Functional analysis of carboxylesterase in human induced pluripotent stem cell-derived enterocytes

• Published in: Biochemical and biophysical research communications Vol. 486; no. 1; pp. 143 - 148
• Main Authors: Kabeya, Tomoki, Matsumura, Wakana, Iwao, Takahiro, Hosokawa, Masakiyo, Matsunaga, Tamihide
• Format: Journal Article
• Language: English
• Published: United States Elsevier Inc 22.04.2017
• Subjects: Benzimidazoles - pharmacology; Benzoates - pharmacology; Blotting, Western; Caco-2 Cells; Caco-2 cells; Carboxylesterase; Carboxylesterase - antagonists & inhibitors; Carboxylesterase - genetics; Carboxylesterase - metabolism; Cell Differentiation; Cell Line; Enterocytes; Enterocytes - cytology; Enterocytes - enzymology; Enterocytes - metabolism; Gene Expression; Human induced pluripotent stem cells; Humans; Hydrolysis - drug effects; Induced Pluripotent Stem Cells - cytology; Induced Pluripotent Stem Cells - enzymology; Induced Pluripotent Stem Cells - metabolism; Intestine, Small - enzymology; Intestine, Small - metabolism; Isoenzymes - antagonists & inhibitors; Isoenzymes - genetics; Isoenzymes - metabolism; Metabolic activity; Nitrophenols - metabolism; Reverse Transcriptase Polymerase Chain Reaction; Substrate Specificity; RT; Metabolic activity; SDS; FGF; S9; PAGE; PNPA; Carboxylesterase; iPS; MEGX; Caco-2 cells; CES; BSA; DMEM; Enterocytes; NEAA; FBS; Human induced pluripotent stem cells; GAPDH; HPLC; PCR

Human carboxylesterase (CES) is a key esterase involved in the metabolism and biotransformation of drugs. Hydrolysis activity in the human small intestine is predominantly mediated by CES2A1 rather than CES1A. In drug development studies, Caco-2 cells are commonly used as a model to predict drug abs...