生物活性 靶点 体外研究
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globomycin

globomycin,67076-74-8,结构式
globomycin
  • CAS号:67076-74-8
  • 英文名:globomycin
  • 中文名:globomycin
  • CBNumber:CB91399227
  • 分子式:C32H57N5O9
  • 分子量:655.828
  • MOL File:67076-74-8.mol
globomycin化学性质
  • 熔点 :105-108 °C
  • 沸点 :987.8±65.0 °C(Predicted)
  • 密度 :1.062±0.06 g/cm3(Predicted)
  • 储存条件 :-20°C
  • 溶解度 :DMSO: soluble1mg/mL
  • 酸度系数(pKa) :12.79±0.70(Predicted)
  • 形态 :powder
  • 颜色 :white
安全信息
  • WGK Germany :3
  • RTECS号 :MC0593500

globomycin性质、用途与生产工艺

  • 生物活性 Globomycin 是一种脂肽抗生素,也是一种信号肽酶 II ( LspA) 抑制剂。Globomycin 通过不可逆地结合肽酶来抑制原脂蛋白的加工。Globomycin 对 Spiroplasma melliferum 有毒性,其 MIC 在 6.25-12.5 μM 范围内。
  • 靶点

    Signal peptidase II (LspA)
    Gram-negative/Gram-positive bacteria

  • 体外研究

    Globomycin is capable of inhibiting the growth of S. melliferum. The MICs are 6.25 µM (4.1 µg/mL) for strain BC3 and 12.5 µM (8.2 µg/mL) for strain B88.
    Globomycin can interfere with the processing of bacterial lipoproteins by inhibition of signal peptidase II in gracilicutes (Gram-negative eubacteria) and firmicutes (Gram-positive eubacteria).
    In B. diminuta DS010 cells, in the Globomycin-treated cultures most of the organophosphate hydrolase (OPH) accumulates in the cytoplasmic fraction in an unprocessed form. This is in contrast with the untreated cells where very little precursor was detectable. Moreover, there is substantially less mature OPH detectable in the membrane fraction following Globomycin treatment. The OPH signal peptide contains an invariant cysteine residue at the junction of the signal peptidase (Spase) cleavage site along with a well conserved lipobox motif. Substitution of the conserved lipobox cysteine to serine resulted in release of OPH into the periplasm, confirming that OPH is a lipoprotein.

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