@misc{oai:repo.qst.go.jp:00072229, author = {Ujita, Shohei and Mmorita, Akinori and Aoki, Shin and Nishi, Yurie and Tatsuro, Teraoka and Sasatani, Megumi and Wang, Bing and Takahashi, Ippei and Tanaka, Kaoru and Yamakawa, Tomoaki and Nenoi, Mitsuru and Kamiya, Kenji and Inaba, Toshiya and 王 冰 and 田中 薫 and 根井 充}, month = {Feb}, note = {Development of radioprotectors is a very important strategy for reducing radiation risk. We have explored compounds that target a zinc-binding site (ZBS) in p53 , and found that 5-chloro-8-quinolinol (5CHQ) has a unique p53-agonistic activity that shifts its transactivation from proapoptotic to protective responses including the enhancement of p21 induction and the suppression of PUMA induction. The dose-reduction factors of 5CHQ in total-body and abdominally irradiated mice were about 1.2 and 1.3, respectively. In this study, in order to investigate the hydroxyl group at the 8-position of the quinolone ring of 5CHO in its radioprotective function, we synthesized 5-chloro-8-methoxyquinoline (5CMQ), whose 8-hydroxyl group is methylated, and comfirmed that it had no antiapoptotic activity against p-53-dependent apoptosis in 10Gy-irradiated MOLT-4 cells when assessed by Annexin V-FITC staining. In addition, immunoblotting analysis revealed that 5CMQ did not alter the expression of P53 and the products of two p53-target genes, p21 and PUMA, These data indicate that the 8-hydroxyl group of 5CHQ is required for its metal-chelating activity in suppressing apoptosis and shifting p-53-transactivation., 「第1回国際シンポジウム」「Scientific Underpinning for Restoration from a Radiation Disaster(放射線災害からの復興を支える科学的基盤)」}, title = {Requirement of the 8-hydroxyl group in the 5-chloro-8-quinolinol for its Action as a Radioprotective Agonist}, year = {2017} }