Title : Irinotecan activation by human carboxylesterases in colorectal adenocarcinoma cells.

Pub. Date : 2002 Aug

PMID : 12171903






5 Functional Relationships(s)
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1 We reported recently that human carboxylesterase-2 (hCE-2) is a higher-affinity, higher-velocity enzyme for irinotecan hydrolysis when compared with hCE-1. Irinotecan carboxylesterase 2 Homo sapiens
2 We reported recently that human carboxylesterase-2 (hCE-2) is a higher-affinity, higher-velocity enzyme for irinotecan hydrolysis when compared with hCE-1. Irinotecan carboxylesterase 2 Homo sapiens
3 Extracts of HT29 cells transfected with hCE-2 exhibited significantly higher irinotecan hydrolysis (5.2 pmol/mg protein/hr) than hCE-1 (1.0 pmol/mg protein/hr). Irinotecan carboxylesterase 2 Homo sapiens
4 HT29 cells over-expressing hCE-2 were more sensitive to the toxic effects of irinotecan than cells expressing hCE-1 (EC50 = 0.3 micro M and 6.8 micro M, respectively). Irinotecan carboxylesterase 2 Homo sapiens
5 Our data further support the notion that hCE-2 plays a substantial role in irinotecan activation in human tissue at relevant pharmacologic concentrations. Irinotecan carboxylesterase 2 Homo sapiens