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Drug Metabolism Synthetic (Phase II) Reactions

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The ADME Encyclopedia

Synonyms

Conjugation reactions; Phase 2 biotransformation; Phase 2 metabolism; Phase 2 reactions; Phase II biotransformation; Phase II metabolism; Phase II reactions; Synthetic metabolism; Synthetic reactions

Definition

In synthetic (or Phase II or conjugation) reactions, an endogenous or exogenous compound (the substrate of the reaction) is coupled to an endogenous conjugating moiety (sometimes called endocon). The conjugating moiety is usually polar and in the range of 100 to 300 Da (there are exceptions to this, though). The endocon is in general supplied by a cofactor (a coenzyme or co-substrate) where a high-energy chemical bond links the cofactor to the endocon. Synthetic reactions are almost always catalyzed by transferases [1]. The Phase II denomination comes from Williams’ classic nomenclature and can be misleading, as it reflects the notion of sequential metabolism, where the parent drug is converted to a primary (or first-generation) metabolite, which in turn is subjected...

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Talevi, A., Bellera, C.L. (2021). Drug Metabolism Synthetic (Phase II) Reactions. In: The ADME Encyclopedia. Springer, Cham. https://doi.org/10.1007/978-3-030-51519-5_64-1

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  • DOI: https://doi.org/10.1007/978-3-030-51519-5_64-1

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