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人尿苷二磷酸葡萄糖醛酸基转移酶的药物基因组学及其临床意义。

Pharmacogenomics of human uridine diphospho-glucuronosyltransferases and clinical implications.

机构信息

1] Pharmacogenomics Laboratory, Centre Hospitalier Universitaire (CHU) de Québec Research Center, Québec, Canada; Faculty of Pharmacy, Laval University, Québec, Canada [2] Pharmacogenomics Laboratory, CHU de Québec Research Center, Québec, Canada.

1] Pharmacogenomics Laboratory, Centre Hospitalier Universitaire (CHU) de Québec Research Center, Québec, Canada; Faculty of Pharmacy, Laval University, Québec, Canada [2] Faculty of Medicine, Laval University, Québec, Canada.

出版信息

Clin Pharmacol Ther. 2014 Sep;96(3):324-39. doi: 10.1038/clpt.2014.126. Epub 2014 Jun 12.

Abstract

Glucuronidation by uridine diphospho-glucuronosyltransferase enzymes (UGTs) is a major phase II biotransformation pathway and, complementary to phase I metabolism and membrane transport, one of the most important cellular defense mechanisms responsible for the inactivation of therapeutic drugs, other xenobiotics, and endogenous molecules. Interindividual variability in UGT pathways is significant and may have profound pharmacological and toxicological implications. Several genetic and genomic processes underlie this variability and are discussed in relation to drug metabolism and diseases such as cancer.

摘要

尿苷二磷酸葡萄糖醛酸基转移酶(UGTs)的葡醛酸化是主要的 II 相生物转化途径,与 I 相代谢和膜转运相辅相成,是负责使治疗药物、其他外源性物质和内源性分子失活的最重要的细胞防御机制之一。UGT 途径的个体间差异具有重要意义,可能具有深远的药理学和毒理学意义。几种遗传和基因组过程是这种差异的基础,并与药物代谢和癌症等疾病有关进行了讨论。

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