期刊
IN VIVO
卷 31, 期 1, 页码 39-43出版社
INT INST ANTICANCER RESEARCH
DOI: 10.21873/invivo.11022
关键词
Oxidative stress; GS-nitroxide; radiation mitigation
资金
- NIAID/NIH [U19-A1068021]
- [P30CA047904]
Background/Aim: Mitochondrial-targeted gramicidin S (GS)-nitroxide, JP4-039, has been demonstrated to be a potent radiation mitigator, and safe over a wide dose range. In addition, JP4-039 has organ-specific effectiveness when locally applied. Materials and Methods: We tested the effect of another GS-nitroxide, XJB-5-131, which has more effective mitochondrial localization, and compared these results to those for radiation mitigation against the hematopoietic syndrome, and two analogs of JP4-039, which have the same mitochondrial localization signal, but different chemical payloads: JRS527.084 contains a second nitroxide per molecule, and TK649.030 contains an ester group attached to the nitroxide. Results: The results demonstrate the superiority of JP4-039 as a systemic radiation mitigator. Conclusion: Structure-activity relationships and bioassays demonstrate that JP4-039 is an optimized small-molecule radiation mitigator.
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