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Epothilone
Epothilones are a class of potential cancer drugs. Like taxanes, they prevent cancer cells from dividing by interfering with tubulin, but in early trials, epothilones have better efficacy and milder adverse effects than taxanes. Epothilones were originally identified as metabolites produced by the soil-dwelling myxobacterium ''Sorangium cellulosum''. , epothilones A to F have been identified and characterized. Early studies in cancer cell lines and human cancer patients indicate superior efficacy to the taxanes. Their mechanism of action is similar, but their chemical structure is simpler. Due to their better water solubility, cremophors (solubilizing agents used for paclitaxel which can affect cardiac function and cause severe hypersensitivity) are not needed. Endotoxin-like properties known from paclitaxel, like activation of macrophages synthesizing inflammatory cytokines and nitric oxide, are not observed for epothilone B. History The structure of epothilone A was determin ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Sagopilone
Sagopilone is a fully synthetic macrolide of the epothilone family with the molecular formula C30H41NO6S. The mechanism of action is similar to taxanes, as they bind to the microtubule and prohibit cell division. These toxic properties and its possibility to cross the blood-brain barrier makes it a promising cancer medication. Substance class Sagopilone, also known as ZK-EPO, belongs to the epothilones, which are derived from polyketides. Structure Sagopilone is a 16-bond macrolide structure, a macrocycle with inner ester In chemistry, an ester is a compound derived from an acid (either organic or inorganic) in which the hydrogen atom (H) of at least one acidic hydroxyl group () of that acid is replaced by an organyl group (R). These compounds contain a distin ... structure. With its C30H41NO6S formula and a molecular weight of only 543.7 g/mol, classifying it as a low molecular-weight epothilone. Sagopilone has structural and mechanistic similarities to epothilone ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Ixabepilone
Ixabepilone ( INN; also known as azaepothilone B, codenamed BMS-247550) is a pharmaceutical drug developed by Bristol-Myers Squibb as a chemotherapeutic medication for cancer. History Ixabepilone is a semi-synthetic analog of epothilone B, a natural chemical compound produced by '' Sorangium cellulosum''. The structural difference between Epothilone B and Ixabepilone consists of only a single atom oxygen-to-nitrogen subsitution that converts the ester into an amide. Epothilone B itself could not be developed as a pharmaceutical drug because of poor metabolic stability and pharmacokinetics. Ixabepilone was designed through medicinal chemistry to improve upon these properties. Pharmacology Much like Taxol, Ixabepilone acts to stabilize microtubules. It is highly potent, capable of damaging cancer cells in very low concentrations, and retains activity in cases where tumor cells are insensitive to taxane type drugs. Approval On October 16, 2007, the U.S. Food and Drug Administ ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Utidelone
Utidelone is a pharmaceutical drug for the treatment of metastatic breast cancer. It was approved for use in China in 2021. Utidelone is a member of the epothilone class of natural products, which are metabolites produced by the soil-dwelling myxobacterium ''Sorangium cellulosum ''Sorangium cellulosum'' is a soil-dwelling Gram-negative bacterium of the group myxobacteria. It is motile and shows gliding motility. Under stressful conditions this motility, as in other myxobacteria, the cells congregate to form fruiting b ...''. It is also known as epothilone D. References Antineoplastic and immunomodulating drugs {{antineoplastic-drug-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Myxobacterium
The myxobacteria ("slime bacteria") are a group of bacteria that predominantly live in the soil and feed on insoluble organic substances. The myxobacteria have very large genomes relative to other bacteria, e.g. 9–10 million nucleotides except for '' Anaeromyxobacter'' and ''Vulgatibacter''. One species of myxobacteria, ''Minicystis rosea'', has the largest known bacterial genome with over 16 million nucleotides. The second largest is another myxobacteria ''Sorangium cellulosum''. Myxobacteria can move by gliding. They typically travel in '' swarms'' (also known as ''wolf packs''), containing many cells kept together by intercellular molecular signals. Individuals benefit from aggregation as it allows accumulation of the extracellular enzymes that are used to digest food; this in turn increases feeding efficiency. Myxobacteria produce a number of biomedically and industrially useful chemicals, such as antibiotics, and export those chemicals outside the cell. Myxobacteria are ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Breast Cancer
Breast cancer is a cancer that develops from breast tissue. Signs of breast cancer may include a Breast lump, lump in the breast, a change in breast shape, dimpling of the skin, Milk-rejection sign, milk rejection, fluid coming from the nipple, a newly inverted nipple, or a red or scaly patch of skin. In those with Metastatic breast cancer, distant spread of the disease, there may be bone pain, swollen lymph nodes, shortness of breath, or yellow skin. Risk factors for developing breast cancer include obesity, a Sedentary lifestyle, lack of physical exercise, alcohol consumption, hormone replacement therapy during menopause, ionizing radiation, an early age at Menarche, first menstruation, having children late in life (or not at all), older age, having a prior history of breast cancer, and a family history of breast cancer. About five to ten percent of cases are the result of an inherited genetic predisposition, including BRCA mutation, ''BRCA'' mutations among others. Breast ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Sorangium Cellulosum
''Sorangium cellulosum'' is a soil-dwelling Gram-negative bacterium of the group myxobacteria. It is motile and shows gliding motility. Under stressful conditions this motility, as in other myxobacteria, the cells congregate to form fruiting bodies and differentiate into myxospores. These congregating cells make isolation of pure culture and colony counts on agar medium difficult as the bacterium spread and colonies merge. It has an unusually-large genome of 13,033,779 base pairs, making it the largest bacterial genome sequenced to date by roughly 4 Mb. Ecology ''S. cellulosum'' is found in soils, animal feces, and tree bark. The bacterium is a saprophyte deriving its nutrition from cellulose aerobically. It is a prolific producer of secondary fungicides and bactericides that reduce competition in soil environments. In lab samples, ''S. cellulosum'' grows on agar medium only when certain cell densities are plated. Quorum-sensing allows Sorangium to grow in communities suff ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Microtubule
Microtubules are polymers of tubulin that form part of the cytoskeleton and provide structure and shape to eukaryotic cells. Microtubules can be as long as 50 micrometres, as wide as 23 to 27 nanometer, nm and have an inner diameter between 11 and 15 nm. They are formed by the polymerization of a Protein dimer, dimer of two globular proteins, Tubulin#Eukaryotic, alpha and beta tubulin into #Structure, protofilaments that can then associate laterally to form a hollow tube, the microtubule. The most common form of a microtubule consists of 13 protofilaments in the tubular arrangement. Microtubules play an important role in a number of cellular processes. They are involved in maintaining the structure of the cell and, together with microfilaments and intermediate filaments, they form the cytoskeleton. They also make up the internal structure of cilia and flagella. They provide platforms for intracellular transport and are involved in a variety of cellular processes, in ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Metabolites
In biochemistry, a metabolite is an intermediate or end product of metabolism. The term is usually used for small molecules. Metabolites have various functions, including fuel, structure, signaling, stimulatory and inhibitory effects on enzymes, catalytic activity of their own (usually as a cofactor to an enzyme), defense, and interactions with other organisms (e.g. pigments, odorants, and pheromones). A primary metabolite is directly involved in normal "growth", development, and reproduction. Ethylene exemplifies a primary metabolite produced large-scale by industrial microbiology. A secondary metabolite is not directly involved in those processes, but usually has an important ecological function. Examples include antibiotics and pigments such as resins and terpenes etc. Some antibiotics use primary metabolites as precursors, such as actinomycin, which is created from the primary metabolite tryptophan. Some sugars are metabolites, such as fructose or glucose, which ar ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Food And Drug Administration
The United States Food and Drug Administration (FDA or US FDA) is a List of United States federal agencies, federal agency of the United States Department of Health and Human Services, Department of Health and Human Services. The FDA is responsible for protecting and promoting public health through the control and supervision of food safety, tobacco products, caffeine products, dietary supplements, Prescription drug, prescription and Over-the-counter drug, over-the-counter pharmaceutical drugs (medications), vaccines, biopharmaceuticals, blood transfusions, medical devices, electromagnetic radiation emitting devices (ERED), cosmetics, Animal feed, animal foods & feed and Veterinary medicine, veterinary products. The FDA's primary focus is enforcement of the Federal Food, Drug, and Cosmetic Act (FD&C). However, the agency also enforces other laws, notably Section 361 of the Public Health Service Act as well as associated regulations. Much of this regulatory-enforcement work is ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
