Improving 15-LOX-2 small molecule inhibitors through medicinal chemistry and structure-guided design

该项目旨在通过开发选择性和有效的15-LOX-2抑制剂，特别是在体外和体内模型中能够破坏15-LOX-2/PEBP1蛋白-蛋白质复合体并调节铁下垂的药物，来建立先前的筛选工作。在此期间，协作团队启动了协作，并概述了实现所述项目目标的研究计划。还进行了初步工作，以设计和开始开发潜在的基于细胞的分析方法，并讨论了针对当前15-LOX-2抑制剂先导的药物化学策略。该项目团队已经确定了一种抑制铁下垂的小分子，目前正在研究化学类型的类似物。

This project aims to build on previous screening work by developing selective and potent 15-LOX-2 inhibitors, specifically ones capable of disrupting the 15-LOX-2/PEBP1 protein-protein complex and modulate ferroptosis both in in vitro and in vivo models. During this period, the collaborative team initiated the collaboration and outlined a research plan to accomplish the stated project goals. Initial work was also done to design and begin development of potential cell-based assays, and a medicinal chemistry strategies were discussed for the current 15-LOX-2 inhibitor leads. The project team has identified a small molecule that inhibits ferroptosis, and is currently pursuing analogs of the chemotype.