Armstrong J I, Bertozzi C R
Department of Chemistry, University of California - Berkeley, Berkeley, CA 94720, USA.
Curr Opin Drug Discov Devel. 2000 Sep;3(5):502-15.
Sulfated biomolecules regulate a diverse array of normal and pathological cellular communication events. The participation of these bioconjugates in a variety of disease states has sparked interest in the enzyme class that installs the sulfate esters: the sulfotransferases. Recent advances in the cloning and characterization of sulfotransferase enzymes and our understanding of the role of sulfated biomolecules in disease states have prompted the search for specific sulfotransferase inhibitors. Evidence for the participation of sulfated carbohydrates and proteins in acute and chronic inflammation, tumor progression and microbial pathogenesis is presented herein, followed by a discussion of sulfotransferase mechanism and approaches to inhibiting sulfotransferase activity.
硫酸化生物分子调节一系列正常和病理细胞通讯事件。这些生物共轭物参与多种疾病状态引发了人们对安装硫酸酯的酶类——硫酸转移酶的兴趣。硫酸转移酶的克隆和特性研究的最新进展以及我们对硫酸化生物分子在疾病状态中作用的理解促使人们寻找特异性硫酸转移酶抑制剂。本文介绍了硫酸化碳水化合物和蛋白质参与急性和慢性炎症、肿瘤进展及微生物致病机制的证据,随后讨论了硫酸转移酶的作用机制以及抑制硫酸转移酶活性的方法。