Most of the natural products isolated at present are heterocyclic compounds, so heterocyclic compounds occupy an important position in the research of organic chemistry. A compound: 128717-77-1, is researched, SMILESS is O=C(C1=CNC2=C1C=CC=C2OC)O, Molecular C10H9NO3Journal, Article, Research Support, Non-U.S. Gov’t, Journal of Medicinal Chemistry called Development and Profiling of Inverse Agonist Tools for the Neuroprotective Transcription Factor Nurr1, Author is Zaienne, Daniel; Willems, Sabine; Schierle, Simone; Heering, Jan; Merk, Daniel, the main research direction is inverse agonist neuroprotective transcription factor Nurr1.Electric Literature of C10H9NO3.
The ligand-sensing transcription factor nuclear receptor related 1 (Nurr1) evolves as an appealing target to treat neurodegenerative diseases. Despite its therapeutic potential observed in various rodent models, potent modulators for Nurr1 are lacking as pharmacol. tools. Here, we report the structure-activity relationship and systematic optimization of indole-based inverse Nurr1 agonists. Optimized analogs decreased the receptor’s intrinsic transcriptional activity by up to more than 90% and revealed preference for inhibiting Nurr1 monomer activity. In orthogonal cell-free settings, we detected displacement of NCoRs and disruption of the Nurr1 homodimer as mol. modes of action. The inverse Nurr1 agonists reduced the expression of Nurr1-regulated genes in T98G cells, and treatment with an inverse Nurr1 agonist mimicked the effect of Nurr1 silencing on interleukin-6 release from LPS-stimulated human astrocytes. The indole-based inverse Nurr1 agonists valuably extend the toolbox of Nurr1 modulators to further probe the role of Nurr1 in neuroinflammation, cancer, and beyond.
There is still a lot of research devoted to this compound(SMILES：O=C(C1=CNC2=C1C=CC=C2OC)O)Electric Literature of C10H9NO3, and with the development of science, more effects of this compound(128717-77-1) can be discovered.
Reference:
Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts