Title : CYP2C8/9 mediate dapsone N-hydroxylation at clinical concentrations of dapsone.

Pub. Date : 2000 Aug

PMID : 10901692






5 Functional Relationships(s)
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1 The apparent Michaelis-Menten Km values for DDS-NHY by cloned CYP2C8, CYP2C9, CYP2C18, and CYP2C19 were 75 microM, 31 microM, 25 microM, and greater than 1 mM, respectively. Fumigant 93 cytochrome P450 family 2 subfamily C member 18 Homo sapiens
2 In contrast, S-mephenytoin inhibited DDS-NHY by CYP2C9, CYP2C18, and CYP2C19 by 27 +/- 2, 49 +/- 1, and 32 +/- 4%, respectively. Mephenytoin cytochrome P450 family 2 subfamily C member 18 Homo sapiens
3 In contrast, S-mephenytoin inhibited DDS-NHY by CYP2C9, CYP2C18, and CYP2C19 by 27 +/- 2, 49 +/- 1, and 32 +/- 4%, respectively. Fumigant 93 cytochrome P450 family 2 subfamily C member 18 Homo sapiens
4 Because CYP2C18 and CYP19 are expressed at low concentrations in the human liver, these observations indicate that at clinical DDS concentrations, CYP2C9 is a major and CYP2C8 is a likely minor contributor to DDS-NHY in human liver microsomes. Fumigant 93 cytochrome P450 family 2 subfamily C member 18 Homo sapiens
5 Because CYP2C18 and CYP19 are expressed at low concentrations in the human liver, these observations indicate that at clinical DDS concentrations, CYP2C9 is a major and CYP2C8 is a likely minor contributor to DDS-NHY in human liver microsomes. Fumigant 93 cytochrome P450 family 2 subfamily C member 18 Homo sapiens