大鼠重组尿苷二磷酸葡萄糖醛酸基转移酶1.1（胆红素UGT）对类视黄醇的葡萄糖醛酸化作用。
Glucuronidation of retinoids by rat recombinant UDP: glucuronosyltransferase 1.1 (bilirubin UGT).
作者信息
Radominska A, Little J M, Lehman P A, Samokyszyn V, Rios G R, King C D, Green M D, Tephly T R
机构信息
Department of Medicine, University of Arkansas for Medical Sciences, Little Rock 72205, USA.
出版信息
Drug Metab Dispos. 1997 Jul;25(7):889-92.
Rat liver recombinant BR1UGT1.1 was found to have significant activity toward retinoid substrates. UGT1.1 glucuronidation activity was 91 +/- 18 pmol/mg x min for atRA and 113 +/- 19 pmol/mg x min for 5,6-epoxy-atRA. The apparent K(M) and V(max) of atRA acid glucuronidation by UGT1.1 were 59.1 +/- 5.4 microM and 158 +/- 43 pmol/mg x min, respectively. SDS-PAGE and Western blot analysis of UGT1.1-transfected HK293 membrane proteins photolabeled with [11,12-3H]atRA revealed a protein of approximately 56 kDa that was labeled by [3H]atRA, detected by anti-pNP UGT antibody and not present in membranes from nontransfected HK293 cells. Liver microsomes from Gunn rats, which lack UGT1.1, had significant activity toward atRA (111 +/- 28 pmol/mg x min).
大鼠肝脏重组BR1UGT1.1对类视黄醇底物具有显著活性。UGT1.1的葡萄糖醛酸化活性对于全反式视黄酸（atRA）为91±18 pmol/mg×min，对于5,6-环氧-atRA为113±19 pmol/mg×min。UGT1.1对atRA酸进行葡萄糖醛酸化的表观米氏常数（K(M)）和最大反应速度（V(max)）分别为59.1±5.4 μM和158±43 pmol/mg×min。用[11,12-³H]atRA进行光标记的UGT1.1转染的HK293膜蛋白的SDS-聚丙烯酰胺凝胶电泳（SDS-PAGE）和蛋白质免疫印迹分析显示，一个约56 kDa的蛋白被[³H]atRA标记，可被抗对硝基苯磷酸酯UGT抗体检测到，且不存在于未转染的HK293细胞的膜中。缺乏UGT1.1的Gunn大鼠的肝脏微粒体对atRA具有显著活性（111±28 pmol/mg×min）。
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