Inhibition of macrophage migration inhibitory factor (MIF) tautomerase activity by dopachrome analogs

被引:0
作者
Zhang, XN [1 ]
Bucala, R [1 ]
机构
[1] Picower Inst Med Res, Manhasset, NY 11030 USA
关键词
D O I
暂无
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
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. (C) 1999 Elsevier Science Ltd. All rights reserved.
引用
收藏
页码:3193 / 3198
页数:6
相关论文
共 17 条
[1]   An essential regulatory role for macrophage migration inhibitory factor in T-cell activation [J].
Bacher, M ;
Metz, CN ;
Calandra, T ;
Mayer, K ;
Chesney, J ;
Lohoff, M ;
Gemsa, D ;
Donnelly, T ;
Bucala, R .
PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA, 1996, 93 (15) :7849-7854
[2]   Biochemical and nutational investigations of the enzymatic activity of macrophage migration inhibitory factor [J].
Bendrat, K ;
AlAbed, Y ;
Callaway, DJE ;
Peng, T ;
Calandra, T ;
Metz, CN ;
Bucala, R .
BIOCHEMISTRY, 1997, 36 (49) :15356-15362
[3]   MIF IS A PITUITARY-DERIVED CYTOKINE THAT POTENTIATES LETHAL ENDOTOXEMIA [J].
BERNHAGEN, J ;
CALANDRA, T ;
MITCHELL, RA ;
MARTIN, SB ;
TRACEY, KJ ;
VOELTER, W ;
MANOGUE, KR ;
CERAMI, A ;
BUCALA, R .
NATURE, 1993, 365 (6448) :756-759
[4]   PURIFICATION, BIOACTIVITY, AND SECONDARY STRUCTURE-ANALYSIS OF MOUSE AND HUMAN MACROPHAGE-MIGRATION INHIBITORY FACTOR (MIF) [J].
BERNHAGEN, J ;
MITCHELL, RA ;
CALANDRA, T ;
VOELTER, W ;
CERAMI, A ;
BUCALA, R .
BIOCHEMISTRY, 1994, 33 (47) :14144-14155
[5]   MIF rediscovered: Cytokine, pituitary hormone, and glucocorticoid-induced regulator of the immune response [J].
Bucala, R .
FASEB JOURNAL, 1996, 10 (14) :1607-1613
[6]   MIF AS A GLUCOCORTICOID-INDUCED MODULATOR OF CYTOKINE PRODUCTION [J].
CALANDRA, T ;
BERNHAGEN, J ;
METZ, CN ;
SPIEGEL, LA ;
BACHER, M ;
DONNELLY, T ;
CERAMI, A ;
BUCALA, R .
NATURE, 1995, 377 (6544) :68-71
[7]  
GEORGE M, 1962, P SOC EXP BIOL MED, V111, P514
[8]   Specific reduction of insulin disulfides by macrophage migration inhibitory factor (MIF) with glutathione and dihydrolipoamide: potential role in cellular redox processes [J].
Kleemann, R ;
Mischke, R ;
Kapurniotu, A ;
Brunner, H ;
Bernhagen, J .
FEBS LETTERS, 1998, 430 (03) :191-196
[9]   The immunoregulatory mediator macrophage migration inhibitory factor (MIF) catalyzes a tautomerization reaction [J].
Rosengren, E ;
Bucala, R ;
Aman, P ;
Jacobsson, L ;
Odh, G ;
Metz, CN ;
Rorsman, H .
MOLECULAR MEDICINE, 1996, 2 (01) :143-149
[10]   The macrophage migration inhibitory factor MIF is a phenylpyruvate tautomerase [J].
Rosengren, E ;
Aman, P ;
Thelin, S ;
Hansson, C ;
Ahlfors, S ;
Bjork, P ;
Jacobsson, L ;
Rorsman, H .
FEBS LETTERS, 1997, 417 (01) :85-88