ACS Med Chem Lett. 2014 Feb 13;5(2):199-204.
Sidhu PS1, Nassif N1, McCallum MM1, Teske K1, Feleke B1, Yuan NY1, Nandhikonda P1, Cook JM1, Singh RK2, Bikle DD3, Arnold LA1 (email@example.com )
1 Department of Chemistry and Biochemistry, University of Wisconsin-Milwaukee, WI 53211, USA.
2 Molecular Therapeutics Laboratory, Program in Women's Oncology, Department of Obstetrics and Gynecology, Woman and Infant's Hospital of Rhode Island, Alpert Medical School of, Brown University, Provence, Rhode Island, USA.
3 Endocrine Research Unit, Department of Medicine, Veterans Affairs Medical Center, San Francisco, CA 94121, USA.
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.
3-indolylmethanamines, CAMP, CYP24A1, HL60, VDR, Vitamin D receptor, apoptosis, fluorescence polarization, high throughput screening, steroid receptor coactivator
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