SMALL MOLECULES REGULATING PROTEIN-PROTEIN INTERACTIONS IN CANCER

这个子项目是许多研究子项目中利用 资源由NIH/NCRR资助的中心拨款提供。子项目和 调查员(PI)可能从NIH的另一个来源获得了主要资金， 并因此可以在其他清晰的条目中表示。列出的机构是 该中心不一定是调查人员的机构。 (A)目标。化学调控和抑制癌基因的调控和表达是治疗多种癌症的一种很有前途的治疗方法。为了推进这一途径，我们的目标是鉴定、优化和表征影响Myc网络和PI3K途径的蛋白质-蛋白质相互作用的小分子抑制剂和稳定剂。对于小分子来说，蛋白质-蛋白质相互作用仍然是具有挑战性的目标；这一领域的进展将为药物开发打开新的机会。这种合作将依赖于AutoDock程序套件中的几个进展，这些程序能够发现可用药部位来调节蛋白质-蛋白质相互作用，并将这些部位的动态特征考虑在内。

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. (A) Objectives. Chemical modulation and inhibition of oncogene regulation and expression is a promising therapeutic approach to the treatment of many cancers. To advance this approach, our goal is the identification, optimization and characterization of small molecule inhibitors and stabilizers of protein-protein interactions affecting the Myc network and the PI 3-kinase (PI3K) pathway. Protein-protein interactions remain challenging targets for small molecules; progress in this area will open new opportunities for drug development. This collaboration will rely upon several advances in the AutoDock suite of programs that enable the discovery of drugable sites to modulate protein-protein interactions, and which factor in dynamic characteristics of these sites.