However, targeting GPX4 is difficult due to its flat active site and similarity to other peroxidases. This technology is the development and use of GPX4 inhibitors to activate ferroptosis for the treatment of cancer. From high-throughput screening hits, structure-based drug design, and structure-activity studies, four generations of structurally distinct analogs have been developed.
This technology preferentially blocks the active site of caspase-2 compared to other caspases and related proteases. This technology describes a group of peptidomimetics that can inhibit the activity of caspase-2, a protease associated with neurodegenerative disorders such as Alzheimer’s disease.
Most existing kinase inhibitors function as competitive inhibitors at the kinase active site. By modulating the prolyl hydroxylation status of CMGC kinases, kinase activity can be inhibited or activated. As such, these allosteric modulators can be developed as inhibitors or activators of kinase activity to treat cancer.