Interaction of the serine hydrolase KIAA1363 with organophosphorus agents: Evaluation of potency and kinetics
详细信息 查看全文
- 作者：Matthew K. Rossa ; b ; mross@cvm.msstate.edu" class="auth_mail" title="E-mail the corresponding author ; Kim Plutaa ; Victoria Bittlesa ; Abdolsamad Borazjania ; b ; J. Allen Crowa ; b ; crow@cvm.msstate.edu" class="auth_mail" title="E-mail the corresponding author
- 关键词：Carboxylesterase ; Oxon ; Bimolecular rate constant ; Enzyme inhibition ; Chlorpyrifos oxon ; Paraoxon
- 刊名：Archives of Biochemistry and Biophysics
- 出版年：2016
- 出版时间：15 January 2016
- 年：2016
- 卷：590
- 期：Complete
- 页码：72-81
- 全文大小：1541 K
文摘
- •
IC50s and apparent bimolecular rate constant (kinact/Ki) for reactions of chlorpyrifos oxon and paraoxon with human KIAA1363 were determined.
- •
Human KIAA1363 was potently inhibited by both chlorpyrifos oxon and paraoxon, with IC50s in the nM range.
- •
Bimolecular rate constants for reactions of chlorpyrifos oxon and paraoxon with human KIAA1363 should prove useful in PBPK/PD modeling efforts.