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Staurosporine
Staurosporine (antibiotic AM-2282 or STS) is a natural product originally isolated in 1977 from the bacterium '' Streptomyces staurosporeus''. It was the first of over 50 alkaloids that were discovered to share this type of bis-indole chemical structure. The chemical structure of staurosporine was elucidated by X-ray crystalography in 1994. Staurosporine was discovered to have biological activities ranging from anti-fungal to anti-hypertensive. The interest in these activities resulted in a large investigative effort in chemistry and biology and the discovery of the potential for anti-cancer treatment. Biological activities The main biological activity of staurosporine is the inhibition of protein kinases through the prevention of ATP binding to the kinase. This is achieved through the stronger affinity of staurosporine to the ATP-binding site on the kinase. Staurosporine is a prototypical ATP-competitive kinase inhibitor in that it binds to many kinases with high affinity, thou ...
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Staurosporine 2
Staurosporine (antibiotic AM-2282 or STS) is a natural product originally isolated in 1977 from the bacterium ''Streptomyces staurosporeus''. It was the first of over 50 alkaloids that were discovered to share this type of bis-indole chemical structure. The chemical structure of staurosporine was elucidated by X-ray crystalography in 1994. Staurosporine was discovered to have biological activities ranging from anti-fungal to anti-hypertensive. The interest in these activities resulted in a large investigative effort in chemistry and biology and the discovery of the potential for anti-cancer treatment. Biological activities The main biological activity of staurosporine is the enzyme inhibition, inhibition of protein kinases through the prevention of ATP binding to the kinase. This is achieved through the stronger affinity of staurosporine to the ATP-binding site on the kinase. Staurosporine is a prototypical ATP-competitive kinase inhibitor in that it binds to many kinases with hi ...
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Indolocarbazole
Indolocarbazoles (ICZs) are a class of compounds that are under current study due to their potential as anti-cancer as well as antimicrobial drugs and the prospective number of derivatives and uses found from the basic backbone alone. First isolated in 1977, a wide range of structures and derivatives have been found or developed throughout the world. Due to the extensive number of structures available, this review will focus on the more important groups here while covering their occurrence, biological activity, biosynthesis, and laboratory synthesis. Chemical classification Indolocarbazoles belong to the alkaloid sub-class of bisindoles. The most frequently isolated indolocarbazoles are Indolo(2,3-a)carbazoles; the most common subgroup of the Indolo(2,3-a)carbazoles are the Indolo(2,3-a)pyrrole(3,4-c)carbazoles. These can be divided into two major classes - halogenated (chlorinated) with a fully oxidized C-7 carbon with only one indole nitrogen containing a β-glycosidic bond an ...
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Fermentek
Fermentek Ltd. is a biotechnological company in the Atarot industrial zone of Jerusalem, Israel. It specializes in the research, development and manufacture of biologically active, natural products isolated from microorganisms as well as from other natural sources such as plants and algae. The main microorganisms used are nonpathogenic actinomycetes, Nocardia and Streptomycetes. The fungi used are: Penicillium, Aspergillus, Fusarium and the like. None of these is a human pathogen. Fermentek does not sell to individuals. Most of its products are marketed through major international distributors specializing in chemicals, under their own brand names. Nevertheless, Fermentek has specific impact on the biochemical market, especially in the field of mycotoxins. Mycotoxins are toxic compounds produced by molds in human food and farm animal feeds, thus being economically important factors. Fermentek manufactures an extensive line of pure mycotoxins used as standards in food analysis. ...
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Protein Kinase
A protein kinase is a kinase which selectively modifies other proteins by covalently adding phosphates to them ( phosphorylation) as opposed to kinases which modify lipids, carbohydrates, or other molecules. Phosphorylation usually results in a functional change of the target protein ( substrate) by changing enzyme activity, cellular location, or association with other proteins. The human genome contains about 500 protein kinase genes and they constitute about 2% of all human genes. There are two main types of protein kinase. The great majority are serine/threonine kinases, which phosphorylate the hydroxyl groups of serines and threonines in their targets. Most of the others are tyrosine kinases, although additional types exist. Protein kinases are also found in bacteria and plants. Up to 30% of all human proteins may be modified by kinase activity, and kinases are known to regulate the majority of cellular pathways, especially those involved in signal transduction. Chemical ...
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Stauprimide
Stauprimide is a semi-synthetic analog of the staurosporine family of indolocarbazoles. Stauprimide was first published in 1994 as part of an extensive structure-activity investigation to improve the selective inhibition of protein kinase C as a potential antitumor agent. More recently, stauprimide has been shown to increase the efficiency of the directed differentiation of mouse and human embryonic stem cells in synergy with defined extracellular signaling cues. Stauprimide interacts with NME2 (PUF) transcription factor to down-regulate c-Myc expression, leading to differentiation of stem cells. See also * Staurosporine * Rebeccamycin * K252a * Midostaurin Midostaurin, sold under the brand name Rydapt by Novartis, is a multi-targeted protein kinase inhibitor that has been investigated for the treatment of acute myeloid leukemia (AML), myelodysplastic syndrome (MDS) and advanced systemic mastocyt ... References {{reflist Indolocarbazoles Protein kinase inhibitors ...
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Glioblastoma
Glioblastoma, previously known as glioblastoma multiforme (GBM), is the most aggressive and most common type of cancer that originates in the brain, and has a very poor prognosis for survival. Initial signs and symptoms of glioblastoma are nonspecific. They may include headaches, personality changes, nausea, and symptoms similar to those of a stroke. Symptoms often worsen rapidly and may progress to unconsciousness. The cause of most cases of glioblastoma is not known. Uncommon risk factors include genetic disorders, such as neurofibromatosis and Li–Fraumeni syndrome, and previous radiation therapy. Glioblastomas represent 15% of all brain tumors. They are thought to arise from astrocytes. The diagnosis typically is made by a combination of a CT scan, MRI scan, and tissue biopsy. There is no known method of preventing the cancer. Treatment usually involves surgery, after which chemotherapy and radiation therapy are used. The medication temozolomide is frequently used a ...
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UC San Diego Health System
UC San Diego Health is the academic health system of the University of California, San Diego in San Diego, California. It is the only academic health system serving San Diego and has one of three adult Level I trauma centers in the region. In operation since 1966, it comprises three major hospitals: UC San Diego Medical Center in Hillcrest, Jacobs Medical Center in La Jolla, and East Campus Medical Center at UC San Diego Health in East County. The La Jolla campus also includes the Moores Cancer Center, Shiley Eye Institute, Sulpizio Cardiovascular Center, and Koman Family Outpatient Pavilion, and the health system also includes several outpatient sites located throughout San Diego County. UC San Diego Health works closely with the university's School of Medicine and Skaggs School of Pharmacy to provide training to medical and pharmacy students and advanced clinical care to patients. It is the official health system of the San Diego Padres and UC San Diego Tritons. Hospit ...
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Nanoparticle
A nanoparticle or ultrafine particle is a particle of matter 1 to 100 nanometres (nm) in diameter. The term is sometimes used for larger particles, up to 500 nm, or fibers and tubes that are less than 100 nm in only two directions. At the lowest range, metal particles smaller than 1 nm are usually called atom clusters instead. Nanoparticles are distinguished from microparticles (1-1000 μm), "fine particles" (sized between 100 and 2500 nm), and "coarse particles" (ranging from 2500 to 10,000 nm), because their smaller size drives very different physical or chemical properties, like colloidal properties and ultrafast optical effects or electric properties. Being more subject to the Brownian motion, they usually do not sediment, like colloid, colloidal particles that conversely are usually understood to range from 1 to 1000 nm. Being much smaller than the wavelengths of visible light (400-700 nm), nanoparticles cannot be seen with ordinary ...
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Violacein
Violacein is a naturally-occurring bis-indole pigment with antibiotic (anti-bacterial, anti-viral, anti-fungal and anti-tumor) properties. Violacein is produced by several species of bacteria, including ''Chromobacterium violaceum'', and gives these organisms their striking purple hues. Violacein shows increasing commercially interesting uses, especially for industrial applications in cosmetics, medicines and fabrics. Biosynthesis Violacein is formed by enzymatic condensation of two tryptophan molecules, requiring the action of five proteins. The genes required for its production, ''vioABCDE'', and the regulatory mechanisms employed haves been studied within a small number of violacein-producing strains. Production of violacein is controlled by quorum sensing using acyl-homoserine lactones (AHLs). Only a few genera of bacteria have been reported to produce violacein. These include ''Chromobacterium'', '' Duganella'', ''Pseudoalteromonas'', '' Janthinobacterium'', ''Iodobacter'' ...
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Liposome
A liposome is a small artificial vesicle, spherical in shape, having at least one lipid bilayer. Due to their hydrophobicity and/or hydrophilicity, biocompatibility, particle size and many other properties, liposomes can be used as drug delivery vehicles for administration of pharmaceutical drugs and nutrients, such as lipid nanoparticles in mRNA vaccines, and DNA vaccines. Liposomes can be prepared by disrupting biological membranes (such as by sonication). Liposomes are most often composed of phospholipids, especially phosphatidylcholine, and cholesterol, but may also include other lipids, such as those found in egg and phosphatidylethanolamine, as long as they are compatible with lipid bilayer structure. A liposome design may employ surface ligands for attaching to desired cells or tissues. Based on vesicle structure, there are seven main categories for liposomes: multilamellar large (MLV), oligolamellar (OLV), small unilamellar (SUV), medium-sized unilamellar (MUV), larg ...
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Glucose
Glucose is a sugar with the Chemical formula#Molecular formula, molecular formula , which is often abbreviated as Glc. It is overall the most abundant monosaccharide, a subcategory of carbohydrates. It is mainly made by plants and most algae during photosynthesis from water and carbon dioxide, using energy from sunlight. It is used by plants to make cellulose, the most abundant carbohydrate in the world, for use in cell walls, and by all living Organism, organisms to make adenosine triphosphate (ATP), which is used by the cell as energy. In energy metabolism, glucose is the most important source of energy in all organisms. Glucose for metabolism is stored as a polymer, in plants mainly as amylose and amylopectin, and in animals as glycogen. Glucose circulates in the blood of animals as blood sugar. The naturally occurring form is -glucose, while its Stereoisomerism, stereoisomer L-glucose, -glucose is produced synthetically in comparatively small amounts and is less biologicall ...
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Fluorescence In The Life Sciences
Fluorescence is widely used in the life sciences as a powerful and minimally invasive method to track and analyze biological molecules in real-time Some proteins or small molecules in cells are naturally fluorescent, which is called intrinsic fluorescence or autofluorescence (such as NADH, tryptophan or endogenous chlorophyll, phycoerythrin or green fluorescent protein). The intrinsic DNA fluorescence is very weak. Alternatively, specific or general proteins, nucleic acids, lipids or small molecules can be "labelled" with an extrinsic fluorophore, a fluorescent dye which can be a small molecule, protein or quantum dot. Several techniques exist to exploit additional properties of fluorophores, such as fluorescence resonance energy transfer, where the energy is passed non-radiatively to a particular neighbouring dye, allowing proximity or protein activation to be detected; another is the change in properties, such as intensity, of certain dyes depending on their environment allo ...
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