Echinocandin B
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Echinocandin B
Echinocandin B, a lipopeptide, is a naturally occurring cyclic hexapeptide with a linoleoyl side chain. It belongs to a class of antifungal agents called echinocandins, which inhibits the synthesis of glucan, a major component of the fungal cell wall, via noncompetitive inhibition of a crucial enzyme, β-(1→3)-D-glucan synthase. Echinocandin B is a fermentation product of ''Aspergillus nidulans'' and the closely related species, ''A. rugulosus''; discovered in 1974 in ''A. nidulans'' var. ''echinulatus'' strain A 32204 in Germany, it was the first of the echinocandin class of antifungals. Echinocandin B can undergo deacylation (removal of the lipid side chain) by the action of a deacylase enzyme from the filamentous bacterium '' Actinoplanes utahensis'', which catalyzes the cleavage of the linoleoyl side chain; in three subsequent synthetic steps, including a chemical reacylation, the antifungal drug anidulafungin Anidulafungin (International nonproprietary name, INN) (tr ...
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Lipopeptide
A lipopeptide is a molecule consisting of a lipid connected to a peptide. They are able to self-assemble into different structures. Many bacteria produced these molecules as a part of their metabolism, especially those of the genus ''Bacillus'', ''Pseudomonas'' and ''Streptomyces''. Certain lipopeptides are used as antibiotics. Other lipopeptides are toll-like receptor agonists. Certain lipopeptides can have strong antifungal and hemolytic activities. It has been demonstrated that their activity is generally linked to interactions with the plasma membrane, and sterol components of the plasma membrane could play a major role in this interaction. It is a general trend that adding a lipid group of a certain length (typically C10–C12) to a lipopeptide will increase its bactericidal activity. Lipopeptides with a higher amount of carbon atoms, for example 14 or 16, in its lipid tail will typically have antibacterial activity as well as anti-fungal activity. Lipopeptide detergents (LPDs ...
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Linoleic Acid
Linoleic acid (LA) is an organic compound with the formula COOH(CH2)7CH=CHCH2CH=CH(CH2)4CH3. Both alkene groups are cis-trans isomerism, ''cis''. It is a fatty acid sometimes denoted 18:2 (n-6) or 18:2 ''cis''-9,12. A linoleate is a salt (chemistry), salt or ester of this acid. Linoleic acid is a polyunsaturated fatty acid, polyunsaturated omega-6 fatty acid. It is a colorless liquid that is virtually insoluble in water but soluble in many organic solvents. It typically occurs in nature as a triglyceride (ester of glycerol, glycerin) rather than as a free fatty acid. It is one of two essential fatty acids for humans, who must obtain it through their diet, and the most essential, because the body uses it as a base to make the others. The word "linoleic" derives from the Latin ''linum'' "flax" + ''oleum'' "oil", reflecting the fact that it was first isolated from linseed oil. History In 1844, F. Sacc, working at the laboratory of Justus von Liebig, isolated linoleic acid from l ...
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Fungicide
Fungicides are biocidal chemical compounds or biological organisms used to kill parasitic fungi or their spores. A fungistatic inhibits their growth. Fungi can cause serious damage in agriculture, resulting in critical losses of yield, quality, and profit. Fungicides are used both in agriculture and to fight fungal infections in animals. Chemicals used to control oomycetes, which are not fungi, are also referred to as fungicides, as oomycetes use the same mechanisms as fungi to infect plants. Fungicides can either be contact, translaminar or systemic. Contact fungicides are not taken up into the plant tissue and protect only the plant where the spray is deposited. Translaminar fungicides redistribute the fungicide from the upper, sprayed leaf surface to the lower, unsprayed surface. Systemic fungicides are taken up and redistributed through the xylem vessels. Few fungicides move to all parts of a plant. Some are locally systemic, and some move upwardly. Most fungicides that can ...
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Echinocandin
Echinocandins are a class of antifungal drugs that inhibit the synthesis of β-glucan in the fungal cell wall via noncompetitive inhibition of the enzyme 1,3-β glucan synthase. The class has been termed the " penicillin of antifungals," along with the related papulacandins, as their mechanism of action resembles that of penicillin in bacteria. β-glucans are carbohydrate polymers that are cross-linked with other fungal cell wall components, the fungal equivalent to bacterial peptidoglycan. Caspofungin, micafungin, and anidulafungin are semisynthetic echinocandin derivatives with limited clinical use due to their solubility, antifungal spectrum, and pharmacokinetic properties. Medical uses Drugs and drug candidates in this class are fungicidal against some yeasts (most species of ''Candida'', but not ''Cryptococcus'', '' Trichosporon'', and ''Rhodotorula''). Echinocandins also have displayed activity against ''Candida'' biofilms, especially in synergistic activity with ampho ...
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Enzyme
Enzymes () are proteins that act as biological catalysts by accelerating chemical reactions. The molecules upon which enzymes may act are called substrates, and the enzyme converts the substrates into different molecules known as products. Almost all metabolic processes in the cell need enzyme catalysis in order to occur at rates fast enough to sustain life. Metabolic pathways depend upon enzymes to catalyze individual steps. The study of enzymes is called ''enzymology'' and the field of pseudoenzyme analysis recognizes that during evolution, some enzymes have lost the ability to carry out biological catalysis, which is often reflected in their amino acid sequences and unusual 'pseudocatalytic' properties. Enzymes are known to catalyze more than 5,000 biochemical reaction types. Other biocatalysts are catalytic RNA molecules, called ribozymes. Enzymes' specificity comes from their unique three-dimensional structures. Like all catalysts, enzymes increase the reaction ra ...
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1,3-Beta-glucan Synthase
1,3-Beta-glucan synthase is a glucosyltransferase enzyme involved in the generation of beta-glucan in fungi. It serves as a pharmacological target for antifungal drugs such as caspofungin, anidulafungin, and micafungin, deemed 1,3-Beta-glucan synthase inhibitors. Under the CAZy classification system, fungi and plant members fall in the glycosyltransferase 48 family (GT48). Some members of the glycosyltransferase 2 family (), such as the curdlan synthase ''CrdS''Q9X2V0, also has a similar activity. The biosynthesis of disaccharides, oligosaccharides, and polysaccharides involves the action of hundreds of different glycosyltransferases. These enzymes catalyse the transfer of sugar moieties from activated donor molecules to specific acceptor molecules, forming glycosidic bonds. The family consists of various 1,3-beta-glucan synthase components including Gls1, Gls2, and Gls3 from yeast. 1,3-Beta-glucan synthase () also known as callose synthase catalyses the formation of a beta ...
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Aspergillus Nidulans
''Aspergillus nidulans'' (also called ''Emericella nidulans'' when referring to its sexual form, or teleomorph) is one of many species of filamentous fungi in the phylum Ascomycota. It has been an important research organism for studying eukaryotic cell biology for over 50 years, being used to study a wide range of subjects including recombination, DNA repair, mutation, cell cycle control, tubulin, chromatin, nucleokinesis, pathogenesis, metabolism, and experimental evolution. It is one of the few species in its genus able to form sexual spores through meiosis, allowing crossing of strains in the laboratory. ''A. nidulans'' is a homothallic fungus, meaning it is able to self-fertilize and form fruiting bodies in the absence of a mating partner. It has septate hyphae with a woolly colony texture and white mycelia. The green colour of wild-type colonies is due to pigmentation of the spores, while mutations in the pigmentation pathway can produce other spore colours. Genome The ' ...
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Aspergillus Rugulosus
''Aspergillus rugulosus'' is a species of fungus in the genus ''Aspergillus''. It is from the ''Nidulantes'' section. The species was first described in 1939. It has been isolated from soil in New Jersey, United States. It has been reported to produce sterigmatocystin, arugosin A, arugosin B, arugosin C, asperthecin, aspertetronin A, aspertetronin B, cyclo-L-isoleucyl-L-proline, cyclo-L-leucyl-L-proline, cyclo-L- valyl-L-proline, desferritriacetylfusigen, 3,30-Dihydroxy-5,50-dimethyldiphenyl ether, 2,4-dihydroxy-6- (hydroxymethyl)-benzaldehyde, 2,4-dihydroxy-6- methylbenzaldehyde, 2,4-dihydroxy-6-(hydroxymethyl)-benzaldehyde, echinocandin B, echinocandin C, echinocandin D, epishamixanthone, shamixanthone, 14-Hydroxytajixanthone 25-O-acetate, 14- Methoxytajixanthone 25-O-acetate, 14-Methoxytajixanthone, orsellinaldehyde, penicillin G Benzylpenicillin, also known as penicillin G (PenG) or BENPEN, and in military slang "Peanut Butter Shot" is an antibiotic used to treat a ...
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Actinoplanes Utahensis
''Actinoplanes utahensis'' is a species of bacteria and a source of the drug acarbose, an alpha-glucosidase inhibitor used in the treatment of diabetes mellitus. Description ''A. utahensis'' are irregular in size and shape. They form sporangia which are 5 to 18 micrometers in diameter, and contain spores arranged in irregular coils. ''A. utahensis'' are motile by way of a number of flagella at one end. History ''A. utahensis'' was originally identified by John Couch from soils collected from Salt Lake City's Liberty Park Liberty Park is a elevated public park at the World Trade Center in Manhattan, New York City, overlooking the National September 11 Memorial & Museum in Lower Manhattan. The park, which opened on June 29, 2016, is located above the World Trad ... as well as along U.S. Route 40 in Nevada. References External links Type strain of ''Actinoplanes utahensis'' at Bac''Dive'' – the Bacterial Diversity Metadatabase {{Taxonbar, from=Q25834615 Micromonosp ...
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Anidulafungin
Anidulafungin (International nonproprietary name, INN) (trade names Eraxis, Ecalta) is a Semisynthesis, semisynthetic echinocandin used as an antifungal medication, antifungal drug. It was previously known as LY303366. It may also have application in treating invasive ''Aspergillus'' infection when used in combination with voriconazole. It is a member of the class of antifungal drugs known as the echinocandins; its mechanism of action is by inhibition of Beta-glucan, (1→3)-β-D-glucan synthase, an enzyme important to the synthesis of the fungal cell wall. It is on the WHO Model List of Essential Medicines, World Health Organization's List of Essential Medicines. Indications * Fungemia, Candidemia and other forms of invasive ''Candida'' infections (intra-abdominal abscess and peritonitis) * Esophageal candidiasis Anidulafungin has not been studied in Infective endocarditis#Fungal, endocarditis, osteomyelitis, and Meningitis#Fungal, meningitis due to ''Candida'', and has not been ...
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Antifungals
An antifungal medication, also known as an antimycotic medication, is a pharmaceutical fungicide or fungistatic used to treat and prevent mycosis such as athlete's foot, ringworm, candidiasis (thrush), serious systemic infections such as cryptococcal meningitis, and others. Such drugs are usually yes obtained by a doctor's prescription, but a few are available over the counter (OTC). Types of antifungal There are two types of antifungals: local and systemic. Local antifungals are usually administered topically or vaginally, depending on the condition being treated. Systemic antifungals are administered orally or intravenously. Of the clinically employed azole antifungals, only a handful are used systemically. These include ketoconazole, itraconazole, fluconazole, fosfluconazole, voriconazole, posaconazole, and isavuconazole. Examples of non-azole systemic antifungals include griseofulvin and terbinafine. Classes Polyenes A polyene is a molecule with multiple conjugated do ...
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