p53阻害剤の作用機序

質問

p53の阻害剤としてpifithrin-alphaという薬物を用いています。
この薬物の作用機序を知りたく、いろいろ調べたのですが、どうしても分かりません。
PUBMEDで調べると、リン酸化の阻害のようなのですが、ではなぜリン酸化が阻害されるのか、阻害部位は何のどこなのかが分かりません。
お分かりの方、どうぞ教えてください。

回答No.1

ga111

オリジナルの最も古い文献によると転写阻害剤らしいですね。
たぶんほかの追加的な事も分かってきているということかもしれませんよ。

1: Science. 1999 Sep 10;285(5434):1733-7.
Chemotherapy and radiation therapy for cancer often have severe side effects that limit their efficacy. Because these effects are in part determined by p53-mediated apoptosis, temporary suppression of p53 has been suggested as a therapeutic strategy to prevent damage of normal tissues during treatment of p53-deficient tumors. To test this possibility, a small molecule was isolated for its ability to reversibly block p53-dependent transcriptional activation and apoptosis. This compound, pifithrin-alpha, protected mice from the lethal genotoxic stress associated with anticancer treatment without promoting the formation of tumors. Thus, inhibitors of p53 may be useful drugs for reducing the side effects of cancer therapy and other types of stress associated with p53 induction.