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Showing 1 to 16 of 16 for “"geldanamycin"”.
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Biosynthetic Studies on Geldanamycin and Pactamycin
The formation of the m-C(,7)N units of geldanamycin and pactamycin via the shikimate pathway was studied. {('13)C(,6)}glucose was used to determine the incorporation of intact carbon units into both molecules. This revealed that the respective m-C(,7)N units were derived from three-carbon and …
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Structural and Synthetic Studies of the Antibiotics Lomofungin and Geldanamycin
Made available in DSpace on 2014-12-10T23:01:14Z (GMT). No. of bitstreams: 1 7207089.pdf: 5598962 bytes, checksum: 98ab6881b049b773698f366a30a9053d (MD5) Previous issue date: 1971
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Total Syntheses of (+)-Geldanamycin, (-)-Ragaglitazar, and (+)-Kurasoin A and Phase-Transfer-Catalyzed Asymmetric Alkylation
<p>Geldanamycin possesses various biological activities as seen in the NCI 60 cell line panel (13 nM avg., 70 nM SKBr-3 cells). The predominant mode of action providing these unique results arises from the ability of geldanamycin (GA) to bind to the chaperone heat shock protein 90 (Hsp90). Despite …
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A quantitative study of the relationships between morphology, physiology and geldanamycin synthesis in submerged cultures of Streptomyces hygroscopicus var. geldanus
… var. geldanus produces the secondary metabolite geldanamycin, a novel chemotherapeutic compound, in submerged fermentation. This organism represents an ideal system for experimentation in order to elucidate the relationships between morphology, physiology and secondary metabolite production. The …
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Synthesis of Resveratrol and Its Analogs, Phase-Transfer Catalyzed Asymmetric Glycolate Aldol Reaction, and Total Synthesis of 8,9-Methylamido-Geldanamycin
… A novel unnatural product, 8,9-Methylamido-Geldanamycin, has been designed and synthesized. Using a convergent route, the total synthesis of the molecule involved only 27 longest linear steps. New synthesis methodologies, including auxiliary controlled asymmetric anti-glycolate aldol, …
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"Clostridium botulinum" C2-Toxin: Interaktion der Toxinkomponenten und Translokation der Enzymkomponente in das Zytosol von Zielzellen
… der spezifischen zellgängigen Hsp90-Inhibitoren Geldanamycin und Radicicol gezeigt. Geldanamycin und Radicicol verzögerten die Vergiftung von Vero-Zellen durch C2-Toxin und schützten das zelluläre Aktin vor ADP-Ribosylierung. Die Inhibitoren hatten keinen Einfluss auf die ADP-Ribosylierung von …
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Part I. Carbon-13 and Carbon-14 Biosynthetic Study of Geldanamycin. Part Ii. Carbon-13 Nuclear Magnetic Resonance Study of Phenazines. Part Iii. Carbon-13 Nuclear Magnetic Resonance Study of Pactamycin
Made available in DSpace on 2014-12-13T20:10:11Z (GMT). No. of bitstreams: 1 7804012.pdf: 10622405 bytes, checksum: 90f99bcf7d45ea611612f521ab6e463d (MD5) Previous issue date: 1977
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Charakterisierung von Schlüsselproteinen der Signaltransduktion (EGF-R, c-erbB2, Hsp90) in humanen Tumorxenografts mittels Gewebemikroarray
… Antikörper EMD72000 wurden entwickelt. Das Geldanamycin Derivat 17-AAG (17-allylamino-geldanamycin) befindet sich in klinischer Phase Studien in England und den USA. Es hemmt die Interaktion des Hsp90 mit anderen Proteinen. <br> <br>In der vorliegenden Arbeit wurden Schlüsselproteine der …
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Liquid-core microcapsules: A mechanism for the recovery and purification of selected molecules in different environments
… the recovery and purification of the antibiotic geldanamycin from Bennett’s medium. From this work it was shown how a small quantity of capsules was capable of rapidly extracting the molecule from the culture medium. Again the limitations to mass transfer were accessed, and it was discovered that …
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Onkogenomische Aspekte Zytokin-assoziierter Signaltransduktion
… dass die Hemmung des Chaperon HSP90 durch das Geldanamycin-Derivat 17-AAG oder RNA-Interferenz gegen HSP90 zu einer Hemmung des Jak-STAT-Signalwegs einhergehend mit einer reduzierten Proliferation der cHL-Zellen führt. Im zweiten Teil der Arbeit konnten durch Genexpressionsanalysen Zielgene von …
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Development and Application of Covalent-Labeling Strategies for the Large-Scale Thermodynamic Analysis of Protein Folding and Ligand Binding
… study included the well-known Hsp90 inhibitor geldanamycin and the less well-understood omeprazole sulfide that inhibits liver-stage malaria. In addition to protein-small molecule interactions, protein-protein interactions involving Puf6 were investigated using the SPROX technique in …
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Novel Cancer Therapeutics, the Generation of ROS, and Cell Survival
… have potential in the treatment of RCC and GBM. Geldanamycins are currently being used in a number of clinical trials in different tumor cell types, such as hepatocellular carcinoma (HCC), targeting the inhibition of the heat shock protein and molecular chaperone Hsp90. Previous studies have …
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Inhibition of Heat Shock Protein 90 Reduces Inflammatory Signal Transduction in Murine J774 Macrophage Cells and Lessens Disease in Autoimmune MRL/lpr Mice: What in vitro, in vivo, and in silico Models Reveal
… of investigation. The HSP90 inhibitors such as geldanamycin (GA) and its derivative 17-dimethylaminoethylamino-17-demethoxygeldanamycin (17-DMAG) have been shown to reduce inflammation. It was hypothesized that inhibiting HSP90 would reduce inflammatory signal cascade levels. To test this, J774 …
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Mechanism-Based Strategies to Enhance The Actions of A
… driven by the binding and hydrolysis of ATP. The geldanamycin analog, 17-AAG, binds to the ATP pocket of HSP90 leading to the degradation of client proteins. However, treatment with 17-AAG results in the elevation of the levels of antiapoptotic proteins HSP70 and HSP27, which may lead to cell …
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Development and Application of Large-Scale Protein Folding Stability Analysis in Drug Target Identification and Disease Biomarker Discovery
… two well-studied drugs, cyclosporin A and geldanamycin. The STEPP-LiP workflow was evaluated in one proof-of-principle experiment on identification of protein conformational changes between a breast cancer cell line, MCF-7, and a normal cell line, MCF-10A. The STEPP protocol increased the …