Tolypocladamides A-G: Cytotoxic Peptaibols from Tolypocladium inflatum.

Tolypocladamides A-G: Cytotoxic Peptaibols from Tolypocladium inflatum.
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DOI:
10.1021/acs.jnatprod.2c00240
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发表时间:
2022-06-24
影响因子:
5.1
通讯作者:
Beutler, John A.
Beutler, John A.
中科院分区:
生物学2区
文献类型:
--
作者:
Senadeera, Sarath P. D.;Wang, Dongdong;Kim, Chang-Kwon;Smith, Emily A.;Durrant, David E.;Alexander, Patrick A.;Wendt, Karen L.;Stephen, Andrew G.;Morrison, Deborah K.;Cichewicz, Robert H.;Henrich, Curtis J.;Beutler, John A.

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Seven new peptaibols named tolypocladamides A-G have been isolated from an extract of the fungus Tolypocladium inflatum which inhibited the interaction between Raf and oncogenic Ras in a cell-based high-throughput screening assay. Each peptaibol contains 11 amino acid residues, an octanoyl or decanoyl fatty acid chain at the N-terminus, and a leucinol moiety at the C-terminus. Their peptaibol sequences were elucidated based on 2D NMR and HR-ESI-MS2 fragmentation analyses. Amino acid configurations were determined by advanced Marfey’s analyses. Tolypocladamides A-G caused significant inhibition of Ras/Raf interactions with IC50 values ranging from 0.5 to 5.0 μM in a NanoBRET assay; however, no interactions were observed in a surface plasmon resonance assay for binding of the compounds to wild type or G12D mutant Ras constructs or to the Ras binding domain of Raf. NCI 60 cell line testing was also conducted, with little panel selectivity observed.
DOI: 10.1021/acs.jnatprod.2c00153
发表时间: 2022-05-27
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DOI: 10.1021/acs.jnatprod.0c00136
发表时间: 2020-04-24
影响因子: 5.1
作者:
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发表时间: 1998-08-01
期刊: PHYTOCHEMISTRY
影响因子: 3.8
作者:
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DOI: 10.1139/v96-020
发表时间: 1996-02-01
期刊: CANADIAN JOURNAL OF CHEMISTRY-REVUE CANADIENNE DE CHIMIE
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作者:
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通讯作者: Widden, P