scholarly journals QM/MM Study of the Active Species of the Human Cytochrome P450 3A4, and the Influence Thereof of the Multiple Substrate Binding

2007 ◽  
Vol 111 (49) ◽  
pp. 13822-13832 ◽  
Author(s):  
Dan Fishelovitch ◽  
Carina Hazan ◽  
Hajime Hirao ◽  
Haim J. Wolfson ◽  
Ruth Nussinov ◽  
...  
Keyword(s):  
Cytochrome P450 ◽  
Substrate Binding ◽  
Active Species ◽  
Cytochrome P450 3A4 ◽  
Human Cytochrome ◽  
Multiple Substrate

scholarly journals Multiple substrate-binding sites are retained in cytochrome P450 3A4 mutants with decreased cooperativity

Xenobiotica ◽  
2010 ◽  
Vol 41 (4) ◽  
pp. 281-289 ◽  
Author(s):  
Harshica Fernando ◽  
Jessica A. O. Rumfeldt ◽  
Nadezhda Y. Davydova ◽  
James R. Halpert ◽  
Dmitri R. Davydov
Keyword(s):  
Cytochrome P450 ◽  
Binding Sites ◽  
Substrate Binding ◽  
Cytochrome P450 3A4 ◽  
Multiple Substrate ◽  
Substrate Binding Sites

Pyrene·Pyrene Complexes at the Active Site of Cytochrome P450 3A4:  Evidence for a Multiple Substrate Binding Site

2002 ◽  
Vol 124 (40) ◽  
pp. 11866-11867 ◽  
Author(s):  
Michael J. Dabrowski ◽  
Michael L. Schrag ◽  
Larry C. Wienkers ◽  
William M. Atkins
Keyword(s):  
Cytochrome P450 ◽  
Binding Site ◽  
Active Site ◽  
Substrate Binding ◽  
Cytochrome P450 3A4 ◽  
Substrate Binding Site ◽  
Multiple Substrate

Multiple Substrate Binding by Cytochrome P450 3A4: Estimation of the Number of Bound Substrate Molecules

2008 ◽  
Vol 36 (10) ◽  
pp. 2136-2144 ◽  
Author(s):  
Yury Kapelyukh ◽  
Mark J. I. Paine ◽  
Jean-Didier Maréchal ◽  
Michael J. Sutcliffe ◽  
C. Roland Wolf ◽  
...  
Keyword(s):  
Cytochrome P450 ◽  
Substrate Binding ◽  
Cytochrome P450 3A4 ◽  
Multiple Substrate

scholarly journals CO Binding Kinetics of Human Cytochrome P450 3A4

1995 ◽  
Vol 270 (10) ◽  
pp. 5014-5018 ◽  
Author(s):  
Aditya P. Koley ◽  
Jeroen T. M. Buters ◽  
Richard C. Robinson ◽  
Allen Markowitz ◽  
Fred K. Friedman
Keyword(s):  
Cytochrome P450 ◽  
Binding Kinetics ◽  
Cytochrome P450 3A4 ◽  
Human Cytochrome ◽  
Kinetics Of

scholarly journals Porcine foetal and neonatal CYP3A liver expression

2011 ◽  
Vol 1 (1) ◽  
pp. 1 ◽  
Author(s):  
Marie Louise Hiort Hermann ◽  
Mette Tingleff Skaanild
Keyword(s):  
Cytochrome P450 ◽  
Liver Microsomes ◽  
Cytochrome P450 3A4 ◽  
Chain Reaction ◽  
Hepatic Expression ◽  
Human Cytochrome ◽  
Foetal Liver ◽  
Polymerase Chain ◽  
Cyp3a Enzyme ◽  
Exogenous Substances

Human cytochrome P450 3A7 (CYP3A7) and cytochrome P450 3A4 (CYP3A4) are hepatic metabolising enzymes which participates in the biotransformation of endo- and exogenous substances in foetuses and neonates respectively. These CYP3A enzymes display an inverse relationship: CYP3A7 is the dominant enzyme in the foetal liver, whereas the expression of CYP3A4 is low. After parturition there is a shift in the expression, thus CYP3A7 is down regulated, while the level of CYP3A4 gradually increases and becomes the dominant metabolising CYP3A enzyme in the adult. The minipig is increasingly being used as a model for humans in biomedical studies, because of its many similarities with the human physiology and anatomy. The aim of this study was to examine whether, as in humans, a shift is seen in the hepatic expression of a CYP3A7- like enzyme to cytochrome P450 3A29 (CYP3A29) (an orthologue to the human CYP3A4) in minipigs. This was elucidated by examining the hepatic mRNA expression of CYP3A7 and CYP3A29 in 39 foetuses and newborn Göttingen minipigs using quantitative real time polymerase chain reaction (qPCR). Furthermore the immunochemical level of CYP3A7-LE and CYP3A29 was measured in liver microsomes using western blotting. The expression of CYP3A29 was approximately 9- fold greater in neonates compared to foetuses, and a similar difference was reflected on the immunochemical level. It was not possible to detect a significant level of foetal CYP3A7 mRNA, but immunoblotting showed a visible difference depending on age. This study demonstrates an increase in the expression of CYP3A29, the CYP3A4 orthologue in perinatal minipigs as in humans, which suggests that the minipig could be a good model when testing for human foetal toxicity towards CYP3A4 substrates.

scholarly journals Human Cytochrome P450 3A4 as a Biocatalyst: Effects of the Engineered Linker in Modulation of Coupling Efficiency in 3A4-BMR Chimeras

2017 ◽  
Vol 8 ◽  
Author(s):  
Danilo Degregorio ◽  
Serena D'Avino ◽  
Silvia Castrignanò ◽  
Giovanna Di Nardo ◽  
Sheila J. Sadeghi ◽  
...  
Keyword(s):  
Cytochrome P450 ◽  
Coupling Efficiency ◽  
Cytochrome P450 3A4 ◽  
Human Cytochrome

Inhibitory effects of polyphenols on human cytochrome P450 3A4 and 2C9 activity

2010 ◽  
Vol 48 (1) ◽  
pp. 429-435 ◽  
Author(s):  
Yuka Kimura ◽  
Hideyuki Ito ◽  
Ryoko Ohnishi ◽  
Tsutomu Hatano
Keyword(s):  
Cytochrome P450 ◽  
Cytochrome P450 3A4 ◽  
Inhibitory Effects ◽  
Human Cytochrome
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