464195-33-3Relevant academic research and scientific papers
Determination of plasma levels of the active thiol form of the direct-acting PrC-210 ROS-scavenger using a fluorescence-based assay
Dreischmeier, Emma,Fahl, William E.
, (2021)
PrC-210 is a direct-acting ROS-scavenger. It's active when administered orally, IV, or topically; it has none of the nausea/emesis nor hypotension side effects that have precluded human amifostine use. PrC-210 confers 100% survival to mice and rats that received an otherwise 100% lethal radiation dose and 36% reduction of ischemia-reperfusion-induced mouse myocardial infarct damage, and thus is a viable candidate to prevent human ROS-induced ischemia-reperfusion and ionizing radiation toxicities. We report the first assay for the pharmacologically active PrC-210 thiol in blood. PrC-210 has no double-bonds nor light absorption, so derivatizing the thiol with a UV-absorbing fluorochrome enables quantification. This assay: i) is done on the benchtop; it's read with a fluorescence plate reader, ii) provides linear product formation through 60 min, iii) quantifies μM to low mM rodent blood levels of PrC-210 that confer complete radioprotection, iv) accurately reflects PrC-210 thiol formation of mixed disulfides with other thiols in blood, and v) shows excellent between-day assay outcome with very low standard deviation and coefficient of variation. A fluorescence assay quantifying formation of a PrC-210 thiol-bimane adduct enables measurement of blood PrC-210 thiol. A blood assay will help in the development of PrC-210 for use in the human clinical setting.
Biomimetic catalytic oxidative coupling of thiols using thiolate-bridged dinuclear metal complexes containing iron in water under mild conditions
Zhang, Yahui,Yang, Dawei,Li, Ying,Zhao, Xiangyu,Wang, Baomin,Qu, Jingping
, p. 6492 - 6502 (2019/11/20)
A green and efficient approach to disulfides via oxidative coupling of thiols was developed by adopting a biomimetic thiolate-bridged iron-ruthenium complex as the catalyst. Using environmentally friendly oxygen as the oxidant, a wide range of thiols including biologically important molecules can be smoothly converted into corresponding disulfides in water. Notably, two potential intermediate species were successfully isolated and unambiguously characterized, which is essential to reveal the detailed mechanism of this transformation. This catalytic system represents a rare and desired heteronuclear bimetallic scaffold for understanding the biological process of S-S bond formation from the viewpoint of bioinspired catalysis.
Semisynthetic tellurosubtilisin with glutathione peroxidase activity
Mao, Shizhong,Dong, Zeyuan,Liu, Junqiu,Li, Xiangqiu,Liu, Xiaoman,Luo, Guimin,Shen, Jiacong
, p. 11588 - 11589 (2007/10/03)
Reaction of the hydroxyl group of serine-221 of subtilisin with phenylmethanesulfonylfluoride followed by nucleophilic substitution with sodium hydrogen telluride, a semisynthetic telluroprotein, tellurosubtilisin, was prepared. Tellurosubtilisin, which displays high substrate specificity for aromatic thiols, exhibits remarkable peroxidase activity and catalyzes the reduction of hydrogen peroxide by 3-carboxy-4-nitrobenzenethiol 20000 times more efficiently than diphenyl diselenide. Copyright
