Sidhu, Preetpal S. published the artcileDevelopment of Novel Vitamin D Receptor-Coactivator Inhibitors, Safety of 2-Methoxynicotinaldehyde, the main research area is novel vitamin D receptor coactivator inhibitor; 3-indolylmethanamines; CAMP; CYP24A1; HL60; VDR; Vitamin D receptor; apoptosis; fluorescence polarization; high throughput screening; steroid receptor coactivator.
Nuclear receptor coregulators are master regulators of transcription and selectively interact with the vitamin D receptor (VDR) to modulate cell differentiation, cell proliferation, and calcium homeostasis. Herein, we report the syntheses and evaluation of highly potent and selective VDR-coactivator inhibitors based on a recently identified 3-indolylmethanamine scaffold. The most active compound, PS121912, selectively inhibited VDR-mediated transcription among eight other nuclear receptors tested. PS121912 is also selectively disrupting the binding between VDR and the third nuclear receptor interaction domain of the coactivator SRC2. Genetic studies revealed that PS121912 behaves like a VDR antagonist by repressing 1,25-(OH)2D3 activated gene transcription. In addition, PS121912 induced apoptosis in HL-60.
ACS Medicinal Chemistry Letters published new progress about Homo sapiens. 71255-09-9 belongs to class pyridine-derivatives, name is 2-Methoxynicotinaldehyde, and the molecular formula is C7H7NO2, Safety of 2-Methoxynicotinaldehyde.