Graham D G, Tye R W, Vogel F S
Cancer Res. 1977 Feb;37(2):436-9.
The 490 quinone, a natural sulfhydryl-arylating reagent from the mushroom, Agaricus bisporus, markedly inhibited L1210 murine leukemia DNA polymerase alpha while resulting in little inhibition of DNA polymerase beta from this source. This quinone was more strongly inhibitory than p-chloromercuri-benzoate or N-ethylmaleimide and was less readily neutralized by sulfhydryl-containing molecules such as dithioerythritol. Preliminary experiments indicate that DNA protects DNA polymerase alpha from inhibition by the 490 quinone. The inhibition of DNA synthesis by quinone 490 may contribute significantly to the cytotoxicity of this compound and to the potential of gamma-L-glutaminyl-4-hydroxybenzene as an antitumor agent.
490醌是一种从双孢蘑菇中提取的天然巯基芳基化试剂，它能显著抑制L1210小鼠白血病DNA聚合酶α，而对该来源的DNA聚合酶β抑制作用很小。这种醌的抑制作用比对氯汞苯甲酸或N-乙基马来酰亚胺更强，且较难被二硫苏糖醇等含巯基分子中和。初步实验表明，DNA可保护DNA聚合酶α免受490醌的抑制。490醌对DNA合成的抑制作用可能在很大程度上导致了该化合物的细胞毒性，以及γ-L-谷氨酰胺基-4-羟基苯作为抗肿瘤药物的潜力。
