NR1

Non-steroid nuclear receptors include thyroid hormone receptor, retinoic acid receptor, vitamin D receptor, Liver X receptor like receptors (LXR and FXR) and PPARγ. Members of this family heterodimerize with the retinoid X receptor (RXR). Prior to ligand binding, receptor heterodimers are located in the nucleus as part of complexes with histone deacetylases (HDACs) and other corepressors that keep target DNA in a tightly wound conformation, preventing exposure to transactivation factors. Ligand binding results in HDAC dissociation, chromatin derepression, and transcriptional activation.In addition to ligand binding, nuclear receptor activity can be modulated through the action of numerous growth factor and cytokine signaling cascades that result in receptor phosphorylation or other post-translational modifications, typically within the N-terminal transactivation domain. [1].     


[1] P. Germain et al. Overview of nomenclature of nuclear receptors. Pharmacol. Rev. 2006, 58, 685-704.

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Axon ID Name Description From price
2679 AR7 RARα antagonist that stimulates chaperone-mediated autophagy €90.00
1194 BMS 189961 RAR-γ agonist €145.00
1173 BMS 270394 RAR-γ agonist €165.00
1676 BXL 628 Vitamin D receptor (VDR) agonist €165.00
1950 CDDO A potent multifunctional anti-tumor agent. PPAR-γ agonist €120.00
1241 CH 55 RAR agonist €90.00
2114 CP 775146 Potent and selective PPARα agonist €85.00
1746 Doxercalciferol Vitamin D2 analog, VDR agonist €115.00
2561 DY 268 Highly potent FXR antagonist with a promising in vitro profile €120.00
2727 Elafibranor Dual PPARα/δ agonist €90.00
2686 FH535 Dual inhibitor of PPAR and Wnt/β-catenin signaling €75.00
2706 FH535 sodium salt Dual inhibitor of PPAR and Wnt/β-catenin signaling €80.00
2363 GSK 2033 The first potent cell-active LXR antagonist €105.00
1628 GSK 3787 PPARδ antagonist €90.00
1266 GW 3965 hydrochloride Liver X receptor agonist €95.00

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