Duan Xinyuan, Trent John O, Ye Hong
James Graham Brown Cancer Center, University of Louisville, 529 South Jackson Street, Louisville, Kentucky, 40202, USA.
Anticancer Agents Med Chem. 2009 Jan;9(1):51-4. doi: 10.2174/187152009787047716.
Sumoylation has been implicated in a variety of cancers, suggesting that sumoylation manipulation could be one approach for regulating tumorgenesis. Ubc9 exerts a central function for the sumoylation pathway, interacting with almost all the partners required for sumoylation. The high-resolution structure available for Ubc9 as well as the recent determination of more interacting partner complex structures makes rational drug design that target Ubc9 possible. Structure-based virtual drug screening has been used increasingly as the first step of drug design to select potential lead templates. This review analyzes all the interfaces between Ubc9 and its binding partners while also highlighting the possible targeting sites on Ubc9 best suited for virtual screening and drug design.
SUMO化与多种癌症有关，这表明操纵SUMO化可能是调节肿瘤发生的一种方法。Ubc9在SUMO化途径中发挥核心作用，与SUMO化所需的几乎所有伙伴相互作用。Ubc9的高分辨率结构以及最近对更多相互作用伙伴复合物结构的确定使得针对Ubc9的合理药物设计成为可能。基于结构的虚拟药物筛选越来越多地被用作药物设计的第一步，以选择潜在的先导模板。本综述分析了Ubc9与其结合伙伴之间的所有界面，同时还强调了Ubc9上最适合虚拟筛选和药物设计的可能靶向位点。
