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K252a
K252a is an alkaloid isolated from '' Nocardiopsis'' bacteria. This staurosporine analog is a highly potent cell permeable inhibitor of CaM kinase and phosphorylase kinase (IC50 = 1.8 and 1.7 nmol/ L, respectively). At higher concentrations it is also an efficient inhibitor of serine/threonine protein kinases (IC50 of 10 to 30 nmol/L).Tapley, P. ''et al.'' (1992) Oncogene 7, 371. K252a is reported to promote myogenic differentiation in C2 mouse myoblasts and has been shown to block the neuronal differentiation of rat pheochromocytoma PC12 cells by inhibition of trk tyrosine kinase activity. K252a has been reported in preclinical research as a potential treatment for psoriasisPromising New Treatments for Psoriasis, Sarah Dubois Declercq and Roxane Pouliot >.The Scientific World Journal; Volume 2013, Article ID 980419; https://dx.doi.org/10.1155/2013/980419 K252a inhibits tyrosine phosphorylation of Trk A induced by NGF. PC12 cells were incubated in the presence or absence of 1 ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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. I ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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 to be isolated with this type of bis-indole chemical structure. The chemical structure of staurosporine was elucidated by X-ray analysis of a single crystal and the absolute stereochemical configuration by the same method 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 ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Lestaurtinib
Lestaurtinib (rINN, codenamed CEP-701) is a tyrosine kinase inhibitor structurally related to staurosporine. This semisynthetic derivative of the indolocarbazole K252a was investigated by Cephalon as a treatment for various types of cancer. It is an inhibitor of the kinases fms-like tyrosine kinase 3 ( FLT3), Janus kinase 2 ( JAK2), tropomyosin receptor kinase (''trk'') A (TrkA), TrkB and TrkC. Uses Lestaurtinib has undergone clinical trials for the treatment of various cancers, including pancreatic and prostate cancers, V617F JAK2 positive polycythemia vera and essential thrombocytosis, and refractory neuroblastoma. The most significant effort was invested in developing lestaurtinib for the treatment of acute myelogenous leukemia (AML). 24% of the adult AML-affected population exhibits FLT3 mutations, which are associated with an increased likelihood of relapse and mortality after treatment above the general AML population. FLT3 mutations suppress apoptosis in mutated cells, ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Nanogram
To help compare different orders of magnitude, the following lists describe various mass levels between 10−59 kg and 1052 kg. The least massive thing listed here is a graviton, and the most massive thing is the observable universe. Typically, an object having greater mass will also have greater weight (see mass versus weight), especially if the objects are subject to the same gravitational field strength. Units of mass The table at right is based on the kilogram (kg), the base unit of mass in the International System of Units ( SI). The kilogram is the only standard unit to include an SI prefix (''kilo-'') as part of its name. The ''gram'' (10−3 kg) is an SI derived unit of mass. However, the ''names'' of all SI mass units are based on ''gram'', rather than on ''kilogram''; thus 103 kg is a ''megagram'' (106 g), not a *''kilokilogram''. The ''tonne'' (t) is an SI-compatible unit of mass equal to a megagram (''Mg''), or 103 kg. The unit is in common use for ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
TrkB Antagonists
Tropomyosin receptor kinase B (TrkB), also known as tyrosine receptor kinase B, or BDNF/NT-3 growth factors receptor or neurotrophic tyrosine kinase, receptor, type 2 is a protein that in humans is encoded by the ''NTRK2'' gene. TrkB is a receptor for brain-derived neurotrophic factor (BDNF). Standard pronunciation is "track bee". Function Tropomyosin receptor kinase B is the high affinity catalytic receptor for several "neurotrophins", which are small protein growth factors that induce the survival and differentiation of distinct cell populations. The neurotrophins that activate TrkB are: BDNF (Brain Derived Neurotrophic Factor), neurotrophin-4 (NT-4), and neurotrophin-3 (NT-3).> As such, TrkB mediates the multiple effects of these neurotrophic factors, which includes neuronal differentiation and survival. Research has shown that activation of the TrkB receptor can lead to down regulation of the KCC2 chloride transporter in cells of the CNS. Except for the role of the path ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Protein Kinase Inhibitors
A protein kinase inhibitor is a type of enzyme inhibitor that blocks the action of one or more protein kinases. Protein kinases are enzymes that phosphorylate (add a phosphate, or PO4, group) to a protein and can modulate its function. The phosphate groups are usually added to serine, threonine, or tyrosine amino acids on the protein: most kinases act on both serine and threonine, the tyrosine kinases act on tyrosine, and a number (dual-specificity kinases) act on all three. There are also protein kinases that phosphorylate other amino acids, including histidine kinases that phosphorylate histidine residues. Phosphorylation regulates many biological processes, and protein kinase inhibitors can be used to treat diseases due to hyperactive protein kinases (including mutant or overexpressed kinases in cancer) or to modulate cell functions to overcome other disease drivers. Clinical use Kinase inhibitors such as dasatinib are often used in the treatment of cancer and inflammation. So ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Lactams
A lactam is a cyclic amide, formally derived from an amino alkanoic acid. The term is a portmanteau of the words ''lactone'' + ''amide''. Nomenclature Greek prefixes in alphabetical order indicate ring size: * α-Lactam (3-atom rings) * β-Lactam (4-atom rings) * γ-Lactam (5-atom rings) * δ-Lactam (6-atom rings) * ε-Lactam (7-atom rings) This ring-size nomenclature stems from the fact that a hydrolyzed α-Lactam leads to an α-amino acid and a β-Lactam to a β-amino acid, ''etc''. Synthesis General synthetic methods exist for the organic synthesis of lactams. Beckmann rearrangement Lactams form by the acid-catalyzed rearrangement of oximes in the Beckmann rearrangement. Schmidt reaction Lactams form from cyclic ketones and hydrazoic acid in the Schmidt reaction. Cyclization of amino acids Lactams can be formed from cyclisation of amino acids via the coupling between an amine and a carboxylic acid within the same molecule. Lactamization is most efficient in this wa ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Indole Alkaloids
Indole alkaloids are a class of alkaloids containing a structural moiety of indole; many indole alkaloids also include isoprene groups and are thus called terpene indole or secologanin tryptamine alkaloids. Containing more than 4100 known different compounds, it is one of the largest classes of alkaloids. Many of them possess significant physiological activity and some of them are used in medicine. The amino acid tryptophan is the biochemical precursor of indole alkaloids. History The action of some indole alkaloids has been known for ages. Aztecs used the psilocybin mushrooms which contain alkaloids psilocybin and psilocin. The flowering plant ''Rauvolfia serpentina'' which contains reserpine was a common medicine in India around 1000 BC. Africans used the roots of the perennial rainforest shrub Tabernanthe iboga, Iboga, which contain ibogaine, as a stimulant. An infusion of Calabar bean seeds was given to people accused of crime in Nigeria: its rejection by stomach was regarded ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Journal Of The American Chemical Society
The ''Journal of the American Chemical Society'' is a weekly peer-reviewed scientific journal that was established in 1879 by the American Chemical Society. The journal has absorbed two other publications in its history, the ''Journal of Analytical and Applied Chemistry'' (July 1893) and the ''American Chemical Journal'' (January 1914). It covers all fields of chemistry. Since 2021, the editor-in-chief is Erick M. Carreira (ETH Zurich). In 2014, the journal moved to a hybrid open access publishing model. Abstracting and indexing The journal is abstracted and indexed in Chemical Abstracts Service, Scopus, EBSCO databases, ProQuest databases, Index Medicus/MEDLINE/PubMed, and the Science Citation Index Expanded. According to the ''Journal Citation Reports'', the journal has a 2021 impact factor of 16.383. Editors-in-chief The following people are or have been editor-in-chief: * 1879–1880 – Hermann Endemann * 1880–1881 – Gideon E. Moore * 1881–1882 – Hermann Endemann ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Cyclotraxin B
Cyclotraxin B (CTX-B) is a small (1200 Da) cyclic peptide and highly potent, selective, non-competitive antagonist or negative allosteric modulator of TrkB (IC50 = 0.30 nM), the main receptor of brain-derived neurotrophic factor (BDNF), which itself was derived from BDNF. It crosses the blood-brain-barrier with systemic administration and produces anxiolytic-like effects in animals, though notably not antidepressant-like effects. The compound has also been found to produce analgesic effects in animal models of neuropathic pain. In addition to TrkB, CTX-B has been found to be an allosteric modulator of VEGFR2, one of the receptors of vascular endothelial growth factor Vascular endothelial growth factor (VEGF, ), originally known as vascular permeability factor (VPF), is a signal protein produced by many cells that stimulates the formation of blood vessels. To be specific, VEGF is a sub-family of growth factors, ... (VEGF). See also * Tropomyosin receptor kinase B § A ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
ANA-12
ANA-12 is a selective, small-molecule non-competitive antagonist of TrkB (Kd = 10 nM and 12 μM for the high- and low-affinity sites, respectively), the main receptor of brain-derived neurotrophic factor (BDNF). The compound crosses the blood-brain-barrier and exerts central TrkB blockade, producing effects as early as 30 minutes (~400 nM) and as long as 6 hours (~10 nM) following intraperitoneal injection in mice. It blocks the neurotrophic actions of BDNF without compromising neuron survival. Research ANA-12 produces rapid antidepressant- and anxiolytic-like effects in animal models, the former of which have been elucidated to be mediated by blockade of BDNF signaling in the nucleus accumbens. It has also been found to alleviate methamphetamine-induced depression-like behavior (including anhedonia), behavioral sensitization, and nucleus accumbens neuroplasticity changes with subchronic (14-day) administration in mice, whereas the TrkB agonist 7,8-dihydroxyflavone was inef ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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