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Understanding Human Carboxylesterase 2
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The first barrier oral drugs and prodrugs encounter prior to reaching an organism’s
systemic circulation is the gastrointestinal (GI) tract, specifically the intestine, which is
the primary section for absorption. Therefore, it is fundamental to understand the
permeability of the therapeutic agent as well as its potential metabolism by human
enterocytes, since biotransformation may result in the inactivation of the therapeutic
agent or, to the contrary, in the formation of more therapeutically active metabolites.
Carboxylesterases (CESs), phase I metabolising enzymes, are important in the
metabolism of several drugs and prodrugs with amide, ester, or thioester functional
groups. After cytochrome (CYP) P450s and UDP-glucuronosyltransferases (UGTs), CESs
are the most relevant enzymes for the metabolism of therapeutic agents.(...)
Descrição
Dissertation presented to obtain the Ph.D degree in Engineering and Technology Sciences, Biotechnology
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Universidade Nova de Lisboa. Instituto de Tecnologia Química e Biológica