量研学術機関リポジトリ「QST-Repository」は、国立研究開発法人 量子科学技術研究開発機構に所属する職員等が生み出した学術成果（学会誌発表論文、学会発表、研究開発報告書、特許等）を集積しインターネット上で広く公開するサービスです。 Welcome to QST-Repository where we accumulates and discloses the academic research results(Journal Publications, Conference presentation, Research and Development Report, Patent, etc.) of the members of National Institutes for Quantum and Radiological Science and Technology.
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Design, Synthesis, and Evaluation of Radioprotecting Agents Targeting p53 Based on Zinc Enzyme Research, Machine Learning, and Random Screening
利用統計を見る
In radiation therapy, adverse side effects are often induc Therefore, development of radioprotective drugs that can protect normal cells from radiation and thus suppress adverse side effects would be highly desirable. The radiation-induced cell death of normal cells is caused, at least in part, by apoptosis, which undergoes via activation of p53 and increase in the p53 protein, a zinc-containing transcriptional factor, in response to cellular damage. In this paper, we report on the radioprotective activity of 8-hydroxyquinoline (8HQ) derivatives that were designed so as to interact with the Zn2+ in p53. and protect MOLT-4 cells against g-ray radiation (10 Gy), accompanied by a low cytotoxicity. The details of design, synthesis, and biological activities of derivatives will be presented. The results of the prediction of radioprotective activity and toxicity of these drugs and random screening from the compound library of Drug Discovery Initiative (DDI), the University of Tokyo, will also be presented.
Design, Synthesis, and Evaluation of Radioprotecting Agents Targeting p53 Based on Zinc Enzyme Research, Machine Learning, and Random Screening
