Aphidicolin
Mostrando 1-12 de 250 artigos, teses e dissertações.
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1. The semisynthetic landscape of aphidicolin: inspiration towards leishmanicidal compounds
Recentes estudos demonstraram que afidicolina, metabólito secundário do fungo endofítico Nigrospora sphaerica, apresenta alta atividade contra o protozoário Leishmania major. Apesar do promissor potencial leishmanicida, a afidicolina apresenta propriedades físico-químicas e perfil farmacocinético inadequado para terapêutica. Neste sentido, uma revis�
J. Braz. Chem. Soc.. Publicado em: 2014-10
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2. Biosynthesis of aphidicolin proceeds via the mevalonate pathway in the endophytic fungus Nigrospora sphaerica
Previamente o fungo endofítico Nigrospora sphaerica foi identificado como um profícuo produtor do diterpeno bioativo afidicolina. Neste artigo foi realizado um estudo a fim de se verificar as melhores condições para a produção do diterpeno em meio Czapek. A fonte de açúcar (glicose e sacarose) e o tempo de incubação (4-15 dias) foram otimizados, pa
Journal of the Brazilian Chemical Society. Publicado em: 2011-01
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3. Obtenção de derivados dos terpenos enidrina e afidicolina por biotransformação e semi-síntese e avaliação da atividade leishmanicida / Obtainment of aphidicolin and enhydrin derivatives through biotransformation and semi-synthesis and evaluation of leishmanical activity.
Biotransformações são reações de compostos orgânicos realizadas por microrganismos, plantas ou enzimas isoladas. A transformação de um composto em particular pode ser realizada em grupos funcionais com ou sem degradação de seu esqueleto. Neste trabalho foram utilizados fungos endofíticos e de solo na biotransformação da lactona sesquiterpênica
Publicado em: 2010
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4. Fragility in the 14q21q translocation region
Aphidicolin (APC)-induced chromosomal breakage was analyzed for women representing three generations of a single family and carrying a Robertsonian translocation rob(14q21q). Fluorescence in situ hybridization (FISH) analysis confirmed the dicentric constitution of the derived chromosome and indicated the absence of beta-satellite signal at the translocation
Genetics and Molecular Biology. Publicado em: 2002
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5. Mutations in the herpes simplex virus DNA polymerase gene conferring hypersensitivity to aphidicolin.
Fourteen mutants known or likely to contain mutations in the herpes simplex virus DNA polymerase gene were examined for their sensitivity to aphidicolin in plaque reduction assays. Eleven of these exhibited some degree of hypersensitivity to the drug; altered aphidicolin-sensitivity correlated with altered sensitivity to the pyrophosphate analog, phosphonoac
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6. Effect of aphidicolin on vaccinia virus: isolation of an aphidicolin-resistant mutant.
Vaccinia virus growth in BSC-1 and HeLa cells was inhibited by aphidicolin concentrations of 20 microM or more. Virus yield, which decreased only when the drug was added early in infection, was reduced several 100-fold by 80 microM aphidicolin. Viral inhibition was reversed by the suspension of the infected cells in drug-free medium. DNA synthesis in uninfec
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7. Adenovirus DNA synthesized in the presence of aphidicolin.
Adenovirus types 2 and 5 DNA synthesized in vivo and in vitro in the presence of aphidicolin were studied. Inhibition of adenoviral DNA synthesis by aphidicolin was only 70% even at a concentration of 30 micrograms/ml of aphidicolin, at which the cellular DNA synthesis was completely inhibited. When initiation of the viral DNA synthesis was synchronized with
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8. Inhibition of DNA polymerase alpha by aphidicolin derivatives.
17-Acetylaphidicolin was 10-fold weaker and two derivatives lacking hydroxyl groups at the 16 and 17 positions were 100-fold weaker than aphidicolin as inhibitors of DNA polymerase alpha from HeLa and Chinese hamster ovary cells. 17,18-Diacetyl, 3,17,18-triacetyl and 3-epi derivatives of aphidicolin were inactive. Active compounds were, like aphidicolin, com
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9. Aphidicolin inhibits DNA synthesis by DNA polymerase alpha and isolated nuclei by a similar mechanism.
Aphidicolin is a selective inhibitor of DNA polymerase alpha. In contrast to earlier reports, the drug was found to inhibit DNA synthesis catalyzed by DNA polymerase alpha and isolated HeLa cell nuclei by a similar mechanism. For both systems aphidicolin primarily competed with dCTP incorporation. However, the apparent Vmax for dCTP incorporation was reduced
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10. Aphidicolin inhibits the synthesis and joining of short DNA fragments but not the union of 10-kilobase DNA replication intermediates.
DNA replication intermediates in human melanoma cells have been investigated by using the drug aphidicolin, which inhibits DNA polymerase alpha. In untreated cells, Okazaki fragments and 10-kilobase (kb) DNA intermediates are formed. In aphidicolin-treated cells, the replication fork is stopped and there is no formation of DNA replication intermediates. Howe
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11. Structure-activity relationships for the inhibition of DNA polymerase alpha by aphidicolin derivatives.
Aphidicolin and 17 derivatives that have been structurally modified in the A- and D-rings were assessed for their ability to inhibit DNA polymerase alpha. No derivative surpassed the activity of aphidicolin; derivatives with structural alterations in the A-ring exhibited significantly greater loss of activity relative to derivatives with structural alteratio
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12. Aphidicolin inhibits growth and DNA synthesis in halophilic arachaebacteria.
Aphidicolin, a specific inhibitor of eucaryotic alpha DNA polymerase, inhibits the growth of halophilic arachaebacteria. In Halobacterium halobium, aphidicolin prevents cell division and DNA synthesis. These results suggest that arachaebacterial replicases are of the eucaryotic type.