Enzyme kinetic and spectroscopic studies of inhibitor and effector interactions with indoleamine 2,3-dioxygenase. 1. Norharman and 4-phenylimidazole binding to the enzyme as inhibitors and heme ligands

Biochemistry ◽  
1989 ◽  
Vol 28 (13) ◽  
pp. 5392-5399 ◽  
Author(s):  
Masanori Sono ◽  
Susan G. Cady
2014 ◽  
Vol 9 (7) ◽  
pp. 1934578X1400900
Author(s):  
Serm Surapinit ◽  
Piyawit Sri-in ◽  
Santi Tip-pyang

Isolated oligostilbenes from G. macrostachyum exhibited sbLOX-1 inhibitory activity with IC50 values ranging from 0.14–11.91 μM. Of these oligostilbenoids, 12 (IC0 0.14±0.01 μM), 10 (IC0 0.33±0.11 μM), 11 (IC50 0.49±0.05 μM) and 7 (IC50 1.03 ± 0.43 μM) were more active than nordihydroguaiaretic acid (NDGA) ( P < 0.05) which was the positive control. The enzyme kinetic analysis revealed that 7 and 11 inhibited sbLOX-1 noncompetitively with K i values of 11.2 and 71.4 nM. Compound 10 inhibited sbLOX-1 through mixed-competitive mechanisms ( K i = 13.8 nM and K' i 56.7 nM). Moreover, 12 was an uncompetitive inhibitor with a K i value of 0.8 nM. The inhibitory activity of oligostilbenes did not result from the antioxidant property, as demonstrated by DPPH and 13-HPOD scavenging assays. These compounds also showed ferric reducing capabilities, but had no effect in a Fe3+-bound sbLOX-1 model, as indicated by UV spectrophotometric and CD spectroscopic studies.


Biochemistry ◽  
2010 ◽  
Vol 49 (24) ◽  
pp. 5028-5034 ◽  
Author(s):  
Changyuan Lu ◽  
Yu Lin ◽  
Syun-Ru Yeh

2001 ◽  
Vol 120 (5) ◽  
pp. A182-A182
Author(s):  
G GREGORY ◽  
W STENSON ◽  
R NEWBERRY

1987 ◽  
Vol 84 ◽  
pp. 443-448 ◽  
Author(s):  
Teresa Kowalik ◽  
Brigitte Decock-Le Reverend ◽  
Claude Loucheux ◽  
Damien Ficheux ◽  
Henryk Kozlowski

1980 ◽  
Vol 41 (C1) ◽  
pp. C1-187-C1-188 ◽  
Author(s):  
G. P. Gupta ◽  
J. A. Baines ◽  
D. M. Cooper ◽  
D. P.E. Dickson ◽  
C. E. Johnson

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