Ligand Binding Analysis for Human α5β1 Integrin: Strategies for Designing New α5β1 Integrin Antagonists
Ligand Binding Analysis for Human α5β1 Integrin: Strategies for Designing New α5β1 Integrin Antagonists
复制标题
人 α5β1 整合素的配体结合分析：设计新 α5β1 整合素拮抗剂的策略
DOI：
10.1021/jm040224i
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发表时间：
2005
影响因子：
7.3
通讯作者：
H. Kessler
中科院分区：
文献类型：
--
作者：
L. Marinelli;A. Meyer;Dominik Heckmann;A. Lavecchia;E. Novellino;H. Kessler
我们报道了迄今为止已知的与最有效和选择性配体（SJ749）结合的α5β1整合素头群的三维模型。模型采用比较蛋白质建模方法建立，与实验数据吻合较好。从这项研究中，我们确定了α5β1受体中两个可能重要的区域，它们是这种整合素所特有的，可能值得考虑用于药物靶向。
We report a three-dimensional model of the α5β1 integrin headgroup bound to the most potent and selective ligand (SJ749) known to date. The model was built using the comparative protein modeling method, and it is consistent with experimental data. From this study, we identified two potentially important regions in the α5β1 receptor that are peculiar to this integrin and might be worth considering for drug targeting.