Heterodimer complex of RXR and NURR1 or NGFI-B
US6458926B1 · kind B1 · utility
Assignee
Inventors
Key dates
| Filing date | Jun 18, 1997 |
| Grant date | Oct 1, 2002 |
| Priority date | — |
| Expiry date | Jun 18, 2017 |
Classification
- Technology area (CPC C)Chemistry; Metallurgy
- CPC primaryC07K2319/00
- WIPO fieldMeasurement
- WIPO sectorInstruments
Abstract
Heterodimerization is a common paradigm among eucaryotic transcription factors, though it remains unclear how individual monomers contribute to the overall transcriptional activities of the complex. The 9-cis retinoic acid receptor (RXR) serves as a common heterodimerization partner for several nuclear receptors including the thyroid hormone (T3R), retinoic acid (RAR) and vitamin D receptors. A strategy has been devised to examine the transcriptional properties of each receptor individually or when tethered to a heterodimeric partner. It has been found that the intrinsic activity of RXR is masked in RXR-T3R and RXR-RAR heterodimers. In contrast, a novel RXR-Nurr1 heterodimer described herein is highly responsive to RXR ligands, suggesting that different partners exert unique allosteric control over the RXR response. These findings establish a novel 9-cis retinoic acid response pathway and resolve the paradox as to how T3R, RAR and VDR contribute to distinct physiologic pathways while sharing a common RXR subunit.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.