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Selective ERĪ² Agonists
Estrogen receptor beta (ERĪ²) also known as NR3A2 (nuclear receptor subfamily 3, group A, member 2) is one of two main types of estrogen receptorāa nuclear receptor which is activated by the sex hormone estrogen. In humans ERĪ² is encoded by the ''ESR2'' gene. Function ERĪ² is a member of the family of estrogen receptors and the superfamily of nuclear receptor transcription factors. The gene product contains an N-terminal DNA binding domain and C-terminal ligand binding domain and is localized to the nucleus, cytoplasm, and mitochondria. Upon binding to 17-Ī²-estradiol, estriol or related ligands, the encoded protein forms homo-dimers or hetero-dimers with estrogen receptor Ī± that interact with specific DNA sequences to activate transcription. Some isoforms dominantly inhibit the activity of other estrogen receptor family members. Several alternatively spliced transcript variants of this gene have been described, but the full-length nature of some of these variants ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Estrogen Receptor
Estrogen receptors (ERs) are proteins found in cell (biology), cells that function as receptor (biochemistry), receptors for the hormone estrogen (17Ī²-estradiol). There are two main classes of ERs. The first includes the intracellular estrogen receptors, namely ERĪ± and ERĪ², which belong to the nuclear receptor family. The second class consists of membrane estrogen receptors (mERs), such as GPER (GPR30), ER-X, and Gq-mER, Gq-mER, which are primarily G protein-coupled receptors. This article focuses on the nuclear estrogen receptors (ERĪ± and ERĪ²). Upon activation by estrogen, intracellular ERs undergo protein targeting, translocation to the nucleus where they bind to specific DNA sequences. As DNA-binding transcription factors, they regulate the activity of various genes. However, ERs also exhibit functions that are independent of their DNA-binding capacity. These non-genomic actions contribute to the diverse effects of estrogen signaling in cells. Estrogen receptors (ERs) b ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
ERB-041
Prinaberel (INN, USAN) (developmental code names ERB-041, WAY-202041) is a synthetic, nonsteroidal, and highly selective agonist of the ERĪ² subtype of the estrogen receptor. It is used in scientific research to elucidate the role of the ERĪ² receptor. Studies have indicated that selective ERĪ² agonists like prinaberel could be useful in the clinical treatment of a variety of medical conditions including inflammatory bowel disease, rheumatoid arthritis, endometriosis, and sepsis. Accordingly, prinaberel either was or still is under investigation by Wyeth for the treatment of some of these conditions. See also * Diarylpropionitrile * ERB-196 * Erteberel * WAY-200070 WAY-200070 is a synthetic compound, synthetic, nonsteroidal, highly binding selectivity, selective agonist of ERĪ². It possesses 68-fold selectivity for ERĪ² over ERĪ± (EC50, EC50 = 2 nM and 155 nM, respectively). WAY-200070 has been found to enh ... * WAY-214156 References External links Prinaberel - AdisInsi ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Cell Proliferation
Cell proliferation is the process by which ''a cell grows and divides to produce two daughter cells''. Cell proliferation leads to an exponential increase in cell number and is therefore a rapid mechanism of tissue growth. Cell proliferation requires both cell growth and cell division to occur at the same time, such that the average size of cells remains constant in the population. Cell division can occur without cell growth, producing many progressively smaller cells (as in cleavage of the zygote), while cell growth can occur without cell division to produce a single larger cell (as in growth of neurons). Thus, cell proliferation is not synonymous with either cell growth or cell division, despite these terms sometimes being used interchangeably. Stem cells undergo cell proliferation to produce proliferating "transit amplifying" daughter cells that later differentiate to construct tissues during normal development and tissue growth, during tissue regeneration after da ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Diarylpropionitrile
Diarylpropionitrile (DPN), also known as 2,3-bis(p-hydroxyphenyl)propionitrile (2,3-BHPPN), is a synthetic, nonsteroidal, and highly selective agonist of ERĪ² ( IC50 = 15 nM) that is used widely in scientific research to study the function of this receptor. It is 70-fold more selective for ERĪ² over ERĪ±, and has 100-fold lower affinity for GPER (GPR30) relative to estradiol. DPN produces antidepressant- and anxiolytic-like effects in animals via activation of the endogenous oxytocin system. First reported in 2001, DPN was the first selective ERĪ² agonist to be discovered, and was followed by prinaberel (ERB-041, WAY-202041), WAY-200070, and 8Ī²-VE2 in 2004, ERB-196 (WAY-202196) in 2005, and certain phytoestrogens like liquiritigenin and nyasol (''cis''-hinokiresinol) since 2007. DPN is a racemic mixture of two enantiomers, (R)-DPN and (S)-DPN. Relative to (R)-DPN, (S)-DPN has between 3- and 7-fold higher affinity for ERĪ² and appears to have higher intrinsic activity in activat ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Corpora Lutea
The corpus luteum (Latin for "yellow body"; : corpora lutea) is a temporary endocrine structure in female ovaries involved in the production of relatively high levels of progesterone, and moderate levels of estradiol, and inhibin A. It is the remains of the ovarian follicle that has released a mature ovum during a previous ovulation. The corpus luteum is colored as a result of concentrating carotenoids (including lutein) from the diet and secretes a moderate amount of estrogen that inhibits further release of gonadotropin-releasing hormone (GnRH) and thus secretion of luteinizing hormone (LH) and follicle-stimulating hormone (FSH). A new corpus luteum develops with each menstrual cycle. Development and structure The corpus luteum develops from an ovarian follicle during the luteal phase of the menstrual cycle or oestrous cycle, following the release of a secondary oocyte from the follicle during ovulation. The follicle first forms a corpus hemorrhagicum before it becomes a corpu ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Progesterone
Progesterone (; P4) is an endogenous steroid and progestogen sex hormone involved in the menstrual cycle, pregnancy, and embryogenesis of humans and other species. It belongs to a group of steroid hormones called the progestogens and is the major progestogen in the body. Progesterone has a variety of important functions in the body. It is also a crucial metabolic intermediate in the production of other endogenous steroids, including the sex hormones and the corticosteroids, and plays an important role in brain function as a neurosteroid. In addition to its role as a natural hormone, progesterone is also used as a medication, such as in combination with estrogen for contraception, to reduce the risk of Uterine cancer, uterine or cervical cancer, in hormone replacement therapy, and in feminizing hormone therapy. It was first prescribed in 1934. Biological activity Progesterone is the most important progestogen in the body. As a potent agonist of the progesterone receptor, nu ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Mastopathy
Breast diseases make up a number of conditions. The most common symptoms are a breast mass, breast pain, and nipple discharge. A majority of breast diseases are noncancerous. Although breast disease may be benign, or non-life threatening there remains an associated risk with potentially a higher risk of developing breast cancer later on. Tumor A breast tumor is an abnormal mass of tissue in the breast as a result of neoplasia. A breast neoplasm may be benign, as in fibroadenoma, or it may be malignant, in which case it is termed breast cancer. Either case commonly presents as a breast lump. Approximately 7% of breast lumps are fibroadenomas and 10% are breast cancer, the rest being other benign conditions or no disease.Page 739 in: 8th edition. Phyllodes tumor is a fibroepithelial tumor which can be benign, borderline or malignant. Breast cancer Breast cancer is cancer of the breast tissues, most commonly arising from the milk ducts. Worldwide, breast cancer is the leading ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Postmenopausal
Menopause, also known as the climacteric, is the time when menstrual periods permanently stop, marking the end of the reproductive stage for the female human. It typically occurs between the ages of 45 and 55, although the exact timing can vary. Menopause is usually a natural change related to a decrease in circulating blood estrogen levels. It can occur earlier in those who smoke tobacco. Other causes include surgery that removes both ovaries, some types of chemotherapy, or anything that leads to a decrease in hormone levels. At the physiological level, menopause happens because of a decrease in the ovaries' production of the hormones estrogen and progesterone. While typically not needed, measuring hormone levels in the blood or urine can confirm a diagnosis. Menopause is the opposite of menarche, the time when periods start. In the years before menopause, a woman's periods typically become irregular, which means that periods may be longer or shorter in duration, or be ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Cystic Mammary Disease
Fibrocystic breast changes is a condition of the breasts where there may be pain, breast cysts, and breast masses. The breasts may be described as "lumpy" or "doughy". Symptoms may worsen during certain parts of the menstrual cycle due to hormonal stimulation. These are normal breast changes, not associated with cancer. Risk factors include an early age at first menstrual period and either having children at a late age or not at all. It is not a disease but represents normal breast changes. Diagnosis involves ruling out breast cancer. Fibrocystic changes include fibroadenomas, fibrosis, papillomas of the breast, and apocrine-type metaplasia. Management may involve education about the condition, using a well fitting bra, and pain medication, if needed. Occasionally danazol or tamoxifen may be used for pain. It is estimated that up to 60% of women are affected, most commonly between the ages of 30 and 50 years. Signs and symptoms The changes in fibrocystic breast disease are ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Epithelium
Epithelium or epithelial tissue is a thin, continuous, protective layer of cells with little extracellular matrix. An example is the epidermis, the outermost layer of the skin. Epithelial ( mesothelial) tissues line the outer surfaces of many internal organs, the corresponding inner surfaces of body cavities, and the inner surfaces of blood vessels. Epithelial tissue is one of the four basic types of animal tissue, along with connective tissue, muscle tissue and nervous tissue. These tissues also lack blood or lymph supply. The tissue is supplied by nerves. There are three principal shapes of epithelial cell: squamous (scaly), columnar, and cuboidal. These can be arranged in a singular layer of cells as simple epithelium, either simple squamous, simple columnar, or simple cuboidal, or in layers of two or more cells deep as stratified (layered), or ''compound'', either squamous, columnar or cuboidal. In some tissues, a layer of columnar cells may appear to be stratified d ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Pregnancy
Pregnancy is the time during which one or more offspring gestation, gestates inside a woman's uterus. A multiple birth, multiple pregnancy involves more than one offspring, such as with twins. Conception (biology), Conception usually occurs following sexual intercourse, vaginal intercourse, but can also occur through assisted reproductive technology procedures. A pregnancy may end in a Live birth (human), live birth, a miscarriage, an Abortion#Induced, induced abortion, or a stillbirth. Childbirth typically occurs around 40 weeks from the start of the Menstruation#Onset and frequency, last menstrual period (LMP), a span known as the Gestational age (obstetrics), ''gestational age''; this is just over nine months. Counting by Human fertilization#Fertilization age, ''fertilization age'', the length is about 38 weeks. Implantation (embryology), Implantation occurs on average 8–9 days after Human fertilization, fertilization. An ''embryo'' is the term for the deve ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Cell Differentiation
Cellular differentiation is the process in which a stem cell changes from one type to a differentiated one. Usually, the cell changes to a more specialized type. Differentiation happens multiple times during the development of a multicellular organism as it changes from a simple zygote to a complex system of Tissue (biology), tissues and cell types. Differentiation continues in adulthood as adult stem cells divide and create fully differentiated Cell division, daughter cells during tissue repair and during normal cell turnover. Some differentiation occurs in response to antigen exposure. Differentiation dramatically changes a cell's size, shape, membrane potential, metabolism, metabolic activity, and responsiveness to signals. These changes are largely due to highly controlled modifications in gene expression and are the study of epigenetics. With a few exceptions, cellular differentiation almost never involves a change in the DNA sequence itself. Metabolic composition, however ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
