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PW-051 Xenobiotic & Drug Metabolism Biotransformation unreviewed

Phase I - Functionalization

Lipophilic xenobiotic/drug Oxidised, reduced or hydrolysed metabolite
Compartment
Smooth ER (microsomes), mitochondria
Main tissue
Liver mainly; intestine, lung, kidney
Rate-limiting
Cytochrome P450 monooxygenases (CYP)
Steps
3

Reaction steps

In source order, 3 total

showing 1–3
  1. 1

    Drug + O2 + NADPH -> hydroxylated/oxidized drug + H2O + NADP+

    Cytochrome P450 monooxygenases (CYP) 1.14.14.1 ST-0367 Irreversible/directional rate-limiting NADPH O2 heme CYP reductase
    In O2 NADPH
    Out Hydroxylated/oxidized drug H2O NADP+
    › Notes

    Smooth ER of hepatocytes. Introduces or exposes a polar group. CYP3A4 handles roughly half of all drugs.

  2. 2

    Ester or amide + H2O -> acid + alcohol/amine

    Esterases and amidases ST-0368 Irreversible/directional H2O
    In Ester or amide H2O
    Out Alcohol/amine
    › Notes

    Non-CYP hydrolysis, e.g. aspirin to salicylate.

  3. 3

    Amine + O2 + H2O -> aldehyde + NH3 + H2O2

    Monoamine oxidase (MAO-A/MAO-B) 1.4.3.4 ST-0369 Irreversible/directional FAD O2
    In Amine O2 H2O
    Out NH3 H2O2
    › Notes

    Outer mitochondrial membrane; MAO inhibition plus dietary tyramine causes hypertensive crisis.

Showing all 3 steps.

Recent literature

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Europe PMC · fetched just now · sorted by publication date

  1. 1
    Transcriptome Analysis and Characterization of Two Detoxification Genes Responding to Imidacloprid in <i>Aphis spiraecola</i>.

    Zhang M, Si C, Liu H, Chai L. · 2026-09-21

    open access unreviewed
  2. 2
    Midlife Growth Hormone Receptor Ablation Extends Healthy Lifespan and Induces Sex-Specific Hepatic Transcriptional Changes at Single-Cell Resolution.

    Duran-Ortiz S, List EO, Young JA, Ikeno Y, Zhu S, McHugh T, O'Connor PM, Kim M, Benayoun BA, Benencia F, Basu… · 2026-09-01

    open access unreviewed
  3. 3
    Analysis of transcriptomic alterations induced by 33 different per- and polyfluoroalkyl substances (PFAS) in differentiated HepaRG cells.

    Sprenger H, Alker W, Rocchi A, Leo C, Giglio R, Immobile Molaro G, Dondero F, Braeuning A, Buhrke T. · 2026-05-13

    open access unreviewed
  4. 4
    Tumor-derived Parathyroid Hormone-Related Protein Is Associated with Suppression of Cytochrome P450 Expression: Evidence From Multimodal Transcriptomics.

    Fujita I, Kaji T, Noguchi I, Tokumaru K, Maeda H, Maruyama T, Watanabe H. · 2026-06-22

    unreviewed
  5. 5
    Target-gene overexpression and metabolic enhancement confer bentazone resistance in Amaranthus retroflexus.

    Liu C, Wang S, Ma D, Liu X, Xu X, Sun W, Li C, Sun Z, Teng C. · 2026-05-01

    unreviewed
  6. 6
    Combined Exposure to 1,2-Dichloropropane and Dichloromethane Enhances Hepatocellular Tumor Development in Mice.

    Gi M, Fujioka M, Vachiraarunwong A, Kawachi S, Qiu G, Guo R, Kawamura Y, Pan J, Kusunoki Y, Kakehashi A, Suzu… · 2026-07-30

    open access unreviewed
  7. 7
    PMconv: How to Compare Proteomes and Metabolomes?

    Kozlova A, Kliuchnikova A, Gordeeva A, Lisitsa A, Ponomarenko E, Ilgisonis E. · 2026-06-04

    open access unreviewed
  8. 8
    Temporal transcriptomic profiling identifies core regulators in cytokine-induced gut barrier disruption in differentiated Caco-2 cells.

    Yoon HS, Ma S, Kanke M, Wu WJ, Hoang U, Tan JA, Wilks A, Patel P, Chandra S, Luo X, Lu D, Martin S, Wilson M,… · 2026-06-08

    open access unreviewed
  9. 9
    High-performance proteomics reveals immune, epithelial, and vascular dysregulation underlying lacrimal fluid defects in patients with aniridia.

    Willems M, Vialaret J, Girard M, Feret N, Bremond-Gignac D, Chassaing N, Kindermans J, Fichter L, Hirtz C, Mo… · 2026-05-27

    cited 1× open access unreviewed
  10. 10
    Transcriptomic and functional responses of human airway cells to vaped ∆8-THC and its oxidation product ∆8-THCQ.

    Love CA, Kim HH, Rager JE, Tallman KA, Schichlein KD, Porter NA, Jaspers I. · 2026-05-15

    open access unreviewed

External claims. These come from an index outside this database and are not checked against it. Treat them as leads.