Pub. Date : 2001 Oct 9
PMID : 11580286
17 Functional Relationships(s)Download |
Sentence | Compound Name | Protein Name | Organism |
| 1 | Ticlopidine as a selective mechanism-based inhibitor of human cytochrome P450 2C19. | Ticlopidine | cytochrome P450 family 2 subfamily C member 19 | Homo sapiens |
| 2 | Experiments using recombinant yeast-expressed human liver cytochromes P450 confirmed previous literature data indicating that ticlopidine is an inhibitor of CYP 2C19. | Ticlopidine | cytochrome P450 family 2 subfamily C member 19 | Homo sapiens |
| 3 | The present studies demonstrated that ticlopidine is selective for CYP 2C19 within the CYP 2C subfamily. | Ticlopidine | cytochrome P450 family 2 subfamily C member 19 | Homo sapiens |
| 4 | UV-visible studies on the interaction of a series of ticlopidine derivatives with CYP 2C19 showed that ticlopidine binds to the CYP 2C19 active site with a K(s) value of 2.8 +/- 1 microM. | Ticlopidine | cytochrome P450 family 2 subfamily C member 19 | Homo sapiens |
| 5 | UV-visible studies on the interaction of a series of ticlopidine derivatives with CYP 2C19 showed that ticlopidine binds to the CYP 2C19 active site with a K(s) value of 2.8 +/- 1 microM. | Ticlopidine | cytochrome P450 family 2 subfamily C member 19 | Homo sapiens |
| 6 | UV-visible studies on the interaction of a series of ticlopidine derivatives with CYP 2C19 showed that ticlopidine binds to the CYP 2C19 active site with a K(s) value of 2.8 +/- 1 microM. | Ticlopidine | cytochrome P450 family 2 subfamily C member 19 | Homo sapiens |
| 7 | UV-visible studies on the interaction of a series of ticlopidine derivatives with CYP 2C19 showed that ticlopidine binds to the CYP 2C19 active site with a K(s) value of 2.8 +/- 1 microM. | Ticlopidine | cytochrome P450 family 2 subfamily C member 19 | Homo sapiens |
| 8 | Ticlopidine is oxidized by CYP 2C19 with formation of two major metabolites, the keto tautomer of 2-hydroxyticlopidine (1) and the dimers of ticlopidine S-oxide (TSOD) (V(max) = 13 +/- 2 and 0.4 +/- 0.1 min(-1)). | Ticlopidine | cytochrome P450 family 2 subfamily C member 19 | Homo sapiens |
| 9 | During this oxidation, CYP 2C19 was inactivated; the rate of its inactivation was time and ticlopidine concentration dependent. | Ticlopidine | cytochrome P450 family 2 subfamily C member 19 | Homo sapiens |
| 10 | It occurs in parralel with CYP 2C19-catalyzed oxidation of ticlopidine, is inhibited by an alternative well-known substrate of CYP 2C19, omeprazole, and correlates with the covalent binding of ticlopidine metabolite(s) to proteins. | Ticlopidine | cytochrome P450 family 2 subfamily C member 19 | Homo sapiens |
| 11 | It occurs in parralel with CYP 2C19-catalyzed oxidation of ticlopidine, is inhibited by an alternative well-known substrate of CYP 2C19, omeprazole, and correlates with the covalent binding of ticlopidine metabolite(s) to proteins. | Ticlopidine | cytochrome P450 family 2 subfamily C member 19 | Homo sapiens |
| 12 | It occurs in parralel with CYP 2C19-catalyzed oxidation of ticlopidine, is inhibited by an alternative well-known substrate of CYP 2C19, omeprazole, and correlates with the covalent binding of ticlopidine metabolite(s) to proteins. | Ticlopidine | cytochrome P450 family 2 subfamily C member 19 | Homo sapiens |
| 13 | It occurs in parralel with CYP 2C19-catalyzed oxidation of ticlopidine, is inhibited by an alternative well-known substrate of CYP 2C19, omeprazole, and correlates with the covalent binding of ticlopidine metabolite(s) to proteins. | Ticlopidine | cytochrome P450 family 2 subfamily C member 19 | Homo sapiens |
| 14 | The effects of ticlopidine on CYP 2C19 are very analogous with those previously described for the inactivation of CYP 2C9 by tienilic acid. | Ticlopidine | cytochrome P450 family 2 subfamily C member 19 | Homo sapiens |
| 15 | This suggests that a similar electrophilic intermediate, possibly a thiophene S-oxide, is involved in the inactivation of CYP 2C19 and CYP 2C9 by ticlopidine and tienilic acid, respectively. | Ticlopidine | cytochrome P450 family 2 subfamily C member 19 | Homo sapiens |
| 16 | Importantly, ticlopidine is the first selective mechanism-based inhibitor of human liver CYP 2C19 and should be a new interesting tool for studying the topology of the active site of CYP 2C19. | Ticlopidine | cytochrome P450 family 2 subfamily C member 19 | Homo sapiens |
| 17 | Importantly, ticlopidine is the first selective mechanism-based inhibitor of human liver CYP 2C19 and should be a new interesting tool for studying the topology of the active site of CYP 2C19. | Ticlopidine | cytochrome P450 family 2 subfamily C member 19 | Homo sapiens |