Pub. Date : 2005 Jun
PMID : 15687373
7 Functional Relationships(s)Download |
Sentence | Compound Name | Protein Name | Organism |
| 1 | Hydrolysis of capecitabine to 5"-deoxy-5-fluorocytidine by human carboxylesterases and inhibition by loperamide. | Capecitabine | carboxylesterase 2 | Homo sapiens |
| 2 | A three-step in vivo-targeted activation process requiring carboxylesterases, cytidine deaminase, and thymidine phosphorylase converts capecitabine to 5-fluorouracil. | Capecitabine | carboxylesterase 2 | Homo sapiens |
| 3 | Carboxylesterases hydrolyze capecitabine"s carbamate side chain to form 5"-deoxy-5-fluorocytidine (5"-DFCR). | Capecitabine | carboxylesterase 2 | Homo sapiens |
| 4 | This study examines the steady-state kinetics of recombinant human carboxylesterase isozymes carboxylesterase (CES) 1A1, CES2, and CES3 for hydrolysis of capecitabine with a liquid chromatography/mass spectroscopy assay. | Capecitabine | carboxylesterase 2 | Homo sapiens |
| 5 | Additionally, a spectrophotometric screening assay was utilized to identify drugs that may inhibit carboxylesterase activation of capecitabine. | Capecitabine | carboxylesterase 2 | Homo sapiens |
| 6 | CES1A1 and CES2 hydrolyze capecitabine to a similar extent, with catalytic efficiencies of 14.7 and 12.9 min(-1) mM(-1), respectively. | Capecitabine | carboxylesterase 2 | Homo sapiens |
| 7 | Both CES1A1 and CES2 are responsible for the activation of capecitabine, whereas CES3 plays little role in 5"-DFCR formation. | Capecitabine | carboxylesterase 2 | Homo sapiens |