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CYP27A1
CYP27A1 is a gene encoding a cytochrome P450 oxidase, and is commonly known as sterol 27-hydroxylase. This enzyme is located in many different tissues where it is found within the mitochondria. It is most prominently involved in the biosynthesis of bile acids. Function CYP27A1 participates in the degradation of cholesterol to bile acids in both the classic and acidic pathways. It is the initiating enzyme in the acidic pathway to bile acids, yielding oxysterols by introducing a hydroxyl group to the carbon at the 27 position in cholesterol. In the acidic pathway, it produces 27-hydroxycholesterol from cholesterol whereas in the classic or neutral pathway, it produces 3β-hydroxy-5-cholestenoic acid. While CYP27A1 is present in many different tissues, its function in these tissues is largely uncharacterized. In macrophages, 27-hydroxycholesterol generated by this enzyme may be helpful against the production of inflammatory factors associated with cardiovascular disease. C ...
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Cerebrotendineous Xanthomatosis
Cerebrotendinous xanthomatosis, also called cerebral cholesterosis, is an autosomal recessive form of xanthomatosis. It falls within a group of genetic disorders called the leukodystrophies. Presentation An inherited disorder associated with the deposition of a steroid known as cholestanol in the brain and other tissues and with elevated levels of cholesterol in plasma but with normal total cholesterol level; it is characterized by progressive cerebellar ataxia beginning after puberty and by juvenile cataracts, juvenile or infantile onset chronic diarrhea, childhood neurological deficit, and tendineous or tuberous xanthomas. Genetics CTX is associated with mutations in the CYP27A1 gene, located on chromosome 2q33-qter. The disorder is inherited in an autosomal recessive manner. This means the defective gene responsible for the disorder is located on an autosome (chromosome 2 is an autosome), and two copies of the defective gene (one inherited from each parent) are required in ...
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Bile Acid
Bile acids are steroid acids found predominantly in the bile of mammals and other vertebrates. Diverse bile acids are synthesized in the liver. Bile acids are conjugated with taurine or glycine residues to give anions called bile salts. Primary bile acids are those synthesized by the liver. Secondary bile acids result from bacterial actions in the colon. In humans, taurocholic acid and glycocholic acid (derivatives of cholic acid) and taurochenodeoxycholic acid and glycochenodeoxycholic acid (derivatives of chenodeoxycholic acid) are the major bile salts. They are roughly equal in concentration. The salts of their 7-alpha-dehydroxylated derivatives, deoxycholic acid and lithocholic acid, are also found, with derivatives of cholic, chenodeoxycholic and deoxycholic acids accounting for over 90% of human biliary bile acids. Bile acids comprise about 80% of the organic compounds in bile (others are phospholipids and cholesterol). An increased secretion of bile acids produ ...
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CYP27 Family
Cytochrome P450, family 27, also known as CYP27, is a Deuterostome cytochrome P450 monooxygenase family found in human genome. This family belongs to Mitochondrial clan ''CYP''s, which is located in the inner membrane of mitochondria(IMM). There are three members in the human genome, CYP27A1, CYP27B1 and CYP27C1, and an ortholog CYP27F1 in sea urchins, ''Strongylocentrotus purpuratus ''Strongylocentrotus purpuratus'', the purple sea urchin, lives along the eastern edge of the Pacific Ocean extending from Ensenada, Mexico, to British Columbia, Canada. This sea urchin species is deep purple in color, and lives in lower int ...''. References Cytochrome P450 {{genetics-stub ...
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Bicalutamide
Bicalutamide, sold under the brand name Casodex among others, is an antiandrogen medication that is primarily used to treat prostate cancer. It is typically used together with a gonadotropin-releasing hormone (GnRH) analogue or surgical removal of the testicles to treat advanced prostate cancer. To a lesser extent, it is used for early prostate cancer at a higher dosage as a monotherapy without castration. Bicalutamide is also used to treat excessive hair growth and scalp hair loss in women, as a component of feminizing hormone therapy for transgender women, to treat early puberty in boys, and to prevent overly long-lasting erections in men. It is taken by mouth. Common side effects in men include breast enlargement, breast tenderness, and hot flashes. Other side effects in men include feminization and sexual dysfunction. Some side effects like breast changes and feminization are minimal when combined with castration. While the medication appears to produce few ...
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Cytochrome P450 Oxidase
Cytochromes P450 (CYPs) are a superfamily of enzymes containing heme as a cofactor that functions as monooxygenases. In mammals, these proteins oxidize steroids, fatty acids, and xenobiotics, and are important for the clearance of various compounds, as well as for hormone synthesis and breakdown. In 1963, Estabrook, Cooper, and Rosenthal described the role of CYP as a catalyst in steroid hormone synthesis and drug metabolism. In plants, these proteins are important for the biosynthesis of defensive compounds, fatty acids, and hormones. CYP enzymes have been identified in all kingdoms of life: animals, plants, fungi, protists, bacteria, and archaea, as well as in viruses. However, they are not omnipresent; for example, they have not been found in ''Escherichia coli''. , more than 300,000 distinct CYP proteins are known. CYPs are, in general, the terminal oxidase enzymes in electron transfer chains, broadly categorized as P450-containing systems. The term "P450" is der ...
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Estrogen Receptor
Estrogen receptors (ERs) are a group of proteins found inside cells. They are receptors that are activated by the hormone estrogen (17β-estradiol). Two classes of ER exist: nuclear estrogen receptors ( ERα and ERβ), which are members of the nuclear receptor family of intracellular receptors, and membrane estrogen receptors (mERs) (GPER (GPR30), ER-X, and Gq-mER), which are mostly G protein-coupled receptors. This article refers to the former (ER). Once activated by estrogen, the ER is able to translocate into the nucleus and bind to DNA to regulate the activity of different genes (i.e. it is a DNA-binding transcription factor). However, it also has additional functions independent of DNA binding. As hormone receptors for sex steroids ( steroid hormone receptors), ERs, androgen receptors (ARs), and progesterone receptors (PRs) are important in sexual maturation and gestation. Proteomics There are two different forms of the estrogen receptor, usually referred to as ...
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Steroidogenic Enzyme
__NOTOC__ Steroidogenic enzymes are enzymes that are involved in steroidogenesis and steroid biosynthesis. They are responsible for the biosynthesis of the steroid hormones, including sex steroids (androgens, estrogens, and progestogens) and corticosteroids (glucocorticoids and mineralocorticoids), as well as neurosteroids, from cholesterol. Steroidogenic enzymes are most highly expressed in classical steroidogenic tissues, such as the testis, ovary, and adrenal cortex, but are also present in other tissues in the body. List of steroidogenic enzymes * Steroid desmolases ** Cholesterol side-chain cleavage enzyme (20,22-desmolase) – steroid synthesis ** 17,20-Lyase (17,20-desmolase) – androgen synthesis * Steroid hydroxylases ** 11β-Hydroxylase – corticosteroid synthesis ** 17α-Hydroxylase – androgen and glucocorticoid synthesis ** 18-Hydroxylase (aldosterone synthase) – mineralocorticoid synthesis ** 21-Hydroxylase – corticosteroid synthesis ** Cytochrome P450 ( ...
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Posaconazole
Posaconazole, sold under the brand name Noxafil among others, is a triazole antifungal medication. It was approved for medical use in the United States in September 2006, and is available as a generic medication. Medical uses Posaconazole is used to treat invasive ''Aspergillus'' and '' Candida'' infections. It is also used for the treatment of oropharyngeal candidiasis (OPC), including OPC refractory to itraconazole and/or fluconazole therapy. It is also used to treat invasive infections by ''Candida'', ''Mucor'', and ''Aspergillus'' species in severely immunocompromised patients. Clinical evidence for its utility in treatment of invasive disease caused by ''Fusarium'' species ( fusariosis) is limited. It appears to be helpful in a mouse model of naegleriasis. Pharmacology Pharmacodynamics Posaconazole works by disrupting the close packing of acyl chains of phospholipids, impairing the functions of certain membrane-bound enzyme systems such as ATPase and enzymes of ...
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Ravuconazole
Ravuconazole (codenamed BMS-207147 and ER-30346) is a potent triazole antifungal, the development of which was discontinued in 2007. The drug has shown to have a similar spectrum of activity to voriconazole, with an increased half-life. However, ravuconazole has limited activity against species of ''Fusarium'', ''Scedosporium'', and ''Zygomycetes''. See also * Albaconazole * Fosravuconazole, a prodrug of ravuconazole * Isavuconazole Isavuconazonium sulfate, sold under the brand name Cresemba, is a systemic antifungal medication of the triazole class which is used to treat invasive aspergillosis and mucormycosis. The most common side effects include abnormal liver tests, ... References 27-Hydroxylase inhibitors Lanosterol 14α-demethylase inhibitors Nitriles Fluoroarenes Phenylethanolamines Tertiary alcohols Thiazoles Triazole antifungals Abandoned drugs {{antiinfective-drug-stub ...
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Dexmedetomidine
Dexmedetomidine, sold under the trade name Precedex among others, is a drug used in humans for sedation. Veterinarians use dexmedetomidine for similar purposes in treating cats, dogs, and horses. It is also used in humans to treat acute agitation associated with schizophrenia or bipolar I or II disorder. Similar to clonidine, it is a sympatholytic drug that acts as an agonist of α2-adrenergic receptors in certain parts of the brain. It was developed by Orion Pharma. Medical uses Intensive care unit sedation Studies suggest dexmedetomidine for sedation in mechanically ventilated adults may reduce time to extubation and ICU stay. Compared with other sedatives, some studies suggest dexmedetomidine may be associated with less delirium. However, this finding is not consistent across multiple studies. At the very least, when aggregating many study results together, use of dexmedetomidine appears to be associated with less neurocognitive dysfunction compared to other sedatives ...
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Fadrozole
Fadrozole (), sold under the brand name Afema (by Novartis), is a selective, nonsteroidal aromatase inhibitor which is or has been used in Japan for the treatment of breast cancer Breast cancer is cancer that develops from breast tissue. Signs of breast cancer may include a lump in the breast, a change in breast shape, dimpling of the skin, milk rejection, fluid coming from the nipple, a newly inverted nipple, or .... References 11β-Hydroxylase inhibitors 27-Hydroxylase inhibitors Aldosterone synthase inhibitors Aromatase inhibitors Hormonal antineoplastic drugs Imidazopyridines Nitriles {{antineoplastic-drug-stub ...
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Anastrozole
Anastrozole, sold under the brand name Arimidex among others, is a medication used in addition to other treatments for breast cancer. Specifically it is used for hormone receptor-positive breast cancer. It has also been used to prevent breast cancer in those at high risk. It is taken by mouth. Common side effects of anastrozole include hot flashes, altered mood, joint pain, and nausea. Severe side effects include an increased risk of heart disease and osteoporosis. Use during pregnancy may harm the baby. Anastrozole is in the aromatase-inhibiting family of medications. It works by blocking the production of estrogens in the body, and hence has antiestrogenic effects. Anastrozole was patented in 1987 and was approved for medical use in 1995. It is on the World Health Organization's List of Essential Medicines. Anastrozole is available as a generic medication. In 2020, it was the 180th most commonly prescribed medication in the United States, with more than 3million pres ...
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