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Streptomyces Isolates
''Streptomyces'' isolates have yielded the majority of human, animal, and agricultural antibiotics, as well as a number of fundamental chemotherapy medicines. ''Streptomyces'' is the largest antibiotic-producing genus of Actinomycetota, producing chemotherapy, antibacterial, antifungal, antiparasitic drugs, and immunosuppressants. ''Streptomyces'' isolates are typically initiated with the aerial hyphal formation from the mycelium. Anticancer medicines ''Streptomyces'', yielded the medicines doxorubicin (Doxil), daunorubicin (DaunoXome), and streptozotocin (Zanosar). Doxorubicin is the precursor to valrubicin (Valstar), myocet, and pirarubicin. Daunorubicin is the precursor to idarubicin (Idamycin), epirubicin (Ellence), and zorubicin. ''Streptomyces'' is the original source of dactinomycin (Cosmegen), bleomycin (Blenoxane), pingyangmycin (Bleomycin A5), mitomycin C (Mutamycin), rebeccamycin, staurosporine (precursor to stauprimide and midostaurin), neothramycin, aclarubicin, t ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Streptomyces
''Streptomyces'' is the largest genus of Actinomycetota and the type genus of the family Streptomycetaceae. Over 500 species of ''Streptomyces'' bacteria have been described. As with the other Actinomycetota, streptomycetes are gram-positive, and have genomes with high GC content. Found predominantly in soil and decaying vegetation, most streptomycetes produce spores, and are noted for their distinct "earthy" odor that results from production of a volatile metabolite, geosmin. Streptomycetes are characterised by a complex secondary metabolism. They produce over two-thirds of the clinically useful antibiotics of natural origin (e.g., neomycin, streptomycin, cypemycin, grisemycin, bottromycins and chloramphenicol). The antibiotic streptomycin takes its name directly from ''Streptomyces''. Streptomycetes are infrequent pathogens, though infections in humans, such as mycetoma, can be caused by '' S. somaliensis'' and '' S. sudanensis'', and in plants can be caused by '' S. cavi ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Dactinomycin
Dactinomycin, also known as actinomycin D, is a chemotherapy medication used to treat a number of types of cancer. This includes Wilms tumor, rhabdomyosarcoma, Ewing's sarcoma, trophoblastic neoplasm, testicular cancer, and certain types of ovarian cancer. It is given by injection into a vein. Most people develop side effects. Common side effects include bone marrow suppression, vomiting, mouth ulcers, hair loss, liver problems, infections, and muscle pains. Other serious side effects include future cancers, allergic reactions, and tissue death at the site of injection. Use in pregnancy may harm the baby. Dactinomycin is in the cytotoxic antibiotic family of medications. It is believed to work by blocking the creation of RNA. Dactinomycin was approved for medical use in the United States in 1964. It is on the World Health Organization's List of Essential Medicines. Medical use Actinomycin is a clear, yellowish liquid administered intravenously and most commonly used in tre ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Macroketone
Macroketones are macrocyclic compounds that contain a ketone functional group. Macroketones form the central rings systems of some synthetic polyketide antibiotic An antibiotic is a type of antimicrobial substance active against bacteria. It is the most important type of antibacterial agent for fighting bacterial infections, and antibiotic medications are widely used in the treatment and prevention of ...s.; * References {{reflist Ketones Macrocycles ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Isomigrastatin
Isomigrastatin is an analogue of migrastatin, an organic compound that naturally occurs in the '' Streptomyces platensis'' bacteria. Isomigrastatin has shown promise as a drug in the treatment of cancer Cancer is a group of diseases involving abnormal cell growth with the potential to invade or spread to other parts of the body. These contrast with benign tumors, which do not spread. Possible signs and symptoms include a lump, abnormal b .... A laboratory synthesis was reported in 2007. Synthesis Total synthesis Migrastatin synthesis is a precursor of isomigrastatin. In order to synthesize isomigrastatin, reagent 11 and 15 need to be prepared. Through LACDAC reaction, Luche reduction, aqueous Ferrier rearrangement and Epoxidation, reagent 6, 7, 8, 9, 10 are synthesized to 11. Aldehyde 12 reacts is alkyldenated by Witting reagent 13 to make 14, and 14 is hydrogenated to afford 15. Fragment coupling of intermediate 11 and 15 would be the next step. Using lithium borohy ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Migrastatin
Migrastatin is an organic compound which naturally occurs in the '' Streptomyces platensis'' bacteria. Migrastatin and several of its analogues (including Isomigrastatin) have shown to have potential in treating cancer, as it inhibits the metastasis Metastasis is a pathogenic agent's spread from an initial or primary site to a different or secondary site within the host's body; the term is typically used when referring to metastasis by a cancerous tumor. The newly pathological sites, then ... of cancer cells. References Macrolides Glutarimides Alcohols Methoxy compounds Ketones {{organic-compound-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Sibiromycin
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Sibiromycin is an antitumor antibiotic with the molecular formula C24H33N3O7 which is produced by the bacterium '' Streptosporangium sibiricum''. Sibiromycin is a pyrrolobenzodiazepine. References Further reading * * * antibiotics Sibiromycin Sibiromycin is an antitumor antibiotic with the molecular formula C24H33N3O7 which is produced by the bacterium '' Streptosporangium sibiricum''. Sibiromycin is a pyrrolobenzodiazepine Pyrrolobenzodiazepines, (PBD) are a class of compound that m ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Aclarubicin
Aclarubicin (INN) or aclacinomycin A is an anthracycline drug that is used in the treatment of cancer. Soil bacteria '' Streptomyces galilaeus'' can produce aclarubicin. It can induce histone eviction from chromatin Chromatin is a complex of DNA and protein found in eukaryotic cells. The primary function is to package long DNA molecules into more compact, denser structures. This prevents the strands from becoming tangled and also plays important roles in r ... upon intercalation. References Anthracyclines Topoisomerase inhibitors {{antineoplastic-drug-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Neothramycin
Neothramycin A and B Neothramycin A and B are stereoisomeric antibiotics with anticancer activity. The stereoisomers are interchangeable in aqueous solution and the antibiotic, Neothramycin, contains both in approximately equal amounts. They belong to the pyrrolo(1,4)benzodiazepine, or anthramycin, group which includes other antibiotics such as anthramycin, tomaymycin, and sibiromycin. Neothramycin was originally isolated from Streptomyces No. MC916-C4, a cycloheximide-producing strain, by Umezawa et al. Subsequent testing has shown its capabilities as an anticancer drug, antiprotozoal drug, and even possible uses in DNA fluorescence based assays. Its activities against cancer warranted phase I testing of the drug. More recently, in 1991, anthramycin derivatives, which are very similar to neothramycin, have been investigated for their ability to link DNA when dimerized. These compounds were tested using a fluorescence based assay. These compounds showed an ability to bind dG-contai ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Midostaurin
Midostaurin, sold under the brand name Rydapt & Tauritmo both 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 mastocytosis. It is a semi-synthetic derivative of staurosporine, an alkaloid from the bacterium ''Streptomyces staurosporeus''. The U.S. Food and Drug Administration (FDA) considers it to be a first-in-class medication. AML and MDS Midostaurin was found to be active against oncogenic CD135 (FMS-like tyrosine kinase 3 receptor, FLT3), in preclinical studies. Clinical trials have primarily focused on relapsed/refractory AML and MDS and have included single agent and combination agent studies. After successful Phase II clinical trials, midostaurin was found to prolong survival of FLT3-mutated AML patients when combined with conventional induction and consolidation therapies in a randomized Phase III clinical trial. On April 28, 2017, ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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 & Tauritmo both 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 sys ... References {{reflist Indolocarbazoles Protein kinase inhibitors ... [...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] |
Rebeccamycin
Rebeccamycin (NSC 655649) is a weak topoisomerase I inhibitor isolated from ''Nocardia sp.'' It is structurally similar to staurosporine, but does not show any inhibitory activity against protein kinases. It shows significant antitumor properties in vitro (IC50=480nM against mouse B16 melanoma cells and IC50=500nM against P388 The NCI-60 cancer cell line panel is a group of 60 human cancer cell lines used by the National Cancer Institute (NCI) for the screening of compounds to detect potential anticancer activity. Purpose The screening procedure is called the NCI- ... leukemia cells). It is an antineoplastic antibiotic and an intercalating agent. Becatecarin (BMS-181176) is a synthetic analog of rebeccamycin. Rebeccamycin and becatecarin have been tested in phase II clinical trials for the treatment of lung cancer, liver cancer, breast cancer, lymphoma, retinoblastoma, kidney cancer, and ovarian cancer. References Further reading * * * * * Experimental can ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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