Title : Comparison of the substrate specificities of human liver cytochrome P450s 2C9 and 2C18: application to the design of a specific substrate of CYP 2C18.

Pub. Date : 1999 Jun 15

PMID : 10387023






3 Functional Relationships(s)
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1 Whereas only compounds bearing a negative charge acted as substrates of CYP 2C9 and were hydroxylated at position 5 of their thiophene ring at a significant rate, many neutral 2-aroylthiophenes were 5-hydroxylated by CYP 2C18 with kcat values of >2 min-1. 2-aroylthiophenes cytochrome P450 family 2 subfamily C member 18 Homo sapiens
2 Among the various compounds that were studied, those bearing an alcohol function were the best CYP 2C18 substrates. Alcohols cytochrome P450 family 2 subfamily C member 18 Homo sapiens
3 It was regioselectively hydroxylated by CYP 2C18 at position 5 of its thiophene ring with a KM value of 9 +/- 1 microM and a kcat value of 125 +/- 25 min-1, which are the highest described so far for a CYP 2C. Thiophenes cytochrome P450 family 2 subfamily C member 18 Homo sapiens