INDUCIBLE NITRIC OXIDE SYNTHASE INHIBITOR COMPLEX DATA COLLECTION

我们必须从闪存中收集七个高分辨率数据集 诱导型一氧化氮加氧酶结构域的冰冻晶体 合成酶(INOS)抑制剂在-180℃下的单色络合物 光束线7-1或9-1处的辐射约为1.0E。同步辐射 由于诱导型一氧化氮合酶的弱衍射性，过去和现在仍然需要 晶体，只有使用旋转的阳极才能衍射到3.5E。这些 结构已经帮助我们开发了选择性的专有抑制剂 人类诱导型一氧化氮合酶。我们从海平面上获得的结构信息 分解结构已经并将显著增强我们的能力 为了了解这些抑制物与iNOS的结合并帮助 未来iNOS抑制剂的设计。我们已经能够增加 一个模板的效力提高了100倍，我们现在有了更好的 对我们化合物在iNOS、nNOS之间的选择性的理解 和ecNOS。

We have to collect seven high resolution data sets from flash frozen crystals of the oxygenase domain of inducible nitric oxide synthase (iNOS) inhibitor complexes at -180 C using monochromatic radiation around 1.0 E at beam line 7-1 or 9-1. Synchrotron radiation has been and still is needed due to the weak diffraction of the iNOS crystals, which only diffract to 3.5 E using a rotating anode. These structures have helped us develop selective proprietary inhibitors of human iNOS. The structural information we have gained from the high resolution structures has and will significantly enhance our ability to understand binding of these inhibitors to the iNOS and aid in the design of future iNOS inhibitors. We have been able to increase the potency of one template by 100 fold, and we now have a better understanding of the selectivity of our compounds between iNOS, nNOS and ecNOS.