Inhibition of macrophage migration inhibitory factor (MIF) tautomerase activity by dopachrome analogs.
A macrophage migration inhibitory factor (MIF) dopachrome tautomerization assay was employed for identification of MIF inhibitors. One group of dopachrome analogs was identified which inhibits MIF tautomerase activity. In particular, the analogs with a leaving group at beta position displayed activity at a concentration of tenfold less than that of the MIF-substrate. These findings could lead to a better understanding of MIF biological activities and the development of agents for the treatment of MIF related diseases.
Zhang
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X
The Picower Institute for Medical Research, Manhasset, NY 11030, USA.
Bucala
R
R
D045563:Indolequinones; D007211:Indoles / Q000737:chemistry / Q000494:pharmacology*; D019746:Intramolecular Oxidoreductases / Q000037:antagonists & inhibitors*; D008263:Macrophage Migration-Inhibitory Factors / Q000037:antagonists & inhibitors*; D011809:Quinones / Q000737:chemistry / Q000494:pharmacology*
D045563:Indolequinones; D007211:Indoles; D008263:Macrophage Migration-Inhibitory Factors; D011809:Quinones; C001123:dopachrome; D019746:Intramolecular Oxidoreductases; C042501:dopachrome isomerase