Propranolol Activates the Orphan Nuclear Receptor TLX to Counteract Proliferation and Migration of Glioblastoma Cells was written by Faudone, Giuseppe;Bischoff-Kont, Iris;Rachor, Lea;Willems, Sabine;Zhubi, Rezart;Kaiser, Astrid;Chaikuad, Apirat;Knapp, Stefan;Fuerst, Robert;Heering, Jan;Merk, Daniel. And the article was included in Journal of Medicinal Chemistry in 2021.Category: pyrimidines This article mentions the following:
The ligand-sensing transcription factor tailless homolog (TLX, NR2E1) is an essential regulator of neuronal stem cell homeostasis with appealing therapeutic potential in neurodegenerative diseases and central nervous system tumors. However, knowledge on TLX ligands is scarce, providing an obstacle to target validation and medicinal chem. To discover TLX ligands, we have profiled a drug fragment collection for TLX modulation and identified several structurally diverse agonists and inverse agonists of the nuclear receptor. Propranolol evolved as the strongest TLX agonist and promoted TLX-regulated gene expression in human glioblastoma cells. Structure-activity relationship elucidation of propranolol as a TLX ligand yielded a structurally related neg. control compound In functional cellular experiments, we observed an ability of propranolol to counteract glioblastoma cell proliferation and migration, while the neg. control had no effect. Our results provide a collection of TLX modulators as initial chem. tools and set of lead compounds and support therapeutic potential of TLX modulation in glioblastoma. In the experiment, the researchers used many compounds, for example, 4-Amino-N-(6-methoxypyrimidin-4-yl)benzenesulfonamide (cas: 1220-83-3Category: pyrimidines).
4-Amino-N-(6-methoxypyrimidin-4-yl)benzenesulfonamide (cas: 1220-83-3) belongs to pyrimidine derivatives. The aromatic compound pyrimidine, and its derivatives, are ubiquitous in nature. They are found in nucleic acids, vitamins, amino acids, antibiotics, alkaloids, and a variety of toxins. Therapy for fungal infections is based mainly on four classes of antifungals: azoles, echinocandins, polyenes, and pyrimidine analogs.Category: pyrimidines
Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia