Chloride and other anions inhibit dichloroacetate-induced inactivation of human liver GSTZ1 in a haplotype-dependent manner
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- 作者：Guo Zhonga ; Wenjun Lia ; Yuan Gua ; Taimour Langaeeb ; Peter W. Stacpoolec ; d ; Margaret O. Jamesa ; mojames@ufl.edu" class="auth_mail
- 关键词：DCA ; dichloroacetate ; Na DCA ; sodium dichloroacetate ; PAH ; pulmonary arterial hypertension ; GSH ; glutathione ; GSTZ1 ; glutathione transferase 味1 ; h ; hour ; MAAI ; maleylacetoacetate isomerase ; SNPs ; single nucleotide polymorphisms ; t1/2 ; half-life ; EC50 ; concentration that protected 50% of the GSTZ1 activity from inactivation
- 刊名：Chemico-Biological Interactions
- 出版年：25 May 2014
- 年：2014
- 卷：215
- 期：Complete
- 页码：33-39
- 全文大小：944 K
文摘
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Inactivation of GSTZ1 by dichloroacetate (DCA) controls DCA pharmacokinetics.
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This work reports factors affecting mechanism-based inactivation of GSTZ1-1 by DCA.
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The physiologically important nucleophile, Cl− protected GSTZ1 from inactivation by DCA.
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A lower concentration of Cl− was required to protect GSTZ1C than GSTZ1A.
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Br−, I− and SO32− protected GSTZ1, but F−, SO42−, CO32−, CN− and CH3COO− did not.