- N-ACETYL-6-HYDROXYTRYPTOPHAN A NATURAL SUBSTRATE OF A MONOPHENOL OXIDASE FROM ASPERGILLUS NIDULANS
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Key Word Index - Aspergillus nidulans; mutant; conidiophore pigment; monophenol oxidase; enzyme substrate; N-acetyl-6-hydroxytryptophan. An ivo B mutant of Aspergillus nidulans, deficient in conidiophore pigment has been shown to accumulate N-acetyl-6-hydroxytryptophan.This acts as a substrate for a specific monophenol oxidase present in the wild type but absent in the mutant.
- Mccorkindale, Norman J.,Hayes, Douglas,Johnston, Grant A.,Clutterbuck, A. John
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- SYNTHESIS OF A-AMANITIN AND ITS DERIVATIVES
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The present invention relates to the chemical synthesis of α-amanitin and its derivatives. The present invention also relates to intermediate products of the α-amanitin synthesis.
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Page/Page column 44
(2021/01/29)
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- A Convergent Total Synthesis of the Death Cap Toxin α-Amanitin
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The toxic bicyclic octapeptide α-amanitin is mostly found in different species of the mushroom genus Amanita, with the death cap (Amanita phalloides) as one of the most prominent members. Due to its high selective inhibition of RNA polymerase II, which is directly linked to its high toxicity, particularly to hepatocytes, α-amanitin received an increased attention as a toxin-component of antibody-drug conjugates (ADC) in cancer research. Furthermore, the isolation of α-amanitin from mushrooms as the sole source severely restricts compound supply as well as further investigations, as structure–activity relationship (SAR) studies. Based on a straightforward access to the non-proteinogenic amino acid dihydroxyisoleucine, we herein present a robust total synthesis of α-amanitin providing options for production at larger scale as well as future structural diversifications.
- Knittel, Caroline H.,Süssmuth, Roderich D.,Siegert, Mary-Ann J.
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supporting information
p. 5500 - 5504
(2020/02/13)
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- Structure-based de novo design, synthesis, and biological evaluation of the indole-based PPARγ ligands (I)
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MCSS and LeapFrog, two de novo drug design programs, were used for the novel indole-based PPARγ ligands' study. The designed compounds were synthesized and tested for the PPARγ protein binding activities in vitro. Out of the compounds that were synthesize
- Dong, Xiaochun,Zhang, Zhenshan,Wen, Ren,Shen, Jianhua,Shen, Xu,Jiang, Hualiang
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p. 5913 - 5916
(2007/10/03)
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