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Dideoxyverticillin A
Dideoxyverticillin A, also known as (+)-11,11′-dideoxyverticillin A, is a complex epipolythiodioxopiperazine initially isolated from the marine fungus ''Penicillium'' sp. in 1999. It has also been found in the marine fungus ''Bionectriaceae'', and belongs to a class of naturally occurring 2,5-diketopiperazines. Dideoxyverticillin A potently inhibits the tyrosine kinase activity of the epidermal growth factor receptor (median inhibitory concentration = 0.14 nM), exhibits antiangiogenic activity, and has efficacy against several cancer cell lines. Its reported anticancer mechanism is that it acts as a farnesyl transferase inhibitor. Dozens of semi-synthetic anticancer compounds have been made from dideoxyverticillin A. Dimeric derivatives are reported to have better anticancer activity. The enantioselective first total synthesis of (+)-11,11′-dideoxyverticillin A, the structure of which contains many sterically congested, contiguous stereogenic centers as well as acid- and b ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Marine Fungus
Marine fungi are species of fungi that live in marine or estuarine environments. They are not a taxonomic group, but share a common habitat. Obligate marine fungi grow exclusively in the marine habitat while wholly or sporadically submerged in sea water. Facultative marine fungi normally occupy terrestrial or freshwater habitats, but are capable of living or even sporulating in a marine habitat. About 444 species of marine fungi have been described, including seven genera and ten species of basidiomycetes, and 177 genera and 360 species of ascomycetes. The remainder of the marine fungi are chytrids and mitosporic or asexual fungi.Species of Higher Marine Fungi University of Mississippi. Retrieved 2012-02-05. Many species of marine fungi are known only from |
Penicillium
''Penicillium'' () is a genus of ascomycetous fungi that is part of the mycobiome of many species and is of major importance in the natural environment, in food spoilage, and in food and drug production. Some members of the genus produce penicillin, a molecule that is used as an antibiotic, which kills or stops the growth of certain kinds of bacteria. Other species are used in cheesemaking. According to the ''Dictionary of the Fungi'' (10th edition, 2008), the widespread genus contains over 300 species. Taxonomy The genus was first described in the scientific literature by Johann Heinrich Friedrich Link in his 1809 work ''Observationes in ordines plantarum naturales''; he wrote, "''Penicillium. Thallus e floccis caespitosis septatis simplicibus aut ramosis fertilibus erectis apice penicillatis''", where ''penicillatis'' means "having tufts of fine hair". Link included three species—'' P. candidum'', '' P. expansum'', and '' P. glaucum''—all of which produ ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Bionectriaceae
The Bionectriaceae are a family of fungi in the order Hypocreales. A 2008 estimate places 35 genera and 281 species in the family. Species in the family tend to grow on plant material, including woody debris, while some species associate with algae, bryophytes, or other fungi. Genera This is a list of the genera in the Bionectriaceae, based on a 2022 review and summary of fungal classification by Wijayawardene and colleagues. Following the genus name is the taxonomic authority (those who first circumscribed the genus; standardized author abbreviations are used), year of publication, and the number of species: *''Acremonium'' – ca. 150 *'' Anthonectria'' – 1 sp. *'' Aphanotria'' – 1 sp. *'' Battarrina'' – 1 sp. *'' Bryocentria'' – 15 spp. *'' Bryotria'' – 2 spp. *'' Bullanockia'' – 1 sp. *'' Chrysonectria'' – 1 sp. *'' Clibanites'' – 1 sp. *'' Clonostachys'' – 78 spp. *'' Dimerosporiella'' – 8 spp. *'' Fusariella'' – 17 spp. *'' Geonectria'' ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Tyrosine Kinase
A tyrosine kinase is an enzyme that can transfer a phosphate group from ATP to the tyrosine residues of specific proteins inside a cell. It functions as an "on" or "off" switch in many cellular functions. Tyrosine kinases belong to a larger class of enzymes known as protein kinases which also attach phosphates to other amino acids such as serine and threonine. Phosphorylation of proteins by kinases is an important mechanism for communicating signals within a cell (signal transduction) and regulating cellular activity, such as cell division. Protein kinases can become mutated, stuck in the "on" position, and cause unregulated growth of the cell, which is a necessary step for the development of cancer. Therefore, kinase inhibitors, such as imatinib and osimertinib, are often effective cancer treatments. Most tyrosine kinases have an associated protein tyrosine phosphatase, which removes the phosphate group. Reaction Protein kinases are a group of enzymes that possess a catal ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Epidermal Growth Factor Receptor
The epidermal growth factor receptor (EGFR; ErbB-1; HER1 in humans) is a transmembrane protein that is a receptor for members of the epidermal growth factor family (EGF family) of extracellular protein ligands. The epidermal growth factor receptor is a member of the ErbB family of receptors, a subfamily of four closely related receptor tyrosine kinases: EGFR (ErbB-1), HER2/neu (ErbB-2), Her 3 (ErbB-3) and Her 4 (ErbB-4). In many cancer types, mutations affecting EGFR expression or activity could result in cancer. Epidermal growth factor and its receptor was discovered by Stanley Cohen of Vanderbilt University. Cohen shared the 1986 Nobel Prize in Medicine with Rita Levi-Montalcini for their discovery of growth factors. Deficient signaling of the EGFR and other receptor tyrosine kinases in humans is associated with diseases such as Alzheimer's, while over-expression is associated with the development of a wide variety of tumors. Interruption of EGFR signalling, either by ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Farnesyl Transferase Inhibitor
The farnesyltransferase inhibitors (FTIs) are a class of experimental cancer drugs that target protein farnesyltransferase with the downstream effect of preventing the proper functioning of the Ras (protein), which is commonly abnormally active in cancer. Background Studies have suggested that interference with certain post-translational modification processes seem to have quite a high selectivity for targeting cells displaying tumour phenotypes, although the reason for this is a matter of controversy. After translation, Ras goes through four steps of modification: isoprenylation, proteolysis, methylation and palmitoylation. Isoprenylation involves the enzyme farnesyltransferase (FTase) transferring a farnesol, farnesyl group from farnesyl pyrophosphate (FPP) to the pre-Ras protein. Also, a related enzyme geranylgeranyltransferase I (GGTase I) has the ability to transfer a geranylgeranyl group to K and N-Ras (the implications of this are discussed below). Farnesyl is necessary to ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Enantioselective
In chemistry, an enantiomer ( /ɪˈnænti.əmər, ɛ-, -oʊ-/ ''ih-NAN-tee-ə-mər''; from Ancient Greek ἐνάντιος ''(enántios)'' 'opposite', and μέρος ''(méros)'' 'part') – also called optical isomer, antipode, or optical antipode – is one of two stereoisomers that are non-superposable onto their own mirror image. Enantiomers are much like one's right and left hands, when looking at the same face, they cannot be superposed onto each other. No amount of reorientation will allow the four unique groups on the chiral carbon (see Chirality (chemistry)) to line up exactly. The number of stereoisomers a molecule has can be determined by the number of chiral carbons it has. Stereoisomers include both enantiomers and diastereomers. Diastereomers, like enantiomers, share the same molecular formula and are non-superposable onto each other however, they are not mirror images of each other. A molecule with chirality rotates plane-polarized light. A mixture of equals amou ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Contiguity
Contiguity or contiguous may refer to: *Contiguous data storage, in computer science *Contiguity (probability theory) *Contiguity (psychology) *Contiguous distribution of species, in biogeography *Geographic contiguity of territorial land *Contiguous zone The term territorial waters is sometimes used informally to refer to any area of water over which a sovereign state has jurisdiction, including internal waters, the territorial sea, the contiguous zone, the exclusive economic zone, and potenti ... in territorial waters See also * * {{disambig ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Redox
Redox (reduction–oxidation, , ) is a type of chemical reaction in which the oxidation states of substrate (chemistry), substrate change. Oxidation is the loss of Electron, electrons or an increase in the oxidation state, while reduction is the gain of electrons or a decrease in the oxidation state. There are two classes of redox reactions: * ''Electron-transfer'' – Only one (usually) electron flows from the reducing agent to the oxidant. This type of redox reaction is often discussed in terms of redox couples and electrode potentials. * ''Atom transfer'' – An atom transfers from one substrate to another. For example, in the rusting of iron, the oxidation state of iron atoms increases as the iron converts to an oxide, and simultaneously the oxidation state of oxygen decreases as it accepts electrons released by the iron. Although oxidation reactions are commonly associated with the formation of oxides, other chemical species can serve the same function. In hydrogen ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Farnesyltransferase Inhibitors
Farnesyltransferase () is one of the three enzymes in the prenyltransferase group. Farnesyltransferase (FTase) adds a 15-carbon isoprenoid called a farnesyl group to proteins bearing a CaaX motif: a four-amino acid sequence at the carboxyl terminus of a protein. Farnesyltransferase's targets include members of the Ras superfamily of small GTP-binding proteins critical to cell cycle progression. For this reason, several FTase inhibitors are undergoing testing as anti-cancer agents. FTase inhibitors have shown efficacy as anti-parasitic agents, as well. FTase is also believed to play an important role in development of progeria and various forms of cancers. Farnesyltransferase catalyzes the chemical reaction :farnesyl diphosphate + protein-cysteine \rightleftharpoons S-farnesyl protein + diphosphate Thus, the two substrates of this enzyme are farnesyl diphosphate and protein-cysteine, whereas its two products are S-farnesyl protein and diphosphate. Overview Farnesyltransfer ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
