STRUCTURAL ANALYSES OF HUMAN ESTROGEN RECEPTOR IN COMPLEX WITH EFFECTOR/REGUL

这个子项目是许多研究子项目中的一个 由NIH/NCRR资助的中心赠款提供的资源。子项目和 研究者（PI）可能从另一个NIH来源获得了主要资金， 因此可以在其他CRISP条目中表示。所列机构为 研究中心，而研究中心不一定是研究者所在的机构。 该提案是我们正在进行的结构研究的一部分，旨在表征多结构域人雌激素受体（hER），其与调节/效应蛋白和潜在的治疗性小分子的相互作用。过去，我们在APS收集了关于hER配体结合结构域（LBD）与其单体（PDB代码：2 OCF）复合的首次蛋白质-蛋白质相互作用的数据，以及LBD与各种配体（在最后一次运行中与Estetrol复合，PDB代码：3L 03）的复合物的数据。我们已经获得了LBD的新配体复合物的晶体，以及hER的其他结构域的晶体。此外，我们还获得了Menin的衍射良好的晶体，Menin是一种多发性内分泌肿瘤蛋白，已被证明与hER形成复合物。我们要求光束时间来筛选这些晶体，评估它们的衍射质量，并收集那些衍射良好的晶体的数据。

This subproject is one of many research subprojects utilizing the resources provided by a Center grant funded by NIH/NCRR. The subproject and investigator (PI) may have received primary funding from another NIH source, and thus could be represented in other CRISP entries. The institution listed is for the Center, which is not necessarily the institution for the investigator. This proposal is part of our ongoing structural studies aimed at the characterization of the multi-domain human Estrogen Receptor (hER), its interaction with regulator/effector proteins and potential therapeutic small molecules. In the past we have collected data at the APS on the first protein-protein interaction of the hER ligand binding domain (LBD), complexed with its monobody (pdb code: 2OCF) and also on complexes of LBD with various ligands (with Estetrol in the last run, pdb code: 3L03). We have obtained crystals of new ligand complexes with the LBD, as well as crystals of the other domains of hER. In addition, we have well-diffracting crystals of Menin, multiple endocrine neoplasia protein, that has been shown to form a complex with the hER. We request beam time to screen these crystals, evaluate them for diffraction quality and collect data on those that diffract well.