title: The Role of Xenobiotic-Metabolizing Enzymes in Anthelmintic Deactivation and Resistance in Helminths.
abstract: Xenobiotic-metabolizing enzymes (XMEs) modulate the biological activity and behavior of many drugs, including anthelmintics. The effects of anthelmintics can often be abolished by XMEs when the drugs are metabolized to an inefficient compound. XMEs therefore play a significant role in anthelmintic efficacy. Moreover, differences in XMEs between helminths are reflected by differences in anthelmintic metabolism between target species. Taking advantage of the newly sequenced genomes of many helminth species, progress in this field has been remarkable. The present review collects up to date information regarding the most important XMEs (phase I and phase II biotransformation enzymes; efflux transporters) in helminths. The participation of these XMEs in anthelmintic metabolism and their possible roles in drug resistance are evaluated.
authors.affiliation: Department of Biochemical Sciences, Charles University in Prague, Faculty of Pharmacy in Hradec Králové, 500 05 Hradec Králové, Czech Republic.
authors.forename: Petra
authors.initials: P
authors.lastname: Matoušková
authors.affiliation: Department of Pharmacology and Toxicology, Charles University in Prague, Faculty of Pharmacy, Heyrovského 1203, Hradec Králové, 500 05, Czech Republic.
authors.forename: Ivan
authors.initials: I
authors.lastname: Vokřál
authors.affiliation: Department of Pharmacology and Toxicology, Charles University in Prague, Faculty of Pharmacy, Heyrovského 1203, Hradec Králové, 500 05, Czech Republic.
authors.forename: Jiří
authors.initials: J
authors.lastname: Lamka
authors.affiliation: Department of Biochemical Sciences, Charles University in Prague, Faculty of Pharmacy in Hradec Králové, 500 05 Hradec Králové, Czech Republic. Electronic address: skaloval@faf.cuni.cz.
authors.forename: Lenka
authors.initials: L
authors.lastname: Skálová
mesh_terms: D000818:Animals; D000871:Anthelmintics / Q000378:metabolism* / Q000494:pharmacology*; D004351:Drug Resistance / Q000235:genetics*; D049751:Genome, Helminth / Q000235:genetics*; D015801:Helminth Proteins / Q000235:genetics / Q000378:metabolism; D006376:Helminths / Q000187:drug effects* / Q000201:enzymology*; D006790:Host-Parasite Interactions / Q000235:genetics
chemical_list: D000871:Anthelmintics; D015801:Helminth Proteins
keywords: detoxification; drug biotransformation; drug resistance; drug transport