Comparative analysis of CYP3A expression in human liver suggests only a minor role for CYP3A5 in drug metabolism

Westlind-Johnsson, Anna; Malmebo, Sarah; Johansson, Anna; Otter, Charlotta; Andersson, Tommy B.; Johansson, Inger; Edwards, Robert J.; Boobis, Alan R.; Ingelman-Sundberg, Magnus

doi:10.1124/dmd.31.6.755

Cited by 258Pharmacogenetics and Drug MetabolismDrug Transport and Resistance MechanismsDrug-Induced Hepatotoxicity and Protection

Comparative analysis of CYP3A expression in human liver suggests only a minor role for CYP3A5 in drug metabolism

Westlind-Johnsson, Anna, Malmebo, Sarah, Johansson, Anna, Otter, Charlotta, Andersson, Tommy B., Johansson, Inger, Edwards, Robert J., Boobis, Alan R. +1 more·2003·Drug Metabolism and Disposition

DOI 10.1124/dmd.31.6.755

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Abstract

To study mechanisms behind the interindividual variability in CYP3A expression and the relative contribution of the different CYP3A enzymes to the overall CYP3A activity, we have analyzed CYP3A4, CYP3A5, CYP3A43, and PXR mRNA and CYP3A4 and CYP3A5 protein expression, catalytic activity, and polymorphism in the CYP3A5 gene in a panel of 46 Caucasian human livers. Protein quantification was performed by Western blotting using enzyme-specific antibodies directed to the C termini of CYP3A4 or CYP3A5, and carrier protein-coupled peptides as standards. The mRNA levels were determined by quantitative real-time PCR. CYP3A activity was measured by analysis of the rate of testosterone 6beta-hydroxylation. A correlation existed between all CYP3A and PXR mRNA transcripts measured. The interindividual variability in CYP3A4 and CYP3A5 mRNA expression was higher than that of CYP3A protein and activity. The CYP3A5 protein was expressed at quantifiable levels in 5 (10.9%) of the livers. Four of those were heterozygous for the CYP3A5*1 allele and had CYP3A5 protein at a mean level of 17% of that of total CYP3A, whereas one liver sample was from a CYP3A5*3 homozygote individual having lower amounts of CYP3A5. In total, CYP3A5 only contributed 2% of the overall CYP3A protein among all samples. In conclusion, our data indicate that CYP3A4, CYP3A5, CYP3A43, and PXR hepatic mRNA expression correlate, indicating common regulatory features, and that the contribution of CYP3A5 to hepatic drug metabolism in Caucasians is insignificant.

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CYP3A5 catalyzes a comparable range of reactions as CYP3A4.
“CYP3A5 catalyzes a comparable range of reactions as CYP3A4”
From Human steroid biosynthesis, metabolism and excretion are differentially reflected by serum and urine steroid metabolomes: a comprehensive review (2019) · cites this paper as [124]
CYP3A5's role in drug and steroid metabolism is limited due to its generally low activity and expression in a relatively small percentage of individuals.
“but its role in drug and steroid metabolism is limited due to its generally low activity and expression in a relatively small percentage of individuals [[123], [124], [125]].”
From Human steroid biosynthesis, metabolism and excretion are differentially reflected by serum and urine steroid metabolomes: a comprehensive review (2019) · cites this paper as [124]

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Authors: Westlind-Johnsson, A., Malmebo, S., Johansson, A., Otter, C., Andersson, T. B., Johansson, I., Edwards, R. J., Boobis, A. R., & Ingelman-Sundberg, M.
Affiliations: Karolinska Institutet (SE)
ORCID: Johansson, Inger
Boobis, Alan R.
Venue: Drug Metabolism and Disposition
Publisher: Elsevier BV
Published: 2003-06
Volume: 31
Issue: 6
Pages: 755-761
ISSN: 0090-9556 (ISSN-L)
DOI: 10.1124/dmd.31.6.755
OpenAlex: W2126772533
Cited by: 258
References: 39
Citations by year: 2026: 2 · 2025: 7 · 2024: 7 · 2023: 3 · 2022: 6 · 2021: 5 · 2020: 5 · 2019: 13 · 2018: 6 · 2017: 6 · 2016: 8 · 2015: 3 · 2014: 9 · 2013: 23 · 2012: 8
FWCI: 22.15
Type: journal article
Language: en
Open access: closed
Licence: www.elsevier.com/tdm/userlicense/1.0/ (tdm)
www.elsevier.com/legal/tdmrep-license (tdm)
Locations: Drug Metabolism and Disposition (publishedVersion)
PubMed (publishedVersion)
Topics: Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmacology › Pharmacogenetics and Drug Metabolism
Health Sciences › Medicine › Oncology › Drug Transport and Resistance Mechanisms
Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmacology › Drug-Induced Hepatotoxicity and Protection
Keywords: CYP3A4, CYP3A5, CYP3A43, pregnane X receptor, interindividual variability, drug metabolism, testosterone 6beta-hydroxylation, CYP3A5*3 allele, hepatic mRNA expression, human liver
MeSH terms: Pregnane X Receptor, Alleles, Aryl Hydrocarbon Hydroxylases, Cytochrome P-450 Enzyme System, Genotype, Humans, Hydroxylation, Microsomes, Liver, Polymorphism, Genetic, Receptors, Steroid, RNA, Messenger, Testosterone, Blotting, Western, Gene Expression, Polymerase Chain Reaction, Receptors, Cytoplasmic and Nuclear, White People, Cytochrome P-450 CYP3A

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Comparative analysis of CYP3A expression in human liver suggests only a minor role for CYP3A5 in drug metabolism

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