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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 ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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 ''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. ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Antifungal Drug
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 multipl ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Anidulafungin
Anidulafungin (INN) (trade names Eraxis, Ecalta) is a semisynthetic echinocandin used as an 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 (1→3)-β-D-glucan synthase, an enzyme important to the synthesis of the fungal cell wall. It is on the World Health Organization's List of Essential Medicines. Indications * Candidemia and other forms of invasive ''Candida'' infections (intra-abdominal abscess and peritonitis) * Esophageal candidiasis Anidulafungin has not been studied in endocarditis, osteomyelitis, and meningitis due to ''Candida'', and has not been studied in sufficient numbers of neutropenic patients to determine efficacy in this group. Pharmacodynamics and pharmacokinetics Anidulafungin significantly differs from other antifu ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Micafungin
Micafungin, sold under the brand name Mycamine, is an echinochandin antifungal medication used to treat and prevent invasive fungal infections including candidemia, abscesses, and esophageal candidiasis. It inhibits the production of beta-1,3-glucan, an essential component of fungal cell walls that is not found in mammals. Micafungin is administered intravenously. It received final approval from the U.S. Food and Drug Administration (FDA) in March 2005, and gained approval in the European Union in April 2008. It is on the ''World Health Organization's List of Essential Medicines''. Indications Micafungin is indicated for the treatment of candidemia, acute disseminated candidiasis, ''Candida'' peritonitis, abscesses and esophageal candidiasis. Since January 23, 2008, micafungin has been approved for the prophylaxis of ''Candida'' infections in patients undergoing hematopoietic stem cell transplantation (HSCT). Micafungin works by way of concentration-dependent inhibition ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Papulacandin B
Papulacandin B is a papulacandin isolated from a strain of '' Papularia sphaerosperma''. It is a molecule with antifungal activity. See also * 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 ... References Antifungals Phenol glycosides Resorcinols Spiro compounds Oxygen heterocycles {{organic-compound-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Caspofungin Structure
Caspofungin (INN) (brand name Cancidas) is a lipopeptide antifungal drug from Merck & Co., Inc. discovered by James Balkovec, Regina Black and Frances A. Bouffard. It is a member of a new class of antifungals termed the echinocandins. It works by inhibiting the enzyme (1→3)-β-D-glucan synthase and thereby disturbing the integrity of the fungal cell wall. Caspofungin was the first inhibitor of fungal (1→3)-β-D-glucan synthesis to be approved by the United States Food and Drug Administration. Caspofungin is administered intravenously. It is on the World Health Organization's List of Essential Medicines. Spectrum of Activity Caspofungin has been effective in treating fungal infections caused by ''Aspergillus'' and ''Candida'' species. It is a member of the echinocandin family, a new class of antifungal agents with broad spectrum of activity against all Candida species. In comparison to treatment with either fluconazole or Amphotericin B, all three drugs in this class have ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Caspofungin
Caspofungin ( INN) (brand name Cancidas) is a lipopeptide antifungal drug from Merck & Co., Inc. discovered by James Balkovec, Regina Black and Frances A. Bouffard. It is a member of a new class of antifungals termed the echinocandins. It works by inhibiting the enzyme (1→3)-β-D-glucan synthase and thereby disturbing the integrity of the fungal cell wall. Caspofungin was the first inhibitor of fungal (1→3)-β-D-glucan synthesis to be approved by the United States Food and Drug Administration. Caspofungin is administered intravenously. It is on the World Health Organization's List of Essential Medicines. Spectrum of Activity Caspofungin has been effective in treating fungal infections caused by ''Aspergillus'' and ''Candida'' species. It is a member of the echinocandin family, a new class of antifungal agents with broad spectrum of activity against all Candida species. In comparison to treatment with either fluconazole or Amphotericin B, all three drugs in this clas ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Cilofungin
Cilofungin (INN) is the first clinically applied member of the echinocandin family of antifungal drugs. It was derived from a fungus in the genus ''Aspergillus ' () is a genus consisting of several hundred mold species found in various climates worldwide. ''Aspergillus'' was first catalogued in 1729 by the Italian priest and biologist Pier Antonio Micheli. Viewing the fungi under a microscope, Mic ...''. It accomplishes this by interfering with an invading fungus' ability to synthesize the cell wall (specifically, it inhibits the synthesis of (1→3)-β-D-glucan). References Abandoned drugs Antifungals Echinocandins {{antiinfective-drug-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
1,3-β 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 formatio ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Penicillin
Penicillins (P, PCN or PEN) are a group of β-lactam antibiotics originally obtained from ''Penicillium'' moulds, principally '' P. chrysogenum'' and '' P. rubens''. Most penicillins in clinical use are synthesised by P. chrysogenum using deep tank fermentation and then purified. A number of natural penicillins have been discovered, but only two purified compounds are in clinical use: penicillin G ( intramuscular or intravenous use) and penicillin V (given by mouth). Penicillins were among the first medications to be effective against many bacterial infections caused by staphylococci and streptococci. They are still widely used today for different bacterial infections, though many types of bacteria have developed resistance following extensive use. 10% of the population claims penicillin allergies but because the frequency of positive skin test results decreases by 10% with each year of avoidance, 90% of these patients can tolerate penicillin. Additionally, those w ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Pneumocystis Jirovecii
''Pneumocystis jirovecii'' (previously ''P. carinii'') is a yeast-like fungus of the genus ''Pneumocystis''. The causative organism of ''Pneumocystis'' pneumonia, it is an important human pathogen, particularly among immunocompromised hosts. Prior to its discovery as a human-specific pathogen, ''P. jirovecii'' was known as ''P. carinii''. Lifecycle The complete lifecycles of any of the species of ''Pneumocystis'' are not known, but presumably all resemble the others in the genus. The terminology follows zoological terms, rather than mycological terms, reflecting the initial misdetermination as a protozoan parasite. It is an extracellular fungus. All stages are found in lungs and because they cannot be cultured '' ex vivo'', direct observation of living ''Pneumocystis'' is difficult. The trophozoite stage is thought to be equivalent to the so-called vegetative state of other species (such as ''Schizosaccharomyces pombe''), which like ''Pneumocystis'', belong to the Taphrinomyco ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
