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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

Live Europe PMC search

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Europe PMC · from cache · sorted by publication date

  1. 1
    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
  2. 2
    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
  3. 3
    Comparative Insights Into Detoxification, Regulation, and Evolution of Neonicotinoid Resistance in Three Planthoppers.

    Choi M, Khan M, Kim J. · 2026-05-01

    open access unreviewed
  4. 4
    A Multidimensional Workflow for Comprehensive Xenometabolome Profiling by Integrating TIMS-PASEF with LC-HRMS and Biotransformation-Informed Suspect and Nontarget Screening.

    Damalas DE, Thomaidis NS. · 2026-05-01

    open access unreviewed
  5. 5
    Dietary salt impairs circadian physiological metabolic adaptations in salt-sensitive hypertension.

    Dissanayake LV, Zietara A, Tiwari R, Lowe M, Kravtsova O, Levchenko V, Bohovyk R, Gumz ML, Staruschenko A. · 2026-03-11

    open access unreviewed
  6. 6
    Identification of potential key genes and molecular mechanisms of oral squamous cell carcinoma based on integrated bioinformatics approach.

    Alam MK, Islam MR, Haque T, Ganji KK, Babkair HA, Rashid ME, Ahmed K, Bui FM. · 2026-03-10

    open access unreviewed
  7. 7
    A Cross-Species Hydroquinone Model Replicates Smoking-Related Corneal Endothelial Oxidative Injury and Enables Therapeutic Screening of FGF10.

    Lee BJ, Agarwal D, Huang JH, Ivanova A, Bu JJ, Hill CA, Noguchi T, Jun JH, Makarenkova HP, Wahlin KJ, Shaw PX… · 2026-03-01

    open access unreviewed
  8. 8
    Molecular Epidemiology of <i>GSTM1</i> and <i>GSTT1</i> Null Genotypes in High-Altitude Andean Populations of Peru.

    Garcia-Paitan M, Campos-Semino C, Cansinos-Delgado Z, Merma-Rosales M, Enriquez-Laurente R, Santivañez SJ, Ja… · 2026-02-20

    open access unreviewed
  9. 9
    Virus-mediated changes in insect vector tolerance to a neonicotinoid insecticide.

    Schmidtbauer M, Withycombe J, Han J, Neher OT, Nachappa P. · 2026-02-20

    open access unreviewed
  10. 10
    LPCAT1 as a prognostic biomarker and risk indicator for hepatocellular carcinoma: insights into genes related to lipid metabolism.

    Zhai H, Wang J, He Y, Hong S, Huang K, Hu S, Xu J, Hao S, Zhang G, Shi X. · 2026-01-30

    open access unreviewed

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