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Using gene-targeting techniques, transgenic, knock-out (KO) mice, homozygous for the disrupted estrogen receptor α (αERKO) and β gene (βERKO) have been produced. Estrogen receptor (ER) β expression does not appear to be dependent on ER α expression. Progesterone receptor (PR) mRNA is detected in αERKO mice and appears to have both estrogen-independent and -dependent gene regulation. The phenotypic...
Selective estrogen receptor modulators (SERMs) appear to reduce the incidence of breast cancer in high-risk women. Five years of tamoxifen administration after the diagnosis of breast cancer results in a 50% reduction in the incidence of contralateral breast cancer. This reduction is maintained for 5 years after therapy is discontinued. The Study of Tamoxifen And Raloxifene (STAR), presently ongoing,...
The discovery of a second estrogen receptor, ER β, in 1996 introduced a new paradigm in our understanding of estrogen action. ER α predominates in the uterus and mammary gland, whereas ER β has significant roles in the central nervous, cardiovascular, and immune systems, urogenital tract, bone, kidney, and lung. ER β appears to be the only form expressed in the embryonal central nervous system. Photoestrogens...
Until 1986, our understanding of estrogen receptor (ER) action was based on information derived from in vitro biochemical analyses and in vivo correlations. With the cloning of the human ER cDNA, the reconstitution of ER responsive transcription units in heterologous cells has permitted the genetic dissection of the ER signal transduction pathway. The recent discovery of ER β and a multitude of adaptor...
The objective of this literature review is to familiarize the reader with the clinical data on selective estrogen receptor modulators (SERMs) and antiestrogens currently in use in the US, excluding data on breast effects. Four compounds in the SERM and antiestrogen families are presently in clinical use in the US: clomiphene (CC), tamoxifen (TAM), toremifene (TOR), and raloxifene (RLX). The clinical...
The progesterone receptor (PR), as a member of the nuclear receptor superfamily of ligand-dependent transcription factors, activates gene transcription through binding to specific palindromic progesterone response elements (PRE) in the promoter region of progestin-responsive genes. The progesterone antagonists ZK98299 (Onapristone) and RU 486 (Mifepristone) inhibit the transcriptional activity of...
Progesterone is essential to the establishment and maintenance of pregnancy. Compounds that inhibit the synthesis of progesterone, or antagonize progesterone action, have multiple effects including the induction of abortion, labor induction, contraception, and cervical ripening. They also may be used in the treatment of endometriosis, fibromyomata, meningiomas, Cushing syndrome, and glaucoma. Antiprogesterone...
Newer, nonsteroidal, orally active, tissue-selective progestins are being developed through a molecular approach to compound selection with human progesterone receptor (hPR) serving as the molecular target. The co-transfection and binding assays are used to test receptor selectivity and cross reactivity with a panel of receptors. Transcriptional products are used to further profile new progestin compounds...
Our current understanding of the steroid/thyroid superfamily of ligand-dependent nuclear transcription factors now involves specific domains for steroid ligand binding, receptor homo- and heterodimer formation, the association of transcription mediators or adaptors that activate, repress, or integrate competing influences, interaction with the hormone response element, transcription modulation based...
The intriguing biology of estrogens and progestins in their diverse target cells is determined by the structure of the hormonal ligand, the receptor subtype or isoform involved, the nature of the hormone-responsive gene promoter, and the character and balance of coactivators and corepressors that modulate the cellular response to the receptor-ligand complex. Estrogens regulate the growth, differentiation,...
Progesterone plays a central coordinate role in regulating reproductive events associated with the establishment and maintenance of pregnancy including ovulation, uterine and mammary gland development and tumorigenesis, and neurobehavioral expression associated with sexual responsiveness. The effects of progesterone are mediated by two receptor proteins (PR), termed A and B, that arise from a single...
Aromatase enzyme is the product of the CYP19 gene. Human aromatase deficiency is a rare disorder and is usually caused by single base-pair changes resulting in amino acid substitution or premature stop codons. In most cases, the affected mother presents with virilization in the third trimester of pregnancy. Affected female newborns have pseudohemaphrodism with clitoromegaly and hypospadias. The cause...
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