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 intracellular, 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 ...
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Protein
Proteins are large biomolecules and macromolecules that comprise one or more long chains of amino acid residue (biochemistry), residues. Proteins perform a vast array of functions within organisms, including Enzyme catalysis, catalysing metabolic reactions, DNA replication, Cell signaling, responding to stimuli, providing Cytoskeleton, structure to cells and Fibrous protein, organisms, and Intracellular transport, transporting molecules from one location to another. Proteins differ from one another primarily in their sequence of amino acids, which is dictated by the Nucleic acid sequence, nucleotide sequence of their genes, and which usually results in protein folding into a specific Protein structure, 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 pep ...
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Testosterone
Testosterone is the primary male sex hormone and androgen in Male, males. In humans, testosterone plays a key role in the development of Male reproductive system, male reproductive tissues such as testicles and prostate, as well as promoting secondary sexual characteristics such as increased muscle and bone mass, and the growth of androgenic hair, body hair. It is associated with increased aggression, sex drive, Dominance hierarchy, dominance, courtship display, and a wide range of behavioral characteristics. In addition, testosterone in both sexes is involved in health and well-being, where it has a significant effect on overall mood, cognition, social and sexual behavior, metabolism and energy output, the cardiovascular system, and in the prevention of osteoporosis. Insufficient levels of testosterone in men may lead to abnormalities including frailty, accumulation of adipose fat tissue within the body, anxiety and depression, sexual performance issues, and bone loss. Excessiv ...
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Atrazine
Atrazine ( ) is a Organochlorine compound, 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, Decis ...
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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 nat ...
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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). In addition to its estrogenic and antiestrogenic activity, afimoxifene has been found to act as an antagoni ...
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2,2',5'-PCB-4-OH
The comma is a punctuation mark that appears in several variants in different languages. Some typefaces render it as a small line, slightly curved or straight, but inclined from the vertical; others give it the appearance of a miniature filled-in figure placed on the baseline. In many typefaces it is the same shape as an apostrophe or single closing quotation mark . 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, Romanian, and Livonian, the comma diacritic appears below the letter, a ...
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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 reported e ...
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G36 (drug)
G36 may refer to: * Heckler & Koch G36 The Heckler & Koch G36 (Gewehr 36) is an assault rifle An assault rifle is a select fire rifle that uses an intermediate cartridge, intermediate-rifle cartridge and a Magazine (firearms), detachable magazine.C. Taylor, ''The Fighting Ri ..., a German assault rifle * 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 * 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. Chile, Iran and Kenya have since joined the Group of 15, whereas Yugoslavia is no longer part of the group, and Peru, a founding member-state, decided to leave the G-15 in 2011. Membership thus has since expanded to 17 countries, but the forum's name remains unchanged. Structure and ...
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G-1 (drug)
Ganesha (G or G-1), also known as 2,5-dimethoxy-3,4-dimethylamphetamine, is a lesser-known psychedelic drug. It is also a substituted amphetamine. It was first synthesized by Alexander Shulgin. In his book ''PiHKAL'', the dosage range is listed as 24–32 mg. The drug is usually taken orally, although other routes such as rectally may also be used. Ganesha is synthesized from 2,5-dimethoxy-3,4-dimethylbenzaldehyde. Ganesha is the amphetamine analog of 2C-G. It is a particularly long lasting drug, with the duration listed in ''PiHKAL'' as being 18–24 hours, which might make it undesirable to some users. It is named after the Hindu deity, Ganesha. Very little is known about the dangers or toxicity of ganesha. Effects of ganesha include: * Strong closed-eye visuals * An increased appreciation of music * Powerful relaxation and tranquility Homologues G-3 2,5-Dimethoxy-3,4-(trimethylene)amphetamine: * Dosage: 12–18 mg * Duration: 8-12 h * Effects: Enhancement of read ...
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CCL18
Chemokine (C-C motif) ligand 18 (CCL18) is a small cytokine belonging to the CC chemokine family. The functions of CCL18 have been well studied in laboratory settings, however the physiological effects of the molecule in living organisms have been difficult to characterize because there is no similar protein in rodents that can be studied. The receptor for CCL18 has been identified in humans only recently, which will help scientists understand the molecule's role in the body. CCL18 is produced and secreted mainly by innate immune system, and has effects mainly on the adaptive immune system. It was previously known as Pulmonary and activation-regulated chemokine (PARC), dendritic cell (DC)-chemokine 1 (DC-CK1), alternative macrophage activation-associated CC chemokine-1 (AMAC-1), and macrophage inflammatory protein-4 (MIP-4). Gene and protein structure The gene of CCL18 is most similar to CCL3. CCL18 is located on chromosome 17, along with many other macrophage inflammatory p ...
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Nicotinamide
Nicotinamide (International nonproprietary name, INN, British Approved Name, BAN ) or niacinamide (United States Adopted Name, USAN ) is a form of vitamin B3, vitamin B3 found in food and used as a dietary supplement and medication. As a supplement, it is used oral administration, orally (swallowed by mouth) to prevent and treat pellagra (niacin deficiency). While nicotinic acid (niacin) may be used for this purpose, nicotinamide has the benefit of not causing Flushing (physiology), skin flushing. As a cream, it is used to treat acne, and has been observed in clinical studies to improve the appearance of aging skin by reducing hyperpigmentation and redness. It is a Water-soluble vitamins, water-soluble vitamin. Side effects are minimal. At high doses, liver problems may occur. Normal amounts are safe for use during pregnancy. Nicotinamide is in the vitamin B family of medications, specifically the vitamin B3 complex, vitamin B3 complex. It is an amide of nicotinic acid. Foods ...
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