Target intelligence / Profile preview

UDP-glucuronosyltransferase 2B28 (UGT2B28)

Target
UGT2B28
Molecular classification
Enzyme, UDP-glucuronosyltransferase family, Glycosyltransferase (GT) 1 family
01

Overview

UDP-glucuronosyltransferase 2B28 is an enzyme of the glycosyltransferase 1 family, coded by the UGT2B28 gene and primarily found in the endoplasmic reticulum of steroidogenic tissues. It catalyzes the transfer of glucuronic acid to a broad range of lipophilic substrates—including steroid hormones (such as androgens and estrogens), bile acids, and xenobiotics—via glucuronidation, a key phase II metabolic process for detoxification and elimination. Beyond its enzymatic role, UGT2B28 is functionally implicated in modulating androgen and lipid signaling, especially in prostate cancer, where its expression is associated with tumor progression and is influenced by androgen receptor activity. UGT2B28 also participates in feedback loops in steroid metabolism, and evidence suggests it may serve as a biomarker for disease aggressiveness and therapeutic response in androgen-driven cancers[1][2][3][5][7].

Other names
UDP glucuronosyltransferase family 2 member B28UDP-glucuronosyltransferase 2B28UDPGT 2B28UDP glucuronosyltransferase 2 family, polypeptide B28UDP glycosyltransferase 2 family, polypeptide B28
02

Mechanism of action

For drugs/substrates: glucuronidation—conjugation with glucuronic acid, increasing water solubility and facilitating excretion. Potential indirect modulation of androgen signaling via enzyme regulatory roles and heterodimerization with other UGTs, blocking clearance of active androgens in cancer.

03

Biological functions

Glucuronidation (phase II drug metabolism)Steroid and androgen metabolismDetoxification and elimination of xenobiotics and endogenous compoundsRegulation of lipid synthesis and metabolism (via SREBP pathway)Modulation of steroid signaling feedback
04

Disease associations

Cancer (notably prostate cancer and possibly breast cancer)Crigler-Najjar syndrome (Type I)Kernicterus
05

Safety considerations

Potential challenges due to inter-individual genetic variability or polymorphism affecting enzyme functionAltered UGT2B28 activity may impact steroid hormone balance and drug metabolism, potentially influencing efficacy and toxicity profiles for affected patients
06

Interacting drugs

No specific drug inhibitors or substrates of UGT2B28 uniquely known; general UGT substrates, which may include steroids (testosterone, dihydrotestosterone, estradiol, estrone), bile acids, and certain phenolic compounds (like eugenol). No FDA-approved drugs are selectively targeting UGT2B28 specifically as of current knowledge.
07

Biomarkers

UGT2B28 expression levels as a potential biomarker for prostate cancer aggressiveness and progressionUGT2B28 expression may also be considered for patient stratification in androgen-driven cancers

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