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anti-Human UGT1A4 Antibodies:
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Genetic polymorphism in UGT1A4 and UGT2B7 may play a modest role in lamotrigine clearance changes during pregnancy. In addition, study indicates that the sex of the foetus influenced significantly the change in LTG clearance.
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 and UGT2B15 appear to be of minor importance.
This study aimed to analyze the relationship of UGT2B7 and UGT1A4 polymorphisms with metabolism of valproic acid (VPA) and lamotrigine (LTG) in epileptic children. UGT1A4 L48V polymorphism was not related with the serum concentration of LTG (F=5.328, P=0.006). L48V polymorphism also showed effects on efficacy of LTG (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.
Influence of valproic acid concentration and polymorphism of UGT1A4*3, UGT2B7 -161C > T and UGT2B7*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, UGT2B15 and UGT2B17 in 132 patients with estrogen receptor-positive breast cancer under treatment with tamoxifen
in tumor liver microsomes from HCC patients, either V(max) (maximum reaction rate, R(max) for UGT1A1) or clearance rates (V(max)/K(m), Clint) of UGT1A, UGT1A1, UGT1A4, UGT1A9 and UGT2B7 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.
Correlation of the UGT1A4 gene polymorphism with serum concentration and therapeutic efficacy of lamotrigine in Han Chinese of Northern China
Human UGT1A4 and UGT1A3 conjugate 25-hydroxyvitamin D3.
the substrate specificity of UGT2B10, highlighting its preference for tertiary amines with higher affinities and clearance values than those of UGT1A4 and UGT1A3.
Present results could be helpful to improve the use of UGT1A4 drug substrates in order to adjust them to the ethnic background of a given population, specifically for Hispanics.
study to determine the allelic frequency of two most common defective alleles: UGT1A4*2 and UGT1A4*3 in a Jordanian population
Polymorphic glucuronidation of olanzapine by uridine diphosphate glucuronosyltransferase 1A4 (UGT1A4) was investigated retrospectively in patient samples
Study identified a large number of genetic variations, including 13 intronic, 39 promoter, as well as 14 exonic polymorphisms, with 10 that lead to amino-acid changes.
UGT1A4(P24T) and UGT1A4(L48V) on LTG glucuronidation may lead to interindividual variations in lamotrigine metabolism in vivo
The frequencies of the heterozygous alleles for L48V or P24T polymorphisms were 22.4% and 3.8%, respectively. L48V polymorphism was found to decrease the serum lamotrigine concentration in Turkish epilepsy patients on monotherapy or polytherapy.
kinetic studies with recombinant UGT1A4 using various substrates: dihydrotestosterone, trans-androsterone, tamoxifen, lamotrigine -- evidence for multiple substrate binding sites
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