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Search results for: ANTIFUNGAL TARGET
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Enzymes of the lysine biosynthetic pathway as targets for antifungals ?
PublicationSystemic infections caused by human pathogenic fungi in immunocompromized patients continue to be one of the important clinical problems. Limited availability of safe and efficacious antifungal chemotherapeutics and emerging resistance to existing drugs stimulates search for novel molecular targets for antifungals. The α-aminoadipate pathway (AAP) of L-lysine biosynthesis is unique in fungi and thus has been so far considered...
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Molecular targets for antifungals in amino acid and protein biosynthetic pathways
PublicationFungi cause death of over 1.5 million people every year, while cutaneous mycoses are among the most common infections in the world. Mycoses vary greatly in severity, there are long-term skin (ringworm), nail or hair infections (tinea capitis), recurrent like vaginal candidiasis or severe, life-threatening systemic, multiorgan infections. In the last few years, increasing importance is attached to the health and economic problems...
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Sporothrix schenckii: purification and partial biochemical characterisation of glucosamine-6-phosphate synthase, a potential antifungal target
PublicationW artykule opisano izolację i charakterystykę właściwości natywnego enzymu, syntazy GlcN-6-P z komórek dimorficznego grzyba patogennego Sporothrix schenckii. Masę cząsteczkową enzymu natywnego określono na 350 kDa, a enzymu zdenaturowanego na około 79 kDa, co sugeruje homotetrameryczną strukturę białka. Wartość punktu izoelektrycznego wyniosła 6,26; wyznaczono także parametry kinetyczne katalizowanej reakcji. Aktywność enzymu była...
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How do sterols determine the antufungal activitiy of amphotericin B? Free energy of binding between the drug and its membrane targets.
PublicationAmphotericin B (AmB) is a well-known polyene antibiotic used to treat systemic fungal infections. It is commonly accepted that the presence of sterols in the membrane is essential for the AmB biological activity, that is, for the formation of transmembrane ion channels. The selective toxicity of AmB for fungal cells is attributed to the fact that it is more potent against fungal cell membranes containing ergosterol than against...
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‘Acridines’ as New Horizons in Antifungal Treatment
PublicationFrequent fungal infections in immunocompromised patients and mortality due to invasive mycosis are important clinical problems. Opportunistic pathogenic Candida species remain one of the leading causes of systemic mycosis worldwide. The repertoire of antifungal chemotherapeutic agents is very limited. Although new antifungal drugs such as lanosterol 14α-demethylase and β-glucan synthase inhibitors have been introduced into clinical...
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Novel dendrimeric lipopeptides with antifungal activity
PublicationZaprojektowano, zsyntezowano i scharakteryzowano serię nowych kationowych lipopeptydów zawierających rozgałęziony, amfifilowy polarny rdzeń strukturalny pochodzący od dendronu (Lys)(Lys)(Lys) oraz łańcuchy C8 i C12 na C-końcu. Otrzymane zwiazki wykazywały aktywność przeciwdrobnoustrojową, w tym szczególnie przeciwgrzybową wobec drożdżaków z rodzaju Candida. Najwyższą aktywność, selektywną wobec drobnoustrojów grzybowych, wykazywały...
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Evaluation of Antifungal Properties of Titania P25
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Antifungal Activity of Homoaconitate and Homoisocitrate Analogs
PublicationThirteen structural analogs of two initial intermediates of the L-alpha-aminoadipate pathway of L-lysine biosynthesis in fungi have been designed and synthesized, including fluoro- and epoxy-derivatives of homoaconitate and homoisocitrate. Some of the obtainedcompounds exhibited at milimolar range moderate enzyme inhibitory properties against homoaconitase and/or homoisocitrate dehydrogenase of Candida albicans. The structural...
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Targeting DNA Topoisomerase II in Antifungal Chemotherapy.
PublicationTopoisomerase inhibitors have been in use clinically for the treatment of several diseases for decades. Although those enzymes are significant molecular targets in antibacterial and anticancer chemotherapy very little is known about the possibilities to target fungal topoisomerase II (topo II). Raising concern for the fungal infections, lack of effective drugs and a phenomenon of multidrug resistance underlie a strong need to expand...
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Antifungal action of the oxathiolone-fused chalcone derivative
PublicationAMG-148, pochodna chalkonu z pierścieniem oksatiolonowym, wykazuje aktywność przeciwgrzybową in vitro wobec szczepów grzybowych patogennych dla człowieka, z wartościami minimalnych stężeń hamujących wzrost mieszczących się w zakresie 1-16 mikrogramów na mililitr, natomiast w wyższych stężeniach związek ten działa grzybobójczo. Obecność głównych białek oporności wielolekowej, Cdr1p, Cgr2p lub Mdr1p nie wpływa znacząco na aktywność...