GPER Agonists
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GPER Agonists
G protein-coupled estrogen receptor 1 (GPER), also known as G protein-coupled receptor 30 (GPR30), is a protein that in humans is encoded by the ''GPER'' gene. GPER binds to and is activated by the female sex hormone estradiol and is responsible for some of the rapid effects that estradiol has on cells. Discovery The classical estrogen receptors first characterized in 1958 are water-soluble proteins located in the interior of cells that are activated by estrogenenic hormones such as estradiol and several of its metabolites such as estrone or estriol. These proteins belong to the nuclear hormone receptor class of transcription factors that regulate gene transcription. Since it takes time for genes to be transcribed into RNA and translated into protein, the effects of estrogens binding to these classical estrogen receptors is delayed. However, estrogens are also known to have effects that are too fast to be caused by regulation of gene transcription. In 2005, it was discovered ...
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Protein
Proteins are large biomolecules and macromolecules that comprise one or more long chains of amino acid residues. Proteins perform a vast array of functions within organisms, including catalysing metabolic reactions, DNA replication, responding to stimuli, providing structure to cells and organisms, and transporting molecules from one location to another. Proteins differ from one another primarily in their sequence of amino acids, which is dictated by the nucleotide sequence of their genes, and which usually results in protein folding into a specific 3D structure that determines its activity. A linear chain of amino acid residues is called a polypeptide. A protein contains at least one long polypeptide. Short polypeptides, containing less than 20–30 residues, are rarely considered to be proteins and are commonly called peptides. The individual amino acid residues are bonded together by peptide bonds and adjacent amino acid residues. The sequence of amino acid resid ...
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Testosterone
Testosterone is the primary sex hormone and anabolic steroid in males. In humans, testosterone plays a key role in the development of male reproductive tissues such as testes and prostate, as well as promoting secondary sexual characteristics such as increased muscle and bone mass, and the growth of body hair. In addition, testosterone in both sexes is involved in health and well-being, including moods, behaviour, and in the prevention of osteoporosis. Insufficient levels of testosterone in men may lead to abnormalities including frailty and bone loss. Testosterone is a steroid from the androstane class containing a ketone and a hydroxyl group at positions three and seventeen respectively. It is biosynthesized in several steps from cholesterol and is converted in the liver to inactive metabolites. It exerts its action through binding to and activation of the androgen receptor. In humans and most other vertebrates, testosterone is secreted primarily by the testicles o ...
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Atrazine
Atrazine is a chlorinated herbicide of the triazine class. It is used to prevent pre-emergence broadleaf weeds in crops such as maize (corn), soybean and sugarcane and on turf, such as golf courses and residential lawns. Atrazine's primary manufacturer is Syngenta and it is one of the most widely used herbicides in the United States, Canadian, and Australian agriculture. Its use was banned in the European Union in 2004, when the EU found groundwater levels exceeding the limits set by regulators, and Syngenta could not show that this could be prevented nor that these levels were safe.European Commission.2004/248/EC: Commission Decision of 10 March 2004 concerning the non-inclusion of atrazine in Annex I to Council Directive 91/414/EEC and the withdrawal of authorisations for plant protection products containing this active substance (Text with EEA relevance) (notified under document number C(2004) 731)Decision 2004/248/EC - Official Journal L 078, Decision 2004/248/EC. March 16 ...
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Aldosterone
Aldosterone is the main mineralocorticoid steroid hormone produced by the zona glomerulosa of the adrenal cortex in the adrenal gland. It is essential for sodium conservation in the kidney, salivary glands, sweat glands, and colon. It plays a central role in the homeostatic regulation of blood pressure, plasma sodium (Na+), and potassium (K+) levels. It does so primarily by acting on the mineralocorticoid receptors in the distal tubules and collecting ducts of the nephron. It influences the reabsorption of sodium and excretion of potassium (from and into the tubular fluids, respectively) of the kidney, thereby indirectly influencing water retention or loss, blood pressure, and blood volume.Marieb Human Anatomy & Physiology 9th edition, chapter:16, page:629, question number:14 When dysregulated, aldosterone is pathogenic and contributes to the development and progression of cardiovascular and kidney disease. Aldosterone has exactly the opposite function of the atrial n ...
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Afimoxifene
Afimoxifene, also known as 4-hydroxytamoxifen (4-OHT) and by its tentative brand name TamoGel, is a selective estrogen receptor modulator (SERM) of the triphenylethylene group and an active metabolite of tamoxifen. The drug is under development under the tentative brand name TamoGel as a topical gel for the treatment of hyperplasia of the breast. It has completed a phase II clinical trial for cyclical mastalgia, but further studies are required before afimoxifene can be approved for this indication and marketed. Afimoxifene is a SERM and hence acts as a tissue-selective agonist–antagonist of the estrogen receptors ERα and ERβ with mixed estrogenic and antiestrogenic activity depending on the tissue. It is also an agonist of the G protein-coupled estrogen receptor (GPER) with relatively low affinity (100–1,000 nM, relative to 3–6 nM for estradiol Estradiol (E2), also spelled oestradiol, is an estrogen steroid hormone and the major female sex hormone ...
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2,2',5'-PCB-4-OH
The comma is a punctuation mark that appears in several variants in different languages. It has the same shape as an apostrophe or single closing quotation mark () in many typefaces, but it differs from them in being placed on the baseline of the text. Some typefaces render it as a small line, slightly curved or straight, but inclined from the vertical. Other fonts give it the appearance of a miniature filled-in figure on the baseline. The comma is used in many contexts and languages, mainly to separate parts of a sentence such as clauses, and items in lists mainly when there are three or more items listed. The word ''comma'' comes from the Greek (), which originally meant a cut-off piece, specifically in grammar, a short clause. A comma-shaped mark is used as a diacritic in several writing systems and is considered distinct from the cedilla. In Byzantine and modern copies of Ancient Greek, the " rough" and "smooth breathings" () appear above the letter. In Latvian, Ro ...
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2-Methoxyestradiol
2-Methoxyestradiol (2-ME2, 2-MeO-E2) is a natural metabolite of estradiol and 2-hydroxyestradiol (2-OHE2). It is specifically the 2- methyl ether of 2-hydroxyestradiol. 2-Methoxyestradiol prevents the formation of new blood vessels that tumors need in order to grow ( angiogenesis), hence it is an angiogenesis inhibitor. It also acts as a vasodilator and induces apoptosis in some cancer cell lines. 2-Methoxyestradiol is derived from estradiol, although it interacts poorly with the estrogen receptors (2,000-fold lower activational potency relative to estradiol). However, it retains activity as a high-affinity agonist of the G protein-coupled estrogen receptor (GPER) (10 nM, relative to 3–6 nM for estradiol). Clinical development 2-Methoxyestradiol was being developed as an experimental drug candidate with the tentative brand name Panzem. It has undergone Phase 1 clinical trials against breast cancer. A phase II trial of 18 advanced ovarian cancer patients rep ...
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G36 (drug)
G36 may refer to: * Beechcraft G36 Bonanza, an American aircraft * G36 Nanjing–Luoyang Expressway, in China * Glock 36, an Austrian pistol * Grumman G-36, a F4F Wildcat aircraft variant * Heckler & Koch G36 The Heckler & Koch G36 (Gewehr 36) is a 5.56×45mm assault rifle designed in the early 1990s by German weapons manufacturer Heckler & Koch as a replacement for the heavier 7.62×51mm G3 battle rifle. It was accepted into service with the ''B ..., a German assault rifle * Kami language (Tanzania) * Matsuchi Station, in Ehime Prefecture, Japan {{Letter-NumberCombDisambig ...
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G15 (drug)
The Group of 15 (G-15)Thofficial website adopts the "G-15" orthography (with a hyphen) in order to distinguish an abbreviated reference to this group -- contrasts with other similarly named entities. is an informal forum set up to foster cooperation and provide input for other international groups, such as the World Trade Organization (WTO) and the Group of Seven. It was established at the Ninth Non-Aligned Movement Summit Meeting in Belgrade, Yugoslavia, in September 1989, and is composed of countries from Latin America, Africa, and Asia with a common goal of enhanced growth and prosperity. The G-15 focuses on cooperation among developing countries in the areas of investment, trade, and technology. Membership has since expanded to 18 countries, but the name has remained unchanged. Chile, Iran and Kenya have since joined the Group of 15, whereas Yugoslavia is no longer part of the group; Peru, a founding member-state, decided to leave the G-15 in 2011. Structure and activities ...
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G-1 (drug)
G1, G01, G.I, G-1, or G One may refer to: Science and technology * G1 phase, in the cellular cycle * G1 regulatory sequence for the insulin gene * ATC code G01 ''Gynecological antiinfectives and antiseptics'', a subgroup of the Anatomical Therapeutic Chemical Classification System * Alkali metal, Group 1 of the periodic table * G1, an informal group of fossil bird eggs from the Gobi desert that were later named '' Gobioolithus minor'' Astronomy * Globular cluster Mayall II * YGKOW G1, a giant elliptical galaxy that lensed the Twin Quasar * G1 star, a subclass of G-class stars * G1, a cloud that passed by Sagittarius A* around 2001-2002 * g1, temporary designation of minor planet , a ''New Horizons'' flyby candidate Computing * Garbage-first collector, of the Oracle HotSpot Java virtual machine * G1, in ISO 2022 character sets, one of 4 groups of characters that may be swapped into the encoding space via control codes Cameras * Contax G1, a Rangefinder camera made by Con ...
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