102324.

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In this study, we synthesized novel sulfonamides with a 1,2,4-triazine moiety according to pharmacophore requirements for biological activity. All the synthesized compounds were tested in vitro to verify whether they exhibited anticancer activity against the human breast cancer cell lines MCF-7 and MDA-MB-231. Among them, two most active ones, having IC50 values of 50 and 42 µM, respectively, were found to show higher anticancer activity than chlorambucil used as the reference in the in vitro tests. In addition, two other compounds, which had IC50 values of 78 and 91 µM, respectively, exhibite

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21

Barlow, John, Theresa Casey, Jen-Fu Chiu, and Karen Plaut. "Estrogen Affects Development of Alveolar Structures in Whole-Organ Culture of Mouse Mammary Glands." Biochemical and Biophysical Research Communications 232, no. 2 (1997): 340–44. http://dx.doi.org/10.1006/bbrc.1997.6283.

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22

Sakkiah, Sugunadevi, Chandrabose Selvaraj, Wenjing Guo та ін. "Elucidation of Agonist and Antagonist Dynamic Binding Patterns in ER-α by Integration of Molecular Docking, Molecular Dynamics Simulations and Quantum Mechanical Calculations". International Journal of Molecular Sciences 22, № 17 (2021): 9371. http://dx.doi.org/10.3390/ijms22179371.

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Estrogen receptor alpha (ERα) is a ligand-dependent transcriptional factor in the nuclear receptor superfamily. Many structures of ERα bound with agonists and antagonists have been determined. However, the dynamic binding patterns of agonists and antagonists in the binding site of ERα remains unclear. Therefore, we performed molecular docking, molecular dynamics (MD) simulations, and quantum mechanical calculations to elucidate agonist and antagonist dynamic binding patterns in ERα. 17β-estradiol (E2) and 4-hydroxytamoxifen (OHT) were docked in the ligand binding pockets of the agonist and ant

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23

Rytel, Liliana, and Slawomir Gonkowski. "The Influence of Bisphenol a on the Nitrergic Nervous Structures in the Domestic Porcine Uterus." International Journal of Molecular Sciences 21, no. 12 (2020): 4543. http://dx.doi.org/10.3390/ijms21124543.

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Bisphenol A (BPA) is one of the most common environmental pollutants among endocrine disruptors. Due to its similarity to estrogen, BPA may affect estrogen receptors and show adverse effects on many internal organs. The reproductive system is particularly vulnerable to the impact of BPA, but knowledge about BPA-induced changes in the innervation of the uterus is relatively scarce. Therefore, this study aimed to investigate the influence of various doses of BPA on nitrergic nerves supplying the uterus with the double immunofluorescence method. It has been shown that even low doses of BPA caused

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24

Yang, Yong-Xiao, Peng Li, Pan Wang та Bao-Ting Zhu. "17β-Estradiol-Induced Conformational Changes of Human Microsomal Triglyceride Transfer Protein: A Computational Molecular Modelling Study". Cells 10, № 7 (2021): 1566. http://dx.doi.org/10.3390/cells10071566.

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Human microsomal triglyceride transfer protein (hMTP) plays an essential role in the assembly of apoB-containing lipoproteins, and has become an important drug target for the treatment of several disease states, such as abetalipoproteinemia, fat malabsorption and familial hypercholesterolemia. hMTP is a heterodimer composed of a larger hMTPα subunit and a smaller hMTPβ subunit (namely, protein disulfide isomerase, hPDI). hPDI can interact with 17β-estradiol (E2), an endogenous female sex hormone. It has been reported that E2 can significantly reduce the blood levels of low-density lipoprotein,

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25

Sapino, Anna, Luigia Macri, Patrizia Gugliotta, et al. "Immunophenotypic properties and estrogen dependency of budding cell structures in the developing mouse mammary gland." Differentiation 55, no. 1 (1993): 13–18. http://dx.doi.org/10.1111/j.1432-0436.1993.tb00028.x.

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26

Madauss, Kevin P., Eugene T. Grygielko, Su-Jun Deng, et al. "A Structural and in Vitro Characterization of Asoprisnil: A Selective Progesterone Receptor Modulator." Molecular Endocrinology 21, no. 5 (2007): 1066–81. http://dx.doi.org/10.1210/me.2006-0524.

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Abstract Selective progesterone receptor modulators (SPRMs) have been suggested as therapeutic agents for treatment of gynecological disorders. One such SPRM, asoprisnil, was recently in clinical trials for treatment of uterine fibroids and endometriosis. We present the crystal structures of progesterone receptor (PR) ligand binding domain complexed with asoprisnil and the corepressors nuclear receptor corepressor (NCoR) and SMRT. This is the first report of steroid nuclear receptor crystal structures with ligand and corepressors. These structures show PR in a different conformation than PR co

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27

Kanamori, Hiroshi, Robin E. Dodson, and David J. Shapiro. "In Vitro Genetic Analysis of the RNA Binding Site of Vigilin, a Multi-KH-Domain Protein." Molecular and Cellular Biology 18, no. 7 (1998): 3991–4003. http://dx.doi.org/10.1128/mcb.18.7.3991.

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ABSTRACT The function(s) and RNA binding properties of vigilin, a ubiquitous protein with 14 KH domains, remain largely obscure. We recently showed that vigilin is the estrogen-inducible protein in polysome extracts which binds specifically to a segment of the 3′ untranslated region (UTR) of estrogen-stabilized vitellogenin mRNA. In order to identify consensus mRNA sequences and structures important in binding of vigilin to RNA, before vigilin was purified, we developed a modified in vitro genetic selection protocol. We subsequently validated our selection procedure, which employed crude polys

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28

Massimiani, Micol, Valentina Lacconi, Fabio La Civita, Carlo Ticconi, Rocco Rago, and Luisa Campagnolo. "Molecular Signaling Regulating Endometrium–Blastocyst Crosstalk." International Journal of Molecular Sciences 21, no. 1 (2019): 23. http://dx.doi.org/10.3390/ijms21010023.

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Implantation of the embryo into the uterine endometrium is one of the most finely-regulated processes that leads to the establishment of a successful pregnancy. A plethora of factors are released in a time-specific fashion to synchronize the differentiation program of both the embryo and the endometrium. Indeed, blastocyst implantation in the uterus occurs in a limited time frame called the “window of implantation” (WOI), during which the maternal endometrium undergoes dramatic changes, collectively called “decidualization”. Decidualization is guided not just by maternal factors (e.g., estroge

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Kobayashi, Ami, Kotaro Azuma, Kazuhiro Ikeda, and Satoshi Inoue. "Mechanisms Underlying the Regulation of Mitochondrial Respiratory Chain Complexes by Nuclear Steroid Receptors." International Journal of Molecular Sciences 21, no. 18 (2020): 6683. http://dx.doi.org/10.3390/ijms21186683.

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Mitochondrial respiratory chain complexes play important roles in energy production via oxidative phosphorylation (OXPHOS) to drive various biochemical processes in eukaryotic cells. These processes require coordination with other cell organelles, especially the nucleus. Factors encoded by both nuclear and mitochondrial DNA are involved in the formation of active respiratory chain complexes and ‘supercomplexes’, the higher-order structures comprising several respiratory chain complexes. Various nuclear hormone receptors are involved in the regulation of OXPHOS-related genes. In this article, w

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Anstead, Gregory M., Scott R. Wilson, and John A. Katzenellenbogen. "2-Arylindenes and 2-arylindenones: molecular structures and considerations in the binding orientation of unsymmetrical nonsteroidal ligands to the estrogen receptor." Journal of Medicinal Chemistry 32, no. 9 (1989): 2163–71. http://dx.doi.org/10.1021/jm00129a024.

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Aditama, Agnis P. R., Burhan Ma’arif, Hening Laswati, and Mangestuti Agil. "In vitro and in silico analysis of phytochemical compounds of 96% ethanol extract of semanggi (Marsilea crenata Presl.) leaves as a bone formation agent." Journal of Basic and Clinical Physiology and Pharmacology 32, no. 4 (2021): 881–87. http://dx.doi.org/10.1515/jbcpp-2020-0515.

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Abstract Objectives Osteoporosis is the result of an imbalance in the rate of bone resorption and bone formation due to a decrease in estrogen. Phytoestrogens are plant compounds with structures and functions similar to estrogen. Phytoestrogens that bind to estrogen receptors in bone cells are able to modulate bone formation. Semanggi (Marsilea crenata Presl.) is a plant that contains phytoestrogens. The purpose of this study was to observe the expression of osteocalcin and predict the content of extract phytoestrogens through a computer simulation study to study the bone formation activity of

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Li, Jiazhong, and Paola Gramatica. "The importance of molecular structures, endpoints’ values, and predictivity parameters in QSAR research: QSAR analysis of a series of estrogen receptor binders." Molecular Diversity 14, no. 4 (2009): 687–96. http://dx.doi.org/10.1007/s11030-009-9212-2.

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Lawal, Hadiza Abdulrahman, Adamu Uzairu, and Sani Uba. "QSAR, molecular docking, design, and pharmacokinetic analysis of 2-(4-fluorophenyl) imidazol-5-ones as anti-breast cancer drug compounds against MCF-7 cell line." Journal of Bioenergetics and Biomembranes 52, no. 6 (2020): 475–94. http://dx.doi.org/10.1007/s10863-020-09858-0.

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AbstractThe anti-proliferative activities of Novel series of 2-(4-fluorophenyl) imidazol-5-ones against MCF-7 breast cancer cell line were explored via in-slico studies which includes Quantitative structure–activity relationship QSAR, molecular docking studies, designing new compounds, and analyzing the pharmacokinetics properties of the designed compounds. From the QSAR analysis, model number one emerged the best as seen from the arithmetic assessments of (R2) = 0.6981, (R2adj) = 0.6433, (Q2) = 0.5460 and (R2pred) of 0.5357. Model number one was used in designing new derivative compounds, wit

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Cheung, Edwin, Alla S. Zarifyan та W. Lee Kraus. "Histone H1 Represses Estrogen Receptor α Transcriptional Activity by Selectively Inhibiting Receptor-Mediated Transcription Initiation". Molecular and Cellular Biology 22, № 8 (2002): 2463–71. http://dx.doi.org/10.1128/mcb.22.8.2463-2471.2002.

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ABSTRACT Chromatin is the physiological template for many nuclear processes in eukaryotes, including transcription by RNA polymerase II. In vivo, chromatin is assembled from genomic DNA, core histones, linker histones such as histone H1, and nonhistone chromatin-associated proteins. Histone H1 is thought to act as a general repressor of transcription by promoting the compaction of chromatin into higher-order structures. We have used a biochemical approach, including an in vitro chromatin assembly and transcription system, to examine the effects of histone H1 on estrogen receptor α (ERα)-mediat

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Zhang, Birong, James R. Kiefer, Robert A. Blake, et al. "Unexpected equivalent potency of a constrained chromene enantiomeric pair rationalized by co-crystal structures in complex with estrogen receptor alpha." Bioorganic & Medicinal Chemistry Letters 29, no. 7 (2019): 905–11. http://dx.doi.org/10.1016/j.bmcl.2019.01.036.

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Park, Sujin, Go Eun Bae, Jiyoung Kim, and Hyun-Soo Kim. "Mesonephric-like Differentiation of Endometrial Endometrioid Carcinoma: Clinicopathological and Molecular Characteristics Distinct from Those of Uterine Mesonephric-like Adenocarcinoma." Diagnostics 11, no. 8 (2021): 1450. http://dx.doi.org/10.3390/diagnostics11081450.

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When diagnosing endometrial carcinoma cases, we encountered histological features that strikingly resembled uterine mesonephric-like adenocarcinoma (MLA), but the differential diagnosis remained challenging after performing immunostaining. Considering the aggressive biological behavior and poor prognosis of uterine MLA, we believe that the accurate recognition of mesonephric-like differentiation (MLD) is important in the diagnosis of endometrial carcinoma. We aimed to investigate the clinicopathological and molecular characteristics of such cases and compared them with those of uterine MLAs. F

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Wang, Liping, William J. Zuercher, Thomas G. Consler та ін. "X-ray Crystal Structures of the Estrogen-related Receptor-γ Ligand Binding Domain in Three Functional States Reveal the Molecular Basis of Small Molecule Regulation". Journal of Biological Chemistry 281, № 49 (2006): 37773–81. http://dx.doi.org/10.1074/jbc.m608410200.

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Niklaus, Andrea L., and Jeffrey W. Pollard. "Mining the Mouse Transcriptome of Receptive Endometrium Reveals Distinct Molecular Signatures for the Luminal and Glandular Epithelium." Endocrinology 147, no. 7 (2006): 3375–90. http://dx.doi.org/10.1210/en.2005-1665.

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Epithelia coat most tissues where they sense and respond to the environment and participate in innate immune responses. In the adult mouse uterus, columnar epithelium lines the central lumen and the glands that penetrate the underlying stroma. A nidatory surge of estrogen causes differentiation of the luminal epithelium to the receptive state that permits blastocyst attachment and allows subsequent implantation. Here, using laser-capture microdissection to isolate the luminal and glandular epithelia separately, we have profiled gene expression 2 h before embryo attachment to determine whether

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Stortz, Martin, Diego M. Presman, Adali Pecci, and Valeria Levi. "Phasing the intranuclear organization of steroid hormone receptors." Biochemical Journal 478, no. 2 (2021): 443–61. http://dx.doi.org/10.1042/bcj20200883.

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Steroid receptors (SRs) encompass a family of transcription factors that regulate the expression of thousands of genes upon binding to steroid hormones and include the glucocorticoid, androgen, progesterone, estrogen and mineralocorticoid receptors. SRs control key physiological and pathological processes, thus becoming relevant drug targets. As with many other nuclear proteins, hormone-activated SRs concentrate in multiple discrete foci within the cell nucleus. Even though these foci were first observed ∼25 years ago, their exact structure and function remained elusive. In the last years, new

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Yu, Xinzhe, and Ping Yi. "Structural Insights of Transcriptionally Active, Full-Length Androgen Receptor Coactivator Complexes." Journal of the Endocrine Society 5, Supplement_1 (2021): A817. http://dx.doi.org/10.1210/jendso/bvab048.1665.

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Abstract Steroid hormone receptors activate gene transcription by binding specific DNA sequences and recruiting coactivators to initiate transcription of their target genes. For most nuclear hormone receptors (NRs), the ligand-dependent activation function domain-2 (AF-2), residing in the C-terminal ligand binding domain (LBD), is a primary contributor to the NR transcriptional activity. In contrast to other steroid receptors such as estrogen receptor-α (ERα), the transcriptional activation function of androgen receptor (AR) is thought to be largely dependent on its ligand-independent activati

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Kym, Philip R., Gregory M. Anstead, Kevin G. Pinney, Scott R. Wilson, and John A. Katzenellenbogen. "Molecular structures, conformational analysis, and preferential modes of binding of 3-aroyl-2-arylbenzo[b]thiophene estrogen receptor ligands: LY117018 and aryl azide photoaffinity labeling analogs." Journal of Medicinal Chemistry 36, no. 24 (1993): 3910–22. http://dx.doi.org/10.1021/jm00076a020.

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Mazurek, Anna Helena, Łukasz Szeleszczuk, Thomas Simonson, and Dariusz Maciej Pisklak. "Application of Various Molecular Modelling Methods in the Study of Estrogens and Xenoestrogens." International Journal of Molecular Sciences 21, no. 17 (2020): 6411. http://dx.doi.org/10.3390/ijms21176411.

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In this review, applications of various molecular modelling methods in the study of estrogens and xenoestrogens are summarized. Selected biomolecules that are the most commonly chosen as molecular modelling objects in this field are presented. In most of the reviewed works, ligand docking using solely force field methods was performed, employing various molecular targets involved in metabolism and action of estrogens. Other molecular modelling methods such as molecular dynamics and combined quantum mechanics with molecular mechanics have also been successfully used to predict the properties of

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Higa, M., T. Kitahashi, Y. Sasaki, H. Okada, and H. Ando. "Distinct promoter sequences of two precursor genes for salmon gonadotropin-releasing hormone in masu salmon." Journal of Molecular Endocrinology 19, no. 2 (1997): 149–61. http://dx.doi.org/10.1677/jme.0.0190149.

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Two types of genes encode salmon gonadotropin-releasing hormone (sGnRH), which is thought to act on both sexual maturation and reproductive behavior, in salmonids. We characterized the two sGnRH genes (sGnRH-I and -II) and their upstream regions in masu salmon, Oncorhynchus masou, since such information is a prerequisite for molecular approaches to salmon reproduction. The two genes have similar exon-intron structures composed of four exons and three introns. Sequence analyses of the two genes showed that coding regions are highly conserved, but upstream regions are distinctively divergent. In

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Houshdaran, Sahar, Joseph C. Chen, Júlia Vallvé-Juanico, et al. "Progestins Related to Progesterone and Testosterone Elicit Divergent Human Endometrial Transcriptomes and Biofunctions." International Journal of Molecular Sciences 21, no. 7 (2020): 2625. http://dx.doi.org/10.3390/ijms21072625.

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Progestins are widely used for the treatment of gynecologic disorders and alone, or combined with an estrogen, are used as contraceptives. While their potencies, efficacies and side effects vary due to differences in structures, doses and routes of administration, little is known about their effects on the endometrial transcriptome in the presence or absence of estrogen. Herein, we assessed the transcriptome and pathways induced by progesterone (P4) and the three most commonly used synthetic progestins, medroxyprogesterone acetate (MPA), levonorgestrel (LNG), and norethindrone acetate (NETA),

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Jin, Jianshi, Teng-fei Lian, Xiaoliang Xie, and Xiao-Dong Su. "Mapping protein binding stability on nucleosomal DNA by single-molecule approach." Acta Crystallographica Section A Foundations and Advances 70, a1 (2014): C111. http://dx.doi.org/10.1107/s205327331409888x.

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The conformation of nucleosomal DNA is significantly different from that of a canonical B-form double stranded DNA (dsDNA), and is generally regarded to be less flexible and less accessible than free dsDNA due to the tight association of histone cores. Previous studies have demonstrated that the key mechanism involved in nucleosomal DNA-protein interaction is the protein accessibility to the DNA binding site. In this work, we used single molecule assays to measure the stability of two transcriptional factors (glucocorticoid receptor DNA binding domain (GRDBD) and estrogen receptor DNA-binding

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Sari, Ramazan, Meric A. Altinoz, Eylem Burcu Kahraman Ozlu, et al. "Treatment Strategies for Dopamine Agonist-Resistant and Aggressive Prolactinomas: A Comprehensive Analysis of the Literature." Hormone and Metabolic Research 53, no. 07 (2021): 413–24. http://dx.doi.org/10.1055/a-1525-2131.

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AbstractDespite most of the prolactinomas can be treated with endocrine therapy and/or surgery, a significant percentage of these tumors can be resistant to endocrine treatments and/or recur with prominent invasion into the surrounding anatomical structures. Hence, clinical, pathological, and molecular definitions of aggressive prolactinomas are important to guide for classical and novel treatment modalities. In this review, we aimed to define molecular endocrinological features of dopamine agonist-resistant and aggressive prolactinomas for designing future multimodality treatments. Besides su

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PUCA, G. A., N. MEDICI, I. ARMETTA, V. NIGRO, B. MONCHARMONT, and A. M. MOLINARI. "Interaction between Estrogen Receptor and Subcellular Structures of Target Cells: Nuclear Localization of Unoccupied Receptor and Its Modification Induced by Estradiol." Annals of the New York Academy of Sciences 464, no. 1 Endocrinology (1986): 168–89. http://dx.doi.org/10.1111/j.1749-6632.1986.tb16003.x.

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Baroi, Sudipta, Achintya Saha, Ritesh Bachar, and Sitesh C. Bachar. "Cannabinoid as Potential Aromatase Inhibitor Through Molecular Modeling and Screening for Anti-Cancer Activity." Dhaka University Journal of Pharmaceutical Sciences 19, no. 1 (2020): 47–58. http://dx.doi.org/10.3329/dujps.v19i1.47818.

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Inhibition of aromatase (CYTP450), a key enzyme in the estrogen biosynthesis, could result in regression of estrogen-dependent tumors and even prevent the promotion of breast cancer. The present research has been designed for searching a potent chemical moiety from natural sources to inhibit aromatase enzyme, the overfunctionality of which causes the breast cancer. Cannabis sativa contains a very much promising group of cannabinoids with more than 66 compounds with reported anticancer property and for the search of a target specific potent aromatase inhibitor, 61 cannabinoids from C. sativa we

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Sudhakaran, P. R., M. Ambili, and Susy Philip. "Matrix Metalloproteinase in Mammary Gland Remodeling-Modulation by Glycosaminoglycans." Bioscience Reports 19, no. 5 (1999): 485–90. http://dx.doi.org/10.1023/a:1020276609159.

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Mammary gland which undergoes proliferation, differentiation and involution in adult life is a useful model system to study the role of extracellular matrix (ECM) in regulating tissue specific functions. The involution that follows weaning results in the suppression of casein gene expression, collapse of alveolar structures and degradation of basement membrane as evidenced by biochemical analysis of matrix components like proteoglycans and collagen. Differential expression of three different MMPs viz. 130 K, 68 K and 60 K with varying specificity to Col IV of basement membrane and Col I of str

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Croft, Daniel R., and Michael F. Olson. "The Rho GTPase Effector ROCK Regulates Cyclin A, Cyclin D1, and p27Kip1 Levels by Distinct Mechanisms." Molecular and Cellular Biology 26, no. 12 (2006): 4612–27. http://dx.doi.org/10.1128/mcb.02061-05.

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ABSTRACT The members of the Rho GTPase family are well known for their regulation of actin cytoskeletal structures. In addition, they influence progression through the cell cycle. The RhoA and RhoC proteins regulate numerous effector proteins, with a central and vital signaling role mediated by the ROCK I and ROCK II serine/threonine kinases. The requirement for ROCK function in the proliferation of numerous cell types has been revealed by studies utilizing ROCK-selective inhibitors such as Y-27632. However, the mechanisms by which ROCK signaling promotes cell cycle progression have not been t

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