ArticleThe Journal of steroid biochemistry and molecular biology2019
Major glucuronide metabolites of testosterone are primarily transported by MRP2 and MRP3 in human liver, intestine and kidney.
Article in The Journal of steroid biochemistry and molecular biology, 2019. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 35 papers, 1 of them a synthesis that pooled it.
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Who cites it
35 citing papers in PubMed, 1 synthesis or guideline pooled it, 71 citations in OpenAlex.
- Association Between Sex Hormone Levels and Gut Microbiota Composition and Diversity-A Systematic Review.Journal of clinical gastroenterologyPooled it
- Assessing Transporter-Mediated Natural Product-Drug Interactions Via In vitro-In Vivo Extrapolation: Clinical Evaluation With a Probe Cocktail.Clinical pharmacology and therapeutics · 2021Trial
- The effects of androgens on drug metabolism and transport: clinical pharmacologic considerations for people assigned female at birth.Expert opinion on drug metabolism & toxicology · 2026Article
- Gut microbiota and their role in male reproductive health.NPJ science of food · 2026Review
- Comprehensive metabolic profiling of fluoxymesterone in vivo by GC-Orbitrap HRMS: a integrated strategy for novel biomarkers discovery in doping analysis.Analytical and bioanalytical chemistry · 2026Article
- Understanding the Secular Decline in Testosterone: Mechanisms, Consequences, and Clinical Perspectives.International journal of molecular sciences · 2026Review
- Enhancing therapeutic strategies and drug development for patients with kidney disease.Expert opinion on drug safety · 2026Review
- The role of metabolites in the causal effect of immune cell phenotypes on immunotherapy toxicity risk.Discover oncology · 2025Article
- Cntn4 Gene Deficiency Promotes Autism-Like Phenotypes Associated with Gut Microbiota Perturbations and Gut-Brain Axis Metabolomic Alterations in Mice.Molecular neurobiology · 2025Article
- Integrating Advanced Metabolomics and Machine Learning for Anti-Doping in Human Athletes.Metabolites · 2025Review
- Human Internal Exposures of Bisphenol A and Six Data-Poor Analogs Predicted by Physiologically Based Kinetic Models with Multimodal Parametrization.Environmental science & technology · 2025Article
- Establishing scientific confidence in a two-chamber co-culture system to evaluate androgenic response in the presence of hepatic metabolism.Toxicology letters · 2025Article
- Comparative Effects of the Single and Binary Fermentations ofMicroorganisms · 2025Article
- Biotransformation and kinetics of selected benzimidazole synthetic opioids in human hepatocytes.Frontiers in pharmacology · 2025Article
- Role of intestinal testosterone-degrading bacteria and 3/17β-HSD in the pathogenesis of testosterone deficiency-induced hyperlipidemia in males.NPJ biofilms and microbiomes · 2024Article
- Article
- Physiologically based pharmacokinetics modeling and transporter proteomics to predict systemic and local liver and muscle disposition of statins.CPT: pharmacometrics & systems pharmacology · 2024Article
- Development of a human liver microphysiological coculture system for higher throughput chemical safety assessment.Toxicological sciences : an official journal of the Society of Toxicology · 2024Article
- Emerging Role of ABC Transporters in Glia Cells in Health and Diseases of the Central Nervous System.Cells · 2024Review
- Article
Corrections and comments
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Authors and funding
6 authors at 3 institutions in 2 countries.
Funding
Abstract
Testosterone glucuronide (TG), androsterone glucuronide (AG), etiocholanolone glucuronide (EtioG) and dihydrotestosterone glucuronide (DHTG) are the major metabolites of testosterone (T), which are excreted in urine and bile. Glucuronides can be deconjugated to active androgen in gut lumen after biliary excretion, which in turn can affect physiological levels of androgens. The goal of this study was to quantitatively characterize the mechanisms by which TG, AG, EtioG and DHTG are eliminated from liver, intestine, and kidney utilizing relative expression factor (REF) approach. Using vesicular transport assay with recombinant human MRP2, MRP3, MRP4, MDR1 and BCRP, we first identified that TG, AG, EtioG, and DHTG were primarily substrates of MRP2 and MRP3, although lower levels of transport were also observed with MDR1 and BCRP vesicles. The transport kinetic analyses revealed higher intrinsic clearances of TG by MRP2 and MRP3 as compared to that of DHTG, AG, and EtioG. MRP3 exhibited higher affinity for the transport of the studied glucuronides than MRP2. We next quantified the protein abundances of these efflux transporters in vesicles and compared the same with pooled total membrane fractions isolated from human tissues by quantitative LC-MS/MS proteomics. The fractional contribution of individual transporters (f
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