Table 3. Human orphan receptors.
| Orphan-Receptors | ||||||||
|---|---|---|---|---|---|---|---|---|
|
NR0B1 (DAX-1) Dosage-sensitive-sex reversal- Adrenal-hypoplasia-critical-region-on-chromosome-X-gene-1 |
X | 2 | NP_000466 | 470 | - | 231-464 | Unknown | Onco-suppressive action |
|
NR0B2 (SHP) Small-Heterodimeric-Partner |
1 | 2 | NP_068804 | 257 | - | 32-254 | CD437 (PUBCHEM:135411)(synth.agonist) Farhana L et al, Cancer Res (2007) 67:318-25 | Onco-suppressive action |
|
NR1D1 (REV-ERBα) Related-to-vERBα |
17 | 8 | NP_068370 | 614 | 127-215 | 418-611 | Heme (PUBCHEM:444097)(end.agonist) Raghuram S et al, Nat Struct Mol Biol (2007) 14:1207-13 GSK4112 (PUBCHEM:50905018) (synth.agonist) Meng QJ et al, J Cell Science (2008) 121:3629-35 SR9009 (PUBCHEM:57394020) (synth.agonist) Solt LA et al, Nature (2012) 485:62-8 |
Onco-suppressive action |
|
NR1D2 (REV-ERBβ) Related-to-vERBβ |
3 | 8 | NP_005117 | 579 | 98-186 | 389-577 |
Heme (PUBCHEM:444097)(end.agonist) Raghuram S et al, Nat Struct Mol Biol (2007) 14:1207-13 SR9009 (PUBCHEM:57394020)(synth.agonist) Solt LA et al, Nature (2012) 485:62-8 SR8278 (PUBCHEM:53393127)(synth.antagonist) Kojetin D et al, ACS Chem Biol (2011) 6:131-4 |
Unknown |
|
NR2C1 (TR2) Testicular-Receptor-2 |
12 | 14 12 12 |
NP_003288 NP_001120834 NP_001027458 |
603 483 467 |
108-194 108-194 108-194 |
368-589 368-465 368-464 |
Unknown | Unknown |
|
NR2C2 (TR4) Testicular-Receptor-4 |
3 | 14 15 |
NP_001278623 NP_003289 |
596 615 |
112-198 131-217 |
361-582 380-601 |
Unknown | Unknown |
|
NR2E1 (TLX) Drosophila-Tailless-Homolog |
6 | 9 9 |
NP_003260 NP_001273031 |
385 422 |
8-99 45136 |
187-354 191-406 |
Ccrp-1, -2 and -3 (synth. agonists) Benod C et al, PLoS One (2014)9:e99440 | Oncogenic Action |
|
NR2E3 (PNR) Photo-specific-Nuclear-Receptor |
15 | 7 8 |
NP_057430 NP_055064 |
367 410 |
39-130 39-130 |
192-367 192-397 |
Unknown | Oncogenic Action |
|
NR2F1 (COUPTF1α) COUP-Transcription-Factor-1α |
5 | 3 | NP_005645 | 423 | 86-158 | 184-419 | Unknown | Onco-suppressive action |
|
NR2F2 (COUPTF1β) COUP-Transcription-Factor-1β |
15 | 3 3 3 |
NP_066285 NP_001138628 NP_001138627 |
414 261 281 |
79-151 - - |
183-414 24-258 44-278 |
Unknown Pyridaben (PUBCHEM:91754)(synth. antagonist) bindingDB database (http://www.bindingdb.org) |
Onco-suppressive action |
|
NR2F6 (COUPTF-1γ) COUP-Transcription-Factor-1γ |
19 | 4 | NP_005225 | 404 | 56-128 | 165-400 | Unknown | Oncogenic action |
|
NR4A1 (NURR77) Nuclear-Receptor-Related-77 |
12 | 8 8 8 |
NP_001189163 NP_001189162 NP_002126 |
652 611 598 |
319-393 278-352 264-339 |
415-652 374-611 409-459 |
Unknown | Onco-suppressive action |
|
NR4A2 (NURR1) Nuclear-Receptor-Related-1 |
2 | 8 | NP_006177 | 598 | 260-335 | 409-459 | Unknown | Unknown |
|
NR4A3 (NOR1) Nuclear-Orphan-Receptor-1 |
9 | 7 8 5 |
NP_775292 NP_008912 NP_775291 |
637 626 443 |
301-375 290-364 290-364 |
407-637 396-626 - |
PGA2 (PUBCHEM:5280880)(end. agonist) Kagaya S et al, Biol Pharm Bull (2005) 28:1603-7 6-mercaptopurine (PUBCHEM:667490)(synth. agonist) Wansa KD et al, J Biol Chem (2003) 278:24776-90 |
Onco-suppressive action |
|
NR6A1 (GCNF) Germ-Cell-Nuclear-Factor |
9 | 10 10 |
NP_201591 NP_001480 |
480 475 |
52-141 48-137 |
256-467 251-462 |
Unknown | Oncogenic Action |
The table contains basic information on the characteristics of the Orphan-Receptors group of nuclear receptors (NRs). The first column lists the human NRs considered in the review article. The official symbol of each NR is indicated in italics, while the original alias of each protein product is indicated in parenthesis. The full name of each NR is indicated underneath in italics. The second column from the left lists the human chromosome (Chr) each NR maps to. The number of exons encoding the transcripts giving rise to the corresponding NR protein-variant is indicated in the third column. The fourth column lists the accession number of each NR protein-variant. The amino acid (aa) length of each NR protein variant, the position of the DNA-binding domain (DBD) and the ligand-binding domain (LBD) are indicated in columns five, six and seven, respectively. Column eight contains a list of representative endogenous (end.) and synthetic (synth.) agonists, antagonists and reverse agonists for each NR along with an appropriate reference. The chemical structures of the listed molecules can be found in the PUBCHEM database with the use of the PUBCHEM-CID accession numbers provided. The PBCHEM chemical structure is not available in the case of the NR2E1 agonists Ccrp-1, -2 and -3. When possible, the predicted onco-suppressive (bold) or oncogenic (black-boxed) action of the corresponding NR is indicated in the last column on the right. Synthetic agonists and antagonists of potential therapeutic interested targeting onco-suppressive and oncogenic NRs, respectively, are marked in bold and boxed in black. Finally, in the few cases where supportive data are available, the type of breast-cancer which is predicted to represent a preferential target of the NR is listed in the last column.