Inactivation of androgens by UDP-glucuronosyltransferase enzymes in humans

Bélanger, Alain; Pelletier, Georges; Labrie, Fernand; Barbier, Olivier; Chouinard, Sarah

doi:10.1016/j.tem.2003.10.005

Cited by 235Pharmacogenetics and Drug MetabolismProstate Cancer Treatment and ResearchDrug Transport and Resistance Mechanisms

Inactivation of androgens by UDP-glucuronosyltransferase enzymes in humans

Bélanger, Alain, Pelletier, Georges, Labrie, Fernand, Barbier, Olivier, Chouinard, Sarah·2003·Trends in Endocrinology & Metabolism

DOI 10.1016/j.tem.2003.10.005

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Abstract

In humans, 3beta-hydroxysteroid dehydrogenase (3beta-HSD), 17beta-HSD and 5alpha-reductase activities in androgen target tissues, such as the prostate and skin, convert dehydroepiandrosterone, androstenedione and testosterone into the most potent natural androgen dihydrotestosterone (DHT). This androgen is converted mainly in situ into two phase I metabolites, androsterone (ADT) and androstane-3alpha,17beta-diol (3alpha-DIOL), which might be back converted to DHT. Here, we discuss the recent findings regarding the characterization of specific UDP-glucuronosyltransferases (UGTs), UGT2B7, B15 and B17, responsible for the glucuronidation of these metabolites. The tissue distribution and cellular localization of the UGT2B transcripts and proteins in humans clearly indicate that these enzymes are synthesized in androgen-sensitive tissues. It is postulated that the conjugating activity of UGT enzymes is the main mechanism for modulating the action of steroids and protecting the androgen-sensitive tissues from deleteriously high concentrations of DHT, ADT and 3alpha-DIOL.

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The glucuronidation of C19 steroids is catalyzed by three members of the UGT2B subfamily: UGT2B7, UGT2B15 and UGT2B17.
“The glucuronidation of C19 steroids is catalyzed by three members of the UGT2B subfamily, namely: UGT2B7, UGT2B15 and UGT2B17 [175].”
From Human steroid biosynthesis, metabolism and excretion are differentially reflected by serum and urine steroid metabolomes: a comprehensive review (2019) · cites this paper as [175]
As opposed to sulfation, glucuronidation is irreversible and ultimately inactivates the androgen and initiates its renal excretion by increasing polarity and water solubility.
“As opposed to sulfation, glucuronidation is irreversible and ultimately inactivates the androgen and initiates its renal excretion by increasing polarity and water solubility of the molecule (Belanger et al., 2003).”
From Intracrine androgen biosynthesis, metabolism and action revisited (2018) · cites this paper as Belanger et al., 2003

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“The expression of UGTs in adipose tissue (Tchernof et al., 1999) and the correlation of plasma 3a-adiol glucuronide with fat mass in men (Tchernof et al., 1997) suggest phase 2 metabolism as final step of androgen inactivation in adipocytes.”
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Authors: Bélanger, A., Pelletier, G., Labrie, F., Barbier, O., & Chouinard, S.
Affiliations: Centre hospitalier de l'Université Laval (CA)
Corresponding author: Bélanger, Alain
ORCID: Barbier, Olivier
Venue: Trends in Endocrinology & Metabolism
Publisher: Elsevier BV
Published: 2003-12
Volume: 14
Issue: 10
Pages: 473-479
ISSN: 1043-2760 (ISSN-L)
DOI: 10.1016/j.tem.2003.10.005
OpenAlex: W1988871942
Cited by: 235
References: 74
Citations by year: 2026: 2 · 2025: 5 · 2024: 8 · 2023: 5 · 2022: 12 · 2021: 9 · 2020: 8 · 2019: 8 · 2018: 8 · 2017: 17 · 2016: 11 · 2015: 13 · 2014: 11 · 2013: 18 · 2012: 8
FWCI: 0.66
Type: journal article
Language: en
Open access: closed
Licence: www.elsevier.com/tdm/userlicense/1.0/ (tdm)
Locations: Trends in Endocrinology and Metabolism (publishedVersion)
PubMed (publishedVersion)
Topics: Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmacology › Pharmacogenetics and Drug Metabolism
Health Sciences › Medicine › Pulmonary and Respiratory Medicine › Prostate Cancer Treatment and Research
Health Sciences › Medicine › Oncology › Drug Transport and Resistance Mechanisms
Keywords: androgen metabolism, UDP-glucuronosyltransferase, UGT2B7, UGT2B15, UGT2B17, dihydrotestosterone, androstanediol, androstanediol glucuronide, glucuronidation, 3β-hydroxysteroid dehydrogenase, 17β-hydroxysteroid dehydrogenase, 5α-reductase, prostate, skin
MeSH terms: Androgens, Humans, Isoenzymes, Male, Prostate, Prostatic Neoplasms, Skin, Glucuronosyltransferase

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Inactivation of androgens by UDP-glucuronosyltransferase enzymes in humans

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