Aurodox: Antibiotic obtained from a Streptomyces variant considered as possibly effective against Streptococcus pyogenes infections. It may promote growth in poultry.Pyridones: Pyridine derivatives with one or more keto groups on the ring.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.Micelles: Particles consisting of aggregates of molecules held loosely together by secondary bonds. The surface of micelles are usually comprised of amphiphatic compounds that are oriented in a way that minimizes the energy of interaction between the micelle and its environment. Liquids that contain large numbers of suspended micelles are referred to as EMULSIONS.Dioctyl Sulfosuccinic Acid: All-purpose surfactant, wetting agent, and solubilizer used in the drug, cosmetics, and food industries. It has also been used in laxatives and as cerumenolytics. It is usually administered as either the calcium, potassium, or sodium salt.Drug Carriers: Forms to which substances are incorporated to improve the delivery and the effectiveness of drugs. Drug carriers are used in drug-delivery systems such as the controlled-release technology to prolong in vivo drug actions, decrease drug metabolism, and reduce drug toxicity. Carriers are also used in designs to increase the effectiveness of drug delivery to the target sites of pharmacological actions. Liposomes, albumin microspheres, soluble synthetic polymers, DNA complexes, protein-drug conjugates, and carrier erythrocytes among others have been employed as biodegradable drug carriers.Hydrophobic and Hydrophilic Interactions: The thermodynamic interaction between a substance and WATER.Polymers: Compounds formed by the joining of smaller, usually repeating, units linked by covalent bonds. These compounds often form large macromolecules (e.g., BIOPOLYMERS; PLASTICS).Patents as Topic: Exclusive legal rights or privileges applied to inventions, plants, etc.Polyethylene Glycols: Polymers of ETHYLENE OXIDE and water, and their ethers. They vary in consistency from liquid to solid depending on the molecular weight indicated by a number following the name. They are used as SURFACTANTS, dispersing agents, solvents, ointment and suppository bases, vehicles, and tablet excipients. Some specific groups are NONOXYNOLS, OCTOXYNOLS, and POLOXAMERS.

Conformational change of elongation factor Tu (EF-Tu) induced by antibiotic binding. Crystal structure of the complex between EF-Tu.GDP and aurodox. (1/16)

Aurodox is a member of the family of kirromycin antibiotics, which inhibit protein biosynthesis by binding to elongation factor Tu (EF-Tu). We have determined the crystal structure of the 1:1:1 complex of Thermus thermophilus EF-Tu with GDP and aurodox to 2.0-A resolution. During its catalytic cycle, EF-Tu adopts two strikingly different conformations depending on the nucleotide bound: the GDP form and the GTP form. In the present structure, a GTP complex-like conformation of EF-Tu is observed, although GDP is bound to the nucleotide-binding site. This is consistent with previous proposals that aurodox fixes EF-Tu on the ribosome by locking it in its GTP form. Binding of EF-Tu.GDP to aminoacyl-tRNA and mutually exclusive binding of kirromycin and elongation factor Ts to EF-Tu can be explained on the basis of the structure. For many previously observed mutations that provide resistance to kirromycin, it can now be understood how they prevent interaction with the antibiotic. An unexpected feature of the structure is the reorientation of the His-85 side chain toward the nucleotide-binding site. We propose that this residue stabilizes the transition state of GTP hydrolysis, explaining the acceleration of the reaction by kirromycin-type antibiotics.  (+info)

Induction of resistance to aurodox by aurodox in the antibiotic-producing culture, Streptomyces goldiniensis. (2/16)

The sensitivity of protein and aurodox synthesis to aurodox was examined in relationship to the development of resistance to aurodix on Streptomyces goldiniensis during fermentation. It was found that the culture remains sensitive to the antibiotic as long as no aurodox is present in the medium. Resistance only develops when aurodox is present, either exogenously added or endogenously synthesized by the culture. These observations suggest that the development of resistance is an inducible process, and evidence is presented indicating that aurodox induces a specific resistance system in S. goldiniensis.  (+info)

A83016F, a new member of the aurodox family. (3/16)

A new member of the aurodox family of antibiotics, A83016F, has been isolated from an unidentified actionmycete designated A83016. The structure and relative stereochemistry of A83016F were elucidated by NMR examination of the parent compound and its diacetate derivative. A83016F exhibits only weak antimicrobial activity.  (+info)

Comparison of the Tu elongation factors from Staphylococcus aureus and Escherichia coli: possible basis for elfamycin insensitivity. (4/16)

In a previous study (C. C. Hall, J. D. Watkins, and N. H. Georgopapadakou, Antimicrob. Agents Chemother. 33:322-325, 1989), the elongation factor Tu (EF-Tu) from Staphylococcus aureus was found to be insensitive to a series of kirromycin analogs which were inhibitory to the EF-Tu from Escherichia coli. In the present study, the EF-Tu from S. aureus was partially purified and characterized. Its apparent molecular mass was approximately 41,000 Da, and the enzyme copurified with EF-Ts (molecular mass, 34,000 Da). S. aureus EF-Tu differed from its E. coli counterpart in that it bound negligible amounts of [3H]GDP, in addition to being insensitive to pulvomycin and aurodox (50% inhibitory concentrations, approximately 100 and 1,000 microM, respectively, versus 2 and 0.2 microM, respectively, for E. coli). The results are consistent with the formation of a stable EF-Tu.EF-Ts complex that affects the interaction of EF-Tu with guanine nucleotides and inhibitors.  (+info)

The structure of heneicomycin. (5/16)

The antibiotic heneicomycin (1), C44H62N2O11, was isolated from cultures of Streptomyces filipinensis as an amorphous yellow powder. Mass spectral and NMR analysis showed the compound to be a deoxy modification of aurodox (2), a member of the elfamycin antibiotic family. A marked change in mass spectral fragmentation compared to aurodox and 1H NMR couplings indicated the absence of the hydroxyl at position 30 of aurodox (position 3 of the tetrahydropyran).  (+info)

Antibiotic SB22484: a novel complex of the aurodox group. I. Taxonomy of the producing organism, isolation of the antibiotics and chemical and biological characterization. (6/16)

Antibiotic SB22484 is a novel member of the aurodox type antibiotic group produced in submerged-fermentation cultures of Streptomyces sp. NRRL 15496. The antibiotic complex is composed of two pairs of isomers with MW's of 752 and 766. The individual isomers, which were separated by preparative HPLC, equilibrate to a mixture of the isomer pair when left in aqueous solution. In vitro, SB22484 antibiotics strongly inhibited neisseriae and were also active against Streptococci, Ureaplasma urealyticum and Haemophilus influenzae.  (+info)

Antibiotic SB22484: a novel complex of the aurodox group. II. Structure elucidation of the four factors. (7/16)

SB22484, active against Neisseriae gonorrhoeae and Neisseriae meningitidis, is a complex of four factors, designed 1 through 4, which from two pairs of isomers, 1 and 3, and 2 and 4. Factors 1 and 3 account for 65% of the complex, factor 3 being the predominant one. On the basis of the existing and implemented correlations between structure and physico-chemical characteristics (UV and IR spectroscopies, ionization properties, MS as FAB and as negative and positive CI, 1H NMR spectroscopy as 2D COSY and NOESY) in the aurodox field, the complete structures were assigned. Factor 3 can be described as N-[7-[5(R)-[7-[1,2-dihydro-4-hydroxy-1H-2-oxo-3-pyridinyl]-6-methyl- 7-oxo-1(E),3(E),5(E)-heptatrienyl]tetrahydro-3(S),4(R)-dihydrox yfuran-2 (S)-yl]-6(S)-methoxy-5,7(R)-dimethyl-2(E),4(E)-heptadienyl]-alpha (S)-methyl-5(S)-methyltetrahydro-2(S),4(S or R)-dihydroxy-6(S)-[1(E), 3(Z)-pentadienyl]-2H-pyran-2-acetamide. Factor 1 is an epimer of factor 3 with the opposite configuration at the anomeric center. Factors 2 and 4 have an ethyl group instead of the methyl group alpha to the acetamide moiety and are in the same stereochemical relationship as the pair 1 and 3.  (+info)

Effects of elfamycins on elongation factor Tu from Escherichia coli and Staphylococcus aureus. (8/16)

Six kirromycin analogs (elfamycins) were compared on the basis of their inhibition of Escherichia coli poly(U)-directed poly(Phe) synthesis and stimulation of elongation factor Tu (EF-Tu)-associated GTPase activity. The elfamycins tested were kirromycin, aurodox, efrotomycin, phenelfamycin A, unphenelfamycin, and L-681,217. The last three lack the pyridone ring present in the other elfamycins. All the elfamycins inhibited poly(U)-dependent poly(Phe) synthesis and stimulated EF-Tu-associated GTPase activity, suggesting that the pyridone ring is not essential for activity. The six elfamycins were also examined in a poly(U)-directed, poly(Phe)-synthesizing system derived from Staphylococcus aureus and had 50% inhibitory concentrations of greater than or equal to 1 mM. When S. aureus ribosomes and E. coli elongation factors were combined in a hybrid poly(Phe)-synthesizing system, aurodox produced essentially complete inhibition of poly(Phe) synthesis with a 50% inhibitory concentration of 0.13 microM. This suggests that the observed high MICs of kirromycin and its congeners in S. aureus reflect a kirromycin-resistant EF-Tu rather than permeability constraints.  (+info)

There is a lack of functional group diversity in the reverse turn motifs nucleating a β-sheet conformation in designed peptides, proteins and foldamers. The majority of these sequences consist of d-Pro-l-Pro, d-Pro-Gly or Asn-Gly as the turn inducing motif restricting their biological application and physico
UOP LLC, a Honeywell Company, Ford Motor Company, and Striatus, Inc., collaborated with Professor Craig Jensen of the University of Hawaii and Professor Vidvuds Ozolins of University of California, Los Angeles on a multi-year cost-shared program to discover novel complex metal hydrides for hydrogen storage. This innovative program combined sophisticated molecular modeling with high throughput combinatorial experiments to maximize the probability of identifying commercially relevant, economical hydrogen storage materials with broad application. A set of tools was developed to pursue the medium throughput (MT) and high throughput (HT) combinatorial exploratory investigation of novel complex metal hydrides for hydrogen storage. The assay programs consisted of monitoring hydrogen evolution as a function of temperature. This project also incorporated theoretical methods to help select candidate materials families for testing. The Virtual High Throughput Screening served as a virtual laboratory, calculating
Massey University student Saskia Stachyshyn talks to the Herald about her studies into the effects of caffeine in regards to genetics.
We synthesized and studied the antitumor properties of the novel complex compound 2,5-dihydroxybenzoate molybdenum(VI) with tetraphenylphosphonium as counterion, which also acts as cancer cell growth inhibitor. A novel complex compound, the 2,5-dihydroxybenzoate molybdenum(VI) complex, (PPh4)2[Mo3O6(mu-O)2(2,5-DHBA)2] was synthesized. 1H NMR, 13C NMR, IR, and UV-Vis analyses were used for its molecular characterization. The human leukemia cell lines HL-60 and K562 were tested for their viability by assessing the metabolic activity of cells (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide; MTT), the structural integrity of the cell membrane (Trypan blue assay), and cell proliferation ability (growth curves). We showed that both leukemia cell lines are induced to decreased proliferation efficiency after treatment with the novel complex, compared to 2,5-dihydroxybenzoate, tetraphenyl-phosphonium polyoxomolybdate, or tetraphenylphosphonium chloride as individual entities, in a time- and
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rso:RSc3041 K02358 elongation factor Tu , (GenBank) tuf2; probable elongation factor tu (ef-tu protein) (A) MAKEKFERTKPHVNVGTIGHVDHGKTTLTAAIATVLSSKFGGEAKKYDEIDAAPEEKARG ITINTAHIEYETANRHYAHVDCPGHADYVKNMITGAAQMDGAILVCSAADGPMPQTREHI LLARQVGVPYIIVFLNKCDMVDDAELLELVEMEVRELLSKYDFPGDDTPIIKGSAKLALE GDKGELGEVAIMNLADALDSYIPTPERAVDGTFLMPVEDVFSISGRGTVVTGRIERGIIK VGEEIEIVGIKATQKTTCTGVEMFRKLLDQGQAGDNVGILLRGTKREDVERGQVLCKPGS IKPHTHFTGEVYILSKDEGGRHTPFFNNYRPQFYFRTTDVTGSIELPKDKEMVMPGDNVS ITVKLIAPIAMEEGLRFAIREGGRTVGAGVVAKIIE ...
Principal Investigator:Hasebe Mitsuyasu, Project Period (FY):2010-04-01 - 2016-03-31, Research Category:Grant-in-Aid for Scientific Research on Innovative Areas (Research in a proposed research area), Project Area:Genetic bases for the evolution of complex adaptive traits
1HA3: Conformational Change of Elongation Factor TU Induced by Antibiotic Binding: Crystal Structure of the Complex between EF-TU:Gdp and Aurodox
Aurodox. Not Available. DB04348. Taurocholic Acid. Not Available. DB04796. Inecalcitol. Investigated for use/treatment in ...
Aurodox is a specialized metabolite of streptomyces goldiniensis discovered in 1973.. T3SSs play a central role in the ... The study, published in Infection and Immunity, looks at how the aurodox was able to block E. coli O157 infections. The ... Researchers suggested a model in which aurodox acts upstream of Ler and not directly on the T3SS itself. The T3SS of EHEC and ... The team found that Aurodox resulted in a concentration dependent inhibition of T3S in EPEC, EHEC and C. rodentium and at the ...
... aurodox, aurothioglycanide, 8-azaguanine, azobenzene; baicalein, Balsam Peru, Balsam Tolu, barban, baxtrobin, bendazac, ...
Effects of nucleotide-and aurodox-induced changes in elongator factor Tu conformation upon its interactions with aminoacyl ...
... aurodox MeSH D02.455.326.271.665.250 --- diphenylhexatriene MeSH D02.455.326.271.665.325 --- filipin MeSH D02.455.326.271. ...
The Aurodox compound was able to reduce the ability of E. coli O157 to bind to human cells and, unlike traditional antibiotics ... The new study, published in Infection and Immunity, found that Aurodox, a compound first discovered in 1973 but found to be ... We were excited to find that Aurodox was able to prevent the E. coli bacteria from binding to human cells and effectively act ...
The study found that aurodox, a chemical compound that inhibits the biosynthesis of bacterial protein, can block the E. coli ... E. coli O157:H7 treatment may become easier due to aurodox discovery. ... E. coli O157:H7 treatment may become easier due to aurodox discovery ...
Characterization of the mode of action of Aurodox, a type III secretion system inhibitor from streptomyces goldiniensis. McHugh ...
... or aurodox? or azithromycin? or azlocillin? or aztreonam? or bacitracin? or bacteriocin? or bambermycin? or bongkrekic acid? or ...
5C; note the similarity to the conformation seen in the aurodox-bound structure of EF-Tu outside of the ribosome, shown in Fig ... A crystal structure of EF-Tu outside the ribosome, but bound to the antibiotic aurodox that is thought to simulate interaction ...
Funded by the NIH/NCATS Clinical and Translational Science Award (CTSA) program, grant number UL1TR001102, and through institutional support from Harvard University, Harvard Medical School, Harvard T.H. Chan School of Public Health, Beth Israel Deaconess Medical Center, Boston Childrens Hospital, Brigham and Womens Hospital, Massachusetts General Hospital and the Dana Farber Cancer Institute ...
0133-1 Aurodox 1 mg 2703 2.5 mg 5247 12704-90-4. 0134-1 Cyclopenin 1 mg 1272 5 mg 5088 19553-26-5. 0135-1 Fulvic acid 1 mg 1431 ...
Dell VA, Miller DL, Johnson AE: Effects of nucleotide- and aurodox-induced changes in elongation factor Tu conformation upon ...
We show that Aurodox downregulates the expression of the type III secretion systems of enteropathogenic and enterohemorrhagic ... Antibacterianos/farmacologia , Aurodox/farmacologia , Proteínas de Escherichia coli/metabolismo , Escherichia coli/efeitos dos ... Characterization of the Mode of Action of Aurodox, a Type III Secretion System Inhibitor from Streptomyces goldiniensis. ... Recent work has demonstrated that the polyketide natural product Aurodox from Streptomyces goldiniensis is able to block the ...
These studies are focused on naturally occurring pathogenesis inhibitors, including guadinomine B and aurodox, which are both ...
... together with a known polyene with pyridone ring compound aurodox (2). The structures of compounds 1 and 2 were determined by ...
X 5108 use Aurodox X ALD use Adrenoleukodystrophy X ALD (X Linked Adrenoleukodystrophy) use Adrenoleukodystrophy ...
X 5108 use Aurodox X ALD use Adrenoleukodystrophy X ALD (X Linked Adrenoleukodystrophy) use Adrenoleukodystrophy ...
X 5108 use Aurodox X ALD use Adrenoleukodystrophy X ALD (X Linked Adrenoleukodystrophy) use Adrenoleukodystrophy ...
X 5108 use Aurodox X ALD use Adrenoleukodystrophy X ALD (X Linked Adrenoleukodystrophy) use Adrenoleukodystrophy ...
E. coli O157:H7 treatment may become easier due to aurodox discovery ...
Kirromycin (Mocimycin, Delvomycin, MYC 8003, NSC 316094), CAS 50935-71-2, high purity chemical. Isolated from Streptomyces collinus. Antibiotic. Antibacterial. Protein biosynthesis inhibitor.
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