PharmGKB summary: very important pharmacogene information for UGT1A1.
PharmGKB summary: very important pharmacogene information for UGT1A1.
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DOI：
10.1097/fpc.0000000000000024
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发表时间：
2014-03
影响因子：
2.6
通讯作者：
Altman RB
中科院分区：
文献类型：
--
作者：
Barbarino JM;Haidar CE;Klein TE;Altman RB
尿苷二磷酸葡萄糖醛酸糖基转移酶（UGT）酶是一个负责靶底物葡萄糖醛酸化的超家族酶。葡萄糖醛酸的转移使外源药物和其他内源性化合物可溶于水，从而使其在胆道或肾脏中消除。UGT家族负责数百种化合物的糖醛酸化，包括激素、类黄酮和环境诱变剂bbb。UGT家族的大多数成员在肝脏以及其他类型的组织（如肠、胃或乳腺组织）中表达。少数成员仅在肝外表达，如UGT1A7、UGT1A8、UGT1A10和UGT2A1[2]。UGT超家族中存在四个家族：UGT1A、UGT2、UGT3和ugt8[3]。UGT2进一步分为UGT2A和UGT2B两个亚家族，它们都存在于染色体4[2]上。UGT2A酶参与化合物的葡萄糖醛酸化，如酚类气味剂和多环芳烃代谢产物，尽管对该亚家族的研究有限。UGT2B蛋白主要负责类固醇[5]的代谢。UGT3和UGT8家族成员的作用尚未得到很好的表征。UGT1A家族位于染色体2q37上，该家族成员含有多种葡萄糖醛酸盐化合物。药物是UGT1A家族[1]的共同底物，这使得该组中的酶与药物遗传学研究相关。这个关于UGT1A1的非常重要的药物基因摘要可在PharmGKB网站http://www上获得遗传变异和药物的互动链接。网页。org/gene/PA420。
The uridine diphosphate glucuronosyltransferase (UGT) enzymes are a superfamily of enzymes responsible for the glucuronidation of target substrates. The transfer of glucuronic acid renders xenobiotics and other endogenous compounds water soluble, allowing for their biliary or renal elimination [1]. The UGT family is responsible for the glucuronidation of hundreds of compounds, including hormones, flavonoids, and environmental mutagens [1]. Most of the members of the UGT family are expressed in the liver, as well as in other types of tissues, such as intestinal, stomach, or breast tissues. A few members are expressed only extrahepatically, such as UGT1A7, UGT1A8, UGT1A10, and UGT2A1 [2]. Four families exist within the UGT superfamily: UGT1A, UGT2, UGT3, and UGT8 [3]. UGT2 is further divided into two subfamilies, UGT2A and UGT2B, both of which are present on chromosome 4 [2]. UGT2A enzymes are involved in the glucuronidation of compounds such as phenolic odorants and polycyclic aromatic hydrocarbon metabolites, although limited studies have been carried out on this subfamily [4]; UGT2B proteins are mainly responsible for the metabolism of steroids [5]. The roles of UGT3 and UGT8 family members have not been well characterized [3]. The UGT1A family is located on chromosome 2q37, and the members of this group glucuronidate a large variety of compounds. Pharmaceutical drugs are a common substrate of the UGT1A family [1], making the enzymes in this group relevant to pharmacogenetic research. This very important pharmacogene summary on UGT1A1 is available with interactive links to genetic variants and drugs on the PharmGKB website at http://www. pharmgkb. org/gene/PA420.