scholarly journals Virtual Screening and Optimization Yield Low-Nanomolar Inhibitors of the Tautomerase Activity of Plasmodium falciparum Macrophage Migration Inhibitory Factor

2012 ◽  
Vol 55 (22) ◽  
pp. 10148-10159 ◽  
Author(s):  
Markus K. Dahlgren ◽  
Alvaro Baeza Garcia ◽  
Alissa A. Hare ◽  
Julian Tirado-Rives ◽  
Lin Leng ◽  
...  
Keyword(s):  
Plasmodium Falciparum ◽  
Virtual Screening ◽  
Migration Inhibitory Factor ◽  
Macrophage Migration Inhibitory Factor ◽  
Inhibitory Factor ◽  
Macrophage Migration

scholarly journals Discovery of Human Macrophage Migration Inhibitory Factor (MIF)-CD74 Antagonists via Virtual Screening

2009 ◽  
Vol 52 (2) ◽  
pp. 416-424 ◽  
Author(s):  
Zoe Cournia ◽  
Lin Leng ◽  
Sunilkumar Gandavadi ◽  
Xin Du ◽  
Richard Bucala ◽  
...  
Keyword(s):  
Virtual Screening ◽  
Migration Inhibitory Factor ◽  
Macrophage Migration Inhibitory Factor ◽  
Inhibitory Factor ◽  
Human Macrophage ◽  
Macrophage Migration

scholarly journals The crystal structures of macrophage migration inhibitory factor from Plasmodium falciparum and Plasmodium berghei

2009 ◽  
Vol 18 (12) ◽  
pp. 2578-2591 ◽  
Author(s):  
Sarah E. Dobson ◽  
Kevin D. Augustijn ◽  
James A. Brannigan ◽  
Claudia Schnick ◽  
Chris J. Janse ◽  
...  
Keyword(s):  
Plasmodium Falciparum ◽  
Crystal Structures ◽  
Migration Inhibitory Factor ◽  
Plasmodium Berghei ◽  
Macrophage Migration Inhibitory Factor ◽  
Inhibitory Factor ◽  
Macrophage Migration

scholarly journals Immunohistological Characterization of Macrophage Migration Inhibitory Factor Expression in Plasmodium falciparum-Infected Placentas

2005 ◽  
Vol 73 (6) ◽  
pp. 3287-3293 ◽  
Author(s):  
Sujittra Chaisavaneeyakorn ◽  
Naomi Lucchi ◽  
Carlos Abramowsky ◽  
Caroline Othoro ◽  
Sansanee C. Chaiyaroj ◽  
...  
Keyword(s):  
Plasmodium Falciparum ◽  
Migration Inhibitory Factor ◽  
Macrophage Migration Inhibitory Factor ◽  
Mononuclear Cells ◽  
Placental Malaria ◽  
Inhibitory Factor ◽  
Immunoperoxidase Staining ◽  
Macrophage Migration ◽  
Human Trophoblast ◽  
Hofbauer Cells

ABSTRACT Previously, we have shown that macrophage migration inhibitory factor (MIF) was highly elevated in the placental intervillous blood (IVB) of Plasmodium falciparum-infected women. Here, we compared the expression of MIF in placental tissues obtained from P. falciparum-infected and -uninfected women. Immunoperoxidase staining showed a consistent pattern of MIF expression in syncytiotrophoblasts, extravillous trophoblasts, IVB mononuclear cells, and amniotic epithelial cells, irrespective of their malaria infection status. Cytotrophoblast, villous stroma, and Hofbauer cells showed focal staining. Only amniotic epithelial and IVB mononuclear cells from P. falciparum-infected placentas exhibited significantly higher level of MIF expression than uninfected placentas. Stimulation of syncytilized human trophoblast BeWo cells with P. falciparum-infected erythrocytes that were selected to bind these cells resulted in significant increases in MIF secretion, whereas control erythrocytes, lipopolysaccharides, and synthetic β-hematin had minimal effect. These findings suggest that placental malaria modulates MIF expression in different placental compartments.

scholarly journals Virtual Screening of Some Active Human Macrophage Migration Inhibitory Factor Antagonists

2014 ◽  
Vol 19 (7) ◽  
pp. 1116-1123 ◽  
Author(s):  
Tsung-Lin Tsai ◽  
Thy-Hou Lin
Keyword(s):  
Virtual Screening ◽  
Migration Inhibitory Factor ◽  
Macrophage Migration Inhibitory Factor ◽  
Inhibitory Factor ◽  
Human Macrophage ◽  
Macrophage Migration ◽  
Active Compounds ◽  
Zinc Database ◽  
Docking Method ◽  
Better Than

Macrophage migration inhibitory factor (MIF) is an autocrine- and paracrine-acting cytokine that is involved in several inflammatory, autoimmune, infectious, and oncogenic diseases. Clinical data have shown that inhibition of MIF, especially its tautomerase activity, with small compounds has been beneficial in some disease models. A virtual screening (VS) experiment is conducted for searching some active compounds to inhibit the tautomerase activity of MIF from the ZINC database. By using an x-ray–determined structure OXIM-11 as the query and an in-house developed two-dimensional scaffold comparing method designated as Sfilter, we have screened out some 1500 compounds for ranking by our previously published docking method ADDock. After further ranking by ADDock on 119 compounds screened, we have decided to choose 17 of them for measuring their inhibitory activity IC50 against the MIF tautomerase experimentally. The IC50’s are measured using both human monocytic THP-1 cell lysate and purified recombinant human MIF protein. We have found that the IC50’s measured for three searched compounds (namely, ZINC02693801, ZINC00141102, and ZINC12368346) are better than that determined for ISO-1, a known MIF tautomerase inhibitor and standard used throughout our VS experiment. Moreover, the scaffolds of most of our active compounds searched are also quite different from those searched and published by others previously.

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