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Plant steroids competitively inhibited the UGT1A4-catalyzed trifluoperazine glucuronidation reaction suggesting potential for herb-drug interactions to occur.
Our findings highlight the influence of UGTT1A4 haplotypes on tamoxifen disposition in Asian breast cancer patients, while genetic variants in UGT2B7 (show UGT2B7 Proteins) and UGT2B15 (show UGT2B15 Proteins) appear to be of minor importance.
This study aimed to analyze the relationship of UGT2B7 (show UGT2B7 Proteins) and UGT1A4 polymorphisms with metabolism of valproic acid (VPA) and lamotrigine (LTG (show TNFSF14 Proteins)) in epileptic children. UGT1A4 L48V polymorphism was not related with the serum concentration of LTG (show TNFSF14 Proteins) (F=5.328, P=0.006). L48V polymorphism also showed effects on efficacy of LTG (show TNFSF14 Proteins) (chi2=17.397, P=0.001).
No association between non-bullous skin reactions from lamotrigine and heterozygosity of UGT1A4 genetic variants *2(P24T) or *3(L48V) in Norwegian patients.
The frequencies of two common UGT1A4 variants, *2 (P24T) and *3 (L48V), and their potential effects on serum concentrations of LTG (show TNFSF14 Proteins).
Influence of valproic acid concentration and polymorphism of UGT1A4*3, UGT2B7 (show UGT2B7 Proteins) -161C > T and UGT2B7 (show UGT2B7 Proteins)*2 on serum concentration of lamotrigine in Chinese epileptic children
This descriptive study examines correlations between concentrations of tamoxifen's glucuronide metabolites and genotypes UGT1A4, UGT2B7 (show UGT2B7 Proteins), UGT2B15 (show UGT2B15 Proteins) and UGT2B17 in 132 patients with estrogen receptor (show ESR1 Proteins)-positive breast cancer under treatment with tamoxifen
in tumor liver microsomes from HCC (show FAM126A Proteins) patients, either V(max) (maximum reaction rate, R(max) for UGT1A1 (show UGT1A1 Proteins)) or clearance rates (V(max)/K(m), Clint (show CLINT1 Proteins)) of UGT1A (show UGT1A1 Proteins), UGT1A1 (show UGT1A1 Proteins), UGT1A4, UGT1A9 (show UGT1A9 Proteins) and UGT2B7 (show UGT2B7 Proteins) were lower than those in the adjacent normal liver microsomes
The association between the UGT1A4 promoter and coding region SNPs and the glucuronidation rates of Tam (show CCNA1 Proteins).
Correlation of the UGT1A4 gene polymorphism with serum concentration and therapeutic efficacy of lamotrigine in Han Chinese of Northern China
This gene encodes a UDP-glucuronosyltransferase, an enzyme of the glucuronidation pathway that transforms small lipophilic molecules, such as steroids, bilirubin, hormones, and drugs, into water-soluble, excretable metabolites. This gene is part of a complex locus that encodes several UDP-glucuronosyltransferases. The locus includes thirteen unique alternate first exons followed by four common exons. Four of the alternate first exons are considered pseudogenes. Each of the remaining nine 5' exons may be spliced to the four common exons, resulting in nine proteins with different N-termini and identical C-termini. Each first exon encodes the substrate binding site, and is regulated by its own promoter. This enzyme has some glucuronidase activity towards bilirubin, although is is more active on amines, steroids, and sapogenins.
UDP glycosyltransferase 1 family, polypeptide A4
, UDP-glucuronosyltransferase 1-4
, UDP-glucuronosyltransferase 1-D
, UDP-glucuronosyltransferase 1A4
, bilirubin UDP-glucuronosyltransferase isozyme 2
, bilirubin-specific UDPGT isozyme 2