Development of Colorimetric HTS Assay of Cytochrome P450 forortho-Specific Hydroxylation, and Engineering of CYP102D1 with Enhanced Catalytic Activity and Regioselectivity

ChemBioChem ◽  
2013 ◽  
Vol 14 (10) ◽  
pp. 1231-1238 ◽  
Author(s):  
Kwon-Young Choi ◽  
Eun-Ok Jung ◽  
Hyungdon Yun ◽  
Yung-Hun Yang ◽  
Romas J. Kazlauskas ◽  
...  
1994 ◽  
Vol 53 ◽  
pp. S273-S278 ◽  
Author(s):  
A Rane ◽  
C Bjelfman ◽  
C Thyr ◽  
I Porsch-Hällström

2008 ◽  
Vol 40 (2) ◽  
pp. 254 ◽  
Author(s):  
Songhee Jeon ◽  
Keon-Hee Kim ◽  
Chul-Ho Yun ◽  
Boo-Whan Hong ◽  
Yoon-Seok Chang ◽  
...  

2009 ◽  
Vol 85 (4) ◽  
pp. 387-393 ◽  
Author(s):  
DJ McConn II ◽  
YS Lin ◽  
TL Mathisen ◽  
DK Blough ◽  
Y Xu ◽  
...  

2000 ◽  
Vol 78 (11) ◽  
pp. 874-881 ◽  
Author(s):  
Thomas KH Chang ◽  
Wendy BK Lee ◽  
Hin Hin Ko

The present study was performed to determine if trans-resveratrol (3,5,4'-trihydroxy-trans-stilbene) modulates the catalytic activity and gene expression of cytochrome P450 1B1 (CYP1B1). In vitro, trans-resveratrol decreased human recombinant CYP1B1-catalyzed 7-ethoxyresorufin O-dealkylation activity, with an IC50 value of 1.4 ± 0.2 µM (mean ± SEM). Enzyme kinetic analysis indicated that trans-resveratrol inhibited CYP1B1 enzyme activity by a mixed-type inhibition and the apparent Ki was 0.75 ± 0.06 µM. To determine if trans-resveratrol modulates constitutive CYP1B1 gene expression, cultured MCF-7 human breast carcinoma cells were treated with trans-resveratrol. As indicated by RT-PCR analysis, treatment of MCF-7 cells with 10 µM trans-resveratrol decreased relative CYP1B1 mRNA levels after 5 h, but not after 1.5 or 3 h, of exposure. trans-Resveratrol treatment at 5, 7.5, 10, or 20 µM for 5 h produced a concentration-dependent decrease in CYP1B1 mRNA levels. The extent of suppression was ~50% at 20 µM concentration. The suppressive effect was not a consequence of a toxic response to the compound as assessed by a cell proliferation assay. Overall, our novel finding that trans-resveratrol inhibits the catalytic activity and suppresses the constitutive gene expression of CYP1B1 leads to the possibility that this nutraceutical confers protection against toxicity and carcinogenicity induced by compounds that undergo CYP1B1-catalyzed bioactivation.Key words: cytochrome P450, CYP1B1, 7-ethoxyresorufin, nutraceutical, trans-resveratrol.


1996 ◽  
Vol 17 (10) ◽  
pp. 2267-2269 ◽  
Author(s):  
M. Legrand ◽  
L. Stücker ◽  
D. Marez ◽  
N. Sabbagh ◽  
JM. Lo-Guidice ◽  
...  

1995 ◽  
Vol 43 (3) ◽  
pp. 233-239 ◽  
Author(s):  
René Feyereisen ◽  
John F. Andersen ◽  
Flerida A. Cariño ◽  
Michael B. Cohen ◽  
Josette F. Koener

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