Pub. Date : 2013 Mar
PMID : 23275066
15 Functional Relationships(s)Download |
Sentence | Compound Name | Protein Name | Organism |
| 1 | Carboxylesterase 1 as a determinant of clopidogrel metabolism and activation. | Clopidogrel | carboxylesterase 1 | Homo sapiens |
| 2 | Clopidogrel, a recognized substrate of hepatic carboxylesterase 1 (CES1), undergoes extensive hydrolytic metabolism in the liver. | Clopidogrel | carboxylesterase 1 | Homo sapiens |
| 3 | Clopidogrel, a recognized substrate of hepatic carboxylesterase 1 (CES1), undergoes extensive hydrolytic metabolism in the liver. | Clopidogrel | carboxylesterase 1 | Homo sapiens |
| 4 | We determined whether CES1 inhibition and CES1 genetic polymorphisms would significantly influence the biotransformation of clopidogrel and alter the formation of the active metabolite. | Clopidogrel | carboxylesterase 1 | Homo sapiens |
| 5 | We determined whether CES1 inhibition and CES1 genetic polymorphisms would significantly influence the biotransformation of clopidogrel and alter the formation of the active metabolite. | Clopidogrel | carboxylesterase 1 | Homo sapiens |
| 6 | Coincubation of clopidogrel with the CES1 inhibitor bis(4-nitrophenyl) phosphate in human liver s9 fractions significantly increased the concentrations of clopidogrel, 2-oxo-clopidogrel, and clopidogrel active metabolite, while the concentrations of all formed carboxylate metabolites were significantly decreased. | Clopidogrel | carboxylesterase 1 | Homo sapiens |
| 7 | Coincubation of clopidogrel with the CES1 inhibitor bis(4-nitrophenyl) phosphate in human liver s9 fractions significantly increased the concentrations of clopidogrel, 2-oxo-clopidogrel, and clopidogrel active metabolite, while the concentrations of all formed carboxylate metabolites were significantly decreased. | Clopidogrel | carboxylesterase 1 | Homo sapiens |
| 8 | Coincubation of clopidogrel with the CES1 inhibitor bis(4-nitrophenyl) phosphate in human liver s9 fractions significantly increased the concentrations of clopidogrel, 2-oxo-clopidogrel, and clopidogrel active metabolite, while the concentrations of all formed carboxylate metabolites were significantly decreased. | Clopidogrel | carboxylesterase 1 | Homo sapiens |
| 9 | As anticipated, clopidogrel and 2-oxo-clopidogrel were efficiently hydrolyzed by the cell s9 fractions prepared from wild-type CES1 transfected cells. | Clopidogrel | carboxylesterase 1 | Homo sapiens |
| 10 | The enzymatic activity of the CES1 variants G143E and D260fs were completely impaired in terms of catalyzing the hydrolysis of clopidogrel and 2-oxo-clopidogrel. | Clopidogrel | carboxylesterase 1 | Homo sapiens |
| 11 | In summary, deficient CES1 catalytic activity resulting from CES1 inhibition or CES1 genetic variation may be associated with higher plasma concentrations of clopidogrel-active metabolite, and hence may enhance antiplatelet activity. | Clopidogrel | carboxylesterase 1 | Homo sapiens |
| 12 | In summary, deficient CES1 catalytic activity resulting from CES1 inhibition or CES1 genetic variation may be associated with higher plasma concentrations of clopidogrel-active metabolite, and hence may enhance antiplatelet activity. | Clopidogrel | carboxylesterase 1 | Homo sapiens |
| 13 | In summary, deficient CES1 catalytic activity resulting from CES1 inhibition or CES1 genetic variation may be associated with higher plasma concentrations of clopidogrel-active metabolite, and hence may enhance antiplatelet activity. | Clopidogrel | carboxylesterase 1 | Homo sapiens |
| 14 | Additionally, CES1 genetic variants have the potential to serve as a biomarker to predict clopidogrel response and individualize clopidogrel dosing regimens in clinical practice. | Clopidogrel | carboxylesterase 1 | Homo sapiens |
| 15 | Additionally, CES1 genetic variants have the potential to serve as a biomarker to predict clopidogrel response and individualize clopidogrel dosing regimens in clinical practice. | Clopidogrel | carboxylesterase 1 | Homo sapiens |