Benzoquinones: Benzene rings which contain two ketone moieties in any position. They can be substituted in any position except at the ketone groups.Lactams, Macrocyclic: LACTAMS forming compounds with a ring size of approximately 1-3 dozen atoms.Quinones: Hydrocarbon rings which contain two ketone moieties in any position. They can be substituted in any position except at the ketone groups.Rifabutin: A broad-spectrum antibiotic that is being used as prophylaxis against disseminated Mycobacterium avium complex infection in HIV-positive patients.HSP90 Heat-Shock Proteins: A class of MOLECULAR CHAPERONES whose members act in the mechanism of SIGNAL TRANSDUCTION by STEROID RECEPTORS.Chloranil: A quinone fungicide used for treatment of seeds and foliage.Aziridines: Saturated azacyclopropane compounds. They include compounds with substitutions on CARBON or NITROGEN atoms.HydroquinonesRifamycins: A group of ANTI-BACTERIAL AGENTS characterized by a chromophoric naphthohydroquinone group spanned by an aliphatic bridge not previously found in other known ANTI-BACTERIAL AGENTS. They have been isolated from fermentation broths of Streptomyces mediterranei.Aminobenzoates: Derivatives of BENZOIC ACID that contain one or more amino groups attached to the benzene ring structure. Included under this heading are a broad variety of acid forms, salts, esters, and amides that include the aminobenzoate structure.Ubiquinone: A lipid-soluble benzoquinone which is involved in ELECTRON TRANSPORT in mitochondrial preparations. The compound occurs in the majority of aerobic organisms, from bacteria to higher plants and animals.Antibiotics, Antineoplastic: Chemical substances, produced by microorganisms, inhibiting or preventing the proliferation of neoplasms.Benzene: Toxic, volatile, flammable liquid hydrocarbon byproduct of coal distillation. It is used as an industrial solvent in paints, varnishes, lacquer thinners, gasoline, etc. Benzene causes central nervous system damage acutely and bone marrow damage chronically and is carcinogenic. It was formerly used as parasiticide.NAD(P)H Dehydrogenase (Quinone): A flavoprotein that reversibly catalyzes the oxidation of NADH or NADPH by various quinones and oxidation-reduction dyes. The enzyme is inhibited by dicoumarol, capsaicin, and caffeine.Arachnida: A class of Arthropoda that includes SPIDERS; TICKS; MITES; and SCORPIONS.Naphthoquinones: Naphthalene rings which contain two ketone moieties in any position. They can be substituted in any position except at the ketone groups.Azirines: Unsaturated azacyclopropane compounds that are three-membered heterocycles of a nitrogen and two carbon atoms.Molecular Structure: The location of the atoms, groups or ions relative to one another in a molecule, as well as the number, type and location of covalent bonds.Leukemia L5178: An experimental lymphocytic leukemia of mice.Triaziquone: Alkylating antineoplastic agent used mainly for ovarian tumors. It is toxic to skin, gastrointestinal tract, bone marrow and kidneys.Terphenyl Compounds: Compounds consisting of benzene rings linked to each other in either ortho, meta or para positions. Permitted are any substitutions, but ring fusion to any of the benzene rings is not allowed.Hydroxybenzoates: Benzoate derivatives substituted by one or more hydroxy groups in any position on the benzene ring.Aniline Mustard: Alkylating anti-neoplastic agent.Streptomyces: A genus of bacteria that form a nonfragmented aerial mycelium. Many species have been identified with some being pathogenic. This genus is responsible for producing a majority of the ANTI-BACTERIAL AGENTS of practical value.ResorcinolsOxidation-Reduction: A chemical reaction in which an electron is transferred from one molecule to another. The electron-donating molecule is the reducing agent or reductant; the electron-accepting molecule is the oxidizing agent or oxidant. Reducing and oxidizing agents function as conjugate reductant-oxidant pairs or redox pairs (Lehninger, Principles of Biochemistry, 1982, p471).Cycloaddition Reaction: Synthetic organic reactions that use reactions between unsaturated molecules to form cyclical products.Quinone Reductases: NAD(P)H:(quinone acceptor) oxidoreductases. A family that includes three enzymes which are distinguished by their sensitivity to various inhibitors. EC 1.6.99.2 (NAD(P)H DEHYDROGENASE (QUINONE);) is a flavoprotein which reduces various quinones in the presence of NADH or NADPH and is inhibited by dicoumarol. EC 1.6.99.5 (NADH dehydrogenase (quinone)) requires NADH, is inhibited by AMP and 2,4-dinitrophenol but not by dicoumarol or folic acid derivatives. EC 1.6.99.6 (NADPH dehydrogenase (quinone)) requires NADPH and is inhibited by dicoumarol and folic acid derivatives but not by 2,4-dinitrophenol.Dicumarol: An oral anticoagulant that interferes with the metabolism of vitamin K. It is also used in biochemical experiments as an inhibitor of reductases.Metals, Alkaline Earth: Metals that constitute the group 2 (formerly group IIa) of the periodic table.Basidiomycota: A phylum of fungi that produce their sexual spores (basidiospores) on the outside of the basidium. It includes forms commonly known as mushrooms, boletes, puffballs, earthstars, stinkhorns, bird's-nest fungi, jelly fungi, bracket or shelf fungi, and rust and smut fungi.Sorghum: A plant genus of the family POACEAE. The grain is used for FOOD and for ANIMAL FEED. This should not be confused with KAFFIR LIME or with KEFIR milk product.Polyporaceae: A family of bracket fungi, order POLYPORALES, living in decaying plant matter and timber.Cyclohexanes: Six-carbon alicyclic hydrocarbons.Anti-Bacterial Agents: Substances that reduce the growth or reproduction of BACTERIA.Biotransformation: The chemical alteration of an exogenous substance by or in a biological system. The alteration may inactivate the compound or it may result in the production of an active metabolite of an inactive parent compound. The alterations may be divided into METABOLIC DETOXICATION, PHASE I and METABOLIC DETOXICATION, PHASE II.Alkylation: The covalent bonding of an alkyl group to an organic compound. It can occur by a simple addition reaction or by substitution of another functional group.Micrococcus luteus: A species of gram-positive, spherical bacteria whose organisms occur in tetrads and in irregular clusters of tetrads. The primary habitat is mammalian skin.Catechols: A group of 1,2-benzenediols that contain the general formula R-C6H5O2.Electron Transport Complex II: A flavoprotein oxidase complex that contains iron-sulfur centers. It catalyzes the oxidation of SUCCINATE to fumarate and couples the reaction to the reduction of UBIQUINONE to ubiquinol.Iodoacetamide: An alkylating sulfhydryl reagent. Its actions are similar to those of iodoacetate.Succinate Dehydrogenase: A flavoprotein containing oxidoreductase that catalyzes the dehydrogenation of SUCCINATE to fumarate. In most eukaryotic organisms this enzyme is a component of mitochondrial electron transport complex II.Oxidoreductases: The class of all enzymes catalyzing oxidoreduction reactions. The substrate that is oxidized is regarded as a hydrogen donor. The systematic name is based on donor:acceptor oxidoreductase. The recommended name will be dehydrogenase, wherever this is possible; as an alternative, reductase can be used. Oxidase is only used in cases where O2 is the acceptor. (Enzyme Nomenclature, 1992, p9)Spectrophotometry: The art or process of comparing photometrically the relative intensities of the light in different parts of the spectrum.Phenols: Benzene derivatives that include one or more hydroxyl groups attached to the ring structure.Mass Spectrometry: An analytical method used in determining the identity of a chemical based on its mass using mass analyzers/mass spectrometers.Glutathione: A tripeptide with many roles in cells. It conjugates to drugs to make them more soluble for excretion, is a cofactor for some enzymes, is involved in protein disulfide bond rearrangement and reduces peroxides.HSP70 Heat-Shock Proteins: A class of MOLECULAR CHAPERONES found in both prokaryotes and in several compartments of eukaryotic cells. These proteins can interact with polypeptides during a variety of assembly processes in such a way as to prevent the formation of nonfunctional structures.Polyketide Synthases: Large enzyme complexes composed of a number of component enzymes that are found in STREPTOMYCES which biosynthesize MACROLIDES and other polyketides.
... (development name, AA-2414; marketed originally as Bronica) is a thromboxane A2 (TXA2) receptor (TP receptor) antagonist used primarily in the treatment of asthma. It was the first TP receptor antagonist that was developed as an anti-asthmatic drug and received marketing approval in Japan in 1997. As of 2017 seratrodast was marketed as Bronica in Japan, and as Changnuo, Mai Xu Jia, Quan Kang Nuo in China. Unlike thromboxane synthase inhibitors such as ozagrel, seratrodast does not affect thrombus formation, time to occlusion and bleeding time. Seratrodast has no effect on prothrombin time and activated partial thromboplastin time, thus ruling out any action on blood coagulation cascade. Seratrodast is used to treat asthma. There are no adequate and well-controlled studies of seratrodast in pregnant women. The drug should be used in pregnancy only if the potential benefits justify the risk to the fetus. Seratrodast should not be used during lactation. The safety and efficacy of ...
An Hsp90 inhibitor is a substance that inhibits that activity of the Hsp90 heat shock protein. Since Hsp90 stabilizes a variety of proteins required for survival of cancer cells, these substances may have therapeutic benefit in the treatment of various types of malignancies. Furthermore, a number of Hsp90 inhibitors are currently undergoing clinical trials for a variety of cancers. Hsp90 inhibitors include the natural products geldanamycin and radicicol as well as semisynthetic derivatives 17-N-Allylamino-17-demethoxygeldanamycin (17AAG). Among heat shock proteins the focus on HSP90 has increased due to its involvement in several cellular phenomenon and more importantly in disease progression. HSP90 keeps the death proteins in an apoptosis resistant state by direct association. Its wide range of functions results from the ability of HSP90 to chaperone several client proteins that play a central pathogenic role in human diseases including cancer, neurodegenerative diseases and viral infection. ...
... , also known as ubiquinone, ubidecarenone, coenzyme Q, and abbreviated at times to CoQ10 /ˌkoʊˌkjuːˈtɛn/, CoQ, or Q10 is a coenzyme that is ubiquitous in animals and most bacteria (hence the name ubiquinone). It is a 1,4-benzoquinone, where Q refers to the quinone chemical group and 10 refers to the number of isoprenyl chemical subunits in its tail. This fat-soluble substance, which resembles a vitamin, is present in all respiring eukaryotic cells, primarily in the mitochondria. It is a component of the electron transport chain and participates in aerobic cellular respiration, which generates energy in the form of ATP. Ninety-five percent of the human body's energy is generated this way.[1][2] Therefore, those organs with the highest energy requirements-such as the heart, liver, and kidney-have the highest CoQ10 concentrations.[3][4][5] There are three redox states of CoQ10: fully oxidized (ubiquinone), semiquinone (ubisemiquinone), and fully reduced (ubiquinol). The capacity ...
Melanoma (yun. melas - qora, ota - oʻsma maʼnosini anglatuvchi qoʻshimcha), melanoblastoma, melanosarkoma - asosan, teri (baʼzan koʻz toʻr pardasi, miya, shilliq pardalar)dagi xavfli oʻsma; qora pigmentlar - melaninlarni ishlab chiqaradigan hujayralar (odatda tugma dogʻlar)dan paydo boʻladi. M.ga turli shikastlanishlar, gormonlar ishlab chiqarilishining izdan chiqishi va boshqa sabab boʻlishi mumkin (etiologiyasi toʻliq oʻrganilmagan). Asosan, burunhalqum, qiqildoq, qiziloʻngach, ichak shilliq qavatlari, shuningdek, koʻzning toʻr va tomirli pardasi, bosh miya bilan orqa miyaning yumshoq miya pardasida boʻladi. M. nihoyatda xavfli oʻsmalardan hisoblanadi, boshqa aʼzolarga metastaz beradi. Davosi : kimyoterapiya, nur bilan davolash, bular naf bermasa jarrohlik usuli qoʻllanadi.[1] ...
An Hsp90 inhibitor is a substance that inhibits that activity of the Hsp90 heat shock protein. Since Hsp90 stabilizes a variety of proteins required for survival of cancer cells, these substances may have therapeutic benefit in the treatment of various types of malignancies. Furthermore, a number of Hsp90 inhibitors are currently undergoing clinical trials for a variety of cancers. Hsp90 inhibitors include the natural products geldanamycin and radicicol as well as semisynthetic derivatives 17-N-Allylamino-17-demethoxygeldanamycin (17AAG). Among heat shock proteins the focus on HSP90 has increased due to its involvement in several cellular phenomenon and more importantly in disease progression. HSP90 keeps the death proteins in an apoptosis resistant state by direct association. Its wide range of functions results from the ability of HSP90 to chaperone several client proteins that play a central pathogenic role in human diseases including cancer, neurodegenerative diseases and viral infection. ...
... (EC 1.1.99.35, soluble glucose dehydrogenase, sGDH, glucose dehydrogenase (PQQ-dependent)) is an enzyme with systematic name D-glucose:acceptor oxidoreductase. This enzyme catalyses the following chemical reaction D-glucose + acceptor ⇌ {\displaystyle \rightleftharpoons } D-glucono-1,5-lactone + reduced acceptor This soluble periplasmic enzyme contains PQQ as prosthetic group, and is bound to a calcium ion. Electron acceptor is not known. Geiger, O.; Gorisch, H. (1986). "Crystalline quinoprotein glucose dehydrogenase from Acinetobacter calcoaceticus". Biochemistry. 25: 6043-6048. doi:10.1021/bi00368a031. Dokter, P.; Frank, J.; Duine, J.A. (1986). "Purification and characterization of quinoprotein glucose dehydrogenase from Acinetobacter calcoaceticus L.M.D. 79.41". Biochem. J. 239 (1): 163-167. PMC 1147254 . PMID 3800975. Cleton-Jansen, A.M.; Goosen, N.; Wenzel, T.J.; van de Putte, P. (1988). "Cloning of the gene encoding quinoprotein glucose ...
The rifamycins are a group of antibiotics that are synthesized either naturally by the bacterium Amycolatopsis rifamycinica or artificially. They are a subclass of the larger family of ansamycins. Rifamycins are particularly effective against mycobacteria, and are therefore used to treat tuberculosis, leprosy, and mycobacterium avium complex (MAC) infections. The rifamycin group includes the "classic" rifamycin drugs as well as the rifamycin derivatives rifampicin (or rifampin), rifabutin, rifapentine, rifalazil and rifaximin. Streptomyces mediterranei was first isolated in 1957 from a soil sample collected near the beach-side town of St Raphael in southern France. The name was originally given by two microbiologists working with the Italian drug company Group Lepetit SpA in Milan, the Italian Grazia Beretta, and Pinhas Margalith of Israel. In 1969, the bacterium was renamed Nocardia mediterranei when another scientist named Thiemann found that it has a cell wall typical of the Nocardia ...
An Hsp90 inhibitor is a substance that inhibits that activity of the Hsp90 heat shock protein. Since Hsp90 stabilizes a variety of proteins required for survival of cancer cells, these substances may have therapeutic benefit in the treatment of various types of malignancies. Furthermore, a number of Hsp90 inhibitors are currently undergoing clinical trials for a variety of cancers. Hsp90 inhibitors include the natural products geldanamycin and radicicol as well as semisynthetic derivatives 17-N-Allylamino-17-demethoxygeldanamycin (17AAG). Among heat shock proteins the focus on HSP90 has increased due to its involvement in several cellular phenomenon and more importantly in disease progression. HSP90 keeps the death proteins in an apoptosis resistant state by direct association. Its wide range of functions results from the ability of HSP90 to chaperone several client proteins that play a central pathogenic role in human diseases including cancer, neurodegenerative diseases and viral infection. ...
An Hsp90 inhibitor is a substance that inhibits that activity of the Hsp90 heat shock protein. Since Hsp90 stabilizes a variety of proteins required for survival of cancer cells, these substances may have therapeutic benefit in the treatment of various types of malignancies. Furthermore, a number of Hsp90 inhibitors are currently undergoing clinical trials for a variety of cancers. Hsp90 inhibitors include the natural products geldanamycin and radicicol as well as semisynthetic derivatives 17-N-Allylamino-17-demethoxygeldanamycin (17AAG). Among heat shock proteins the focus on HSP90 has increased due to its involvement in several cellular phenomenon and more importantly in disease progression. HSP90 keeps the death proteins in an apoptosis resistant state by direct association. Its wide range of functions results from the ability of HSP90 to chaperone several client proteins that play a central pathogenic role in human diseases including cancer, neurodegenerative diseases and viral infection. ...
... (heat shock protein 90) is a chaperone protein that assists other proteins to fold properly, stabilizes proteins against heat stress, and aids in protein degradation. It also stabilizes a number of proteins required for tumor growth, which is why Hsp90 inhibitors are investigated as anti-cancer drugs. Heat shock proteins, as a class, are among the most highly expressed cellular proteins across all species. As their name implies, heat shock proteins protect cells when stressed by elevated temperatures. They account for 1-2% of total protein in unstressed cells. However, when cells are heated, the fraction of heat shock proteins increases to 4-6% of cellular proteins. Heat shock protein 90 (Hsp90) is one of the most common of the heat-related proteins. The "90" comes from the fact that it weighs roughly 90 kiloDaltons. A 90 kDa protein is considered fairly large for a non-fibrous protein. Hsp90 is found in bacteria and all branches of eukarya, but it is apparently absent in archaea. Whereas ...
A Lewis acid is a chemical species that contains an empty orbital which is capable of accepting an electron pair from a Lewis base to form a Lewis adduct. A Lewis base, then, is any species that has a filled orbital containing an electron pair which is not involved in bonding but may form a dative bond with a Lewis acid to form a Lewis adduct. For example, NH3 is a Lewis base, because it can donate its lone pair of electrons. Trimethylborane (Me3B) is a Lewis acid as it is capable of accepting a lone pair. In a Lewis adduct, the Lewis acid and base share an electron pair furnished by the Lewis base, forming a dative bond.[1] In the context of a specific chemical reaction between NH3 and Me3B, the lone pair from NH3 will form a dative bond with the empty orbital of Me3B to form an adduct NH3•BMe3. The terminology refers to the contributions of Gilbert N. Lewis.[2]. The terms nucleophile and electrophile are more or less interchangeable with Lewis base and Lewis acid, respectively. However, ...
... (BEI) is a preparation of aziridine. It can be produced by heating bromoethylamine hydrobromide or 2-aminoethyl hydrogen sulfate in the presence of sodium hydroxide (Gabriel method). It contains at least one three-membered ring which is very reactive because of the ring strain. It is used to inactivate the foot-and-mouth disease virus in vaccines for cattle, as well as other viruses and mycoplasma in blood samples. Contrary to early assumptions that ethylenimines only modified nucleic acids, it was found that trimeric ethyleimine also alters proteins in virus preparations, especially at higher pH values. The modification of the proteins affected viral particle uptake into cells. This should be taken into consideration when using BEI and other ethyleneimines as well. BEI is very hazardous since it attacks nucleic acids and proteins as described above. It can be neutralised by sodium thiosulfate; the thiosulfate is a nucleophile which opens the three-membered ring. The presence ...
Usually imines refer to compounds with the connectivity R2C=NR, as discussed below. In the older literature, imine refers to the aza analogue of an epoxide. Thus, ethyleneimine is the three-membered ring species C2H4NH.[6]. Imines are related to ketones and aldehydes by replacement of the oxygen with an NR group. When R = H, the compound is a primary imine, when R is hydrocarbyl, the compound is a secondary imine. Imines exhibit diverse reactivity and are commonly encountered throughout chemistry.[4] When R3 is OH, the imine is called an oxime, and when R3 is NH2 the imine is called a hydrazone. A primary imine in which C is attached to both a hydrocarbyl and a H is called a primary aldimine; a secondary imine with such groups is called a secondary aldimine.[7] A primary imine in which C is attached to two hydrocarbyls is called a primary ketimine; a secondary imine with such groups is called a secondary ketimine .[8]. ...
... an ansamycin-derivative benzoquinone compound, was originally isolated as a natural product with anti-fungal activity. Later, ... Geldanamycin, an ansamycin-derivative benzoquinone compound, was originally isolated as a natural product with anti-fungal ... Benzoquinones * HSP90 Heat-Shock Proteins / antagonists & inhibitors* * HSP90 Heat-Shock Proteins / metabolism ...
... we examined the effects of treating different cancer cell lines with the benzoquinone ansamycin 17-allylamino geldanamycin (17- ... Benzoquinones/pharmacology. *CDC2-CDC28 Kinases/metabolism*. *Cell Cycle/drug effects. *Cell Line, Tumor ...
... it has been suggested in several reports that NQO1/DT-diaphorase is necessary for benzoquinone ansamycin function. This enzyme ... Another possibility is that although less potent, the nonreduced benzoquinones may also have an activity and be able to exert ...
... it has been suggested in several reports that NQO1/DT-diaphorase is necessary for benzoquinone ansamycin function. This enzyme ... Another possibility is that although less potent, the nonreduced benzoquinones may also have an activity and be able to exert ...
Purpose: There is currently much interest in developing analogues of the benzoquinone ansamycin geldanamycin that may overcome ... Benzoquinones * Drug Delivery Systems* * Drug Therapy, Combination * Half-Life * In Vitro Techniques ...