@article{52339f4c947f4fb581b6105bac71667b,
title = "Thiazolidine reacts with thioreactive biomolecules",
abstract = "The thiazolidine ring is a biologically active chemical structure and is associated with many pharmacological activities. However, the biological molecules that can interact with the thiazolidine ring are not known. We show that thiazolidine causes sustained activation of the TRPA1 channel and chemically reacts with glutathione, and the chemical reactivity of thiazolidine ring is required for TRPA1 activation. Reducing agents reverse thiazolidine-induced TRPA1 activation, and mutagenesis studies show that nucleophilic cysteine residues in TRPA1 are critical, suggesting an activation mechanism involving thioreactive chemical reactions. In vivo studies show that thiazolidine induces acute pain and inflammation in mouse and these responses are specifically dependent on TRPA1. These results indicate that thiazolidine compounds can chemically react with biological molecules containing nucleophilic cysteines, thereby exerting biological activities.",
keywords = "Glutathione, TRPA1 channel, Thiazolidine",
author = "Deyuan Su and Yin Nian and Fenglei Zhang and Jinsheng Hu and Jianmin Cui and Ming Zhou and Jian Yang and Shu Wang",
note = "Funding Information: We thank David Julius of University of California San Francisco for providing TRPA1+/- mice. We also thank members of the Ion Channel Research and Drug Development Center at Kunming Institute of Zoology for reading and commenting on the manuscript. This work was supported by grants from the National Natural Science Foundation of China (81302865), Yunnan Applied Basic Research Projects (2013FB074), Youth Innovation Promotion Association of the Chinese Academy of Sciences, Key Research Program of the Chinese Academy of Sciences (KJZD-EW-L03) and West Light Foundation of the Chinese Academy of Sciences to Shu Wang; grants from the National Basic Research Program of China (2014CB910301), Top Talents Program of Yunnan Province (2011HA012), High-level Overseas Talents of Yunnan Province, Yunnan Major Science and Technology Project (2015ZJ002) and the National Natural Science Foundation of China (31370821) to Jian Yang; Grants from the High-level Overseas Talents of Yunnan Province and the National Basic Research Program of China (2014CB910301) to Ming Zhou; and a Grant from High-level Overseas Talents of Yunnan Province to Jianmin Cui. Publisher Copyright: {\textcopyright} 2017 Elsevier Inc.",
year = "2017",
month = mar,
day = "1",
doi = "10.1016/j.freeradbiomed.2017.01.032",
language = "English",
volume = "104",
pages = "272--279",
journal = "Free Radical Biology and Medicine",
issn = "0891-5849",
}