Irregularities in enzyme assays: The case of macrophage migration inhibitory factor
Irregularities in enzyme assays: The case of macrophage migration inhibitory factor
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DOI:
10.1016/j.bmcl.2016.04.074
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发表时间:
2016-06-15
影响因子:
2.7
通讯作者:
Jorgensen, William L.
中科院分区:
文献类型:
--
作者:
Cisneros, Jose A.;Robertson, Michael J.;Jorgensen, William L.
Inhibitors of human macrophage migration inhibitory factor (MIF) previously reported in the literature have been reexamined by synthesis, assaying for tautomerase activity, and protein crystallography. Substantial inconsistencies between prior and current assay results are noted. They appear to arise from difficulties with the tautomerase substrates, solubility issues, and especially covalent inhibition. Incubation time variation shows that 3, 4, 6, and 9 are covalent or slow-binding inhibitors. Two protein crystal structures are provided; one confirms that the twice-discovered 3 is a covalent inhibitor. (C) 2016 Elsevier Ltd. All rights reserved.