Table 1.
Selectivity of Pharmacological Ligand Compounds for Estrogen Receptor-α and Estrogen Receptor-β
| Ligand Compound | ER-α/ER-β Selectivity |
Agonist/Antagonist | Relative Binding Selectivity |
Reference |
|---|---|---|---|---|
| Estradiol-17β | ER-α/ER-β | Agonist | N/A | Kuiper et al46 |
| ICI 182,780 | ER-α/ER-β | Antagonist | N/A | Wakeling et al126 |
| *4-OH Tamoxifen | ER-α/ER-β | Antagonist* | N/A | Wakeling et al127 |
| ZK 164015 | ER-α/ER-β | Antagonist | N/A | Walter et al128 |
| PPT | ER-α | Agonist | ~410-fold | Kraichely et al129 |
| Y 134 | ER-α | Agonist | ~125-fold | Yang et al130 |
| *(R,R)-THC | ER-α | Agonist* | ~120-fold | Sun et al131 |
| Raloxifene | ER-α | Agonist | ~15-fold | Sun et al131 |
| MPP | ER-α | Antagonist | ~200-fold | Sun et al77 |
| Genistein | ER-β | Agonist | ~26-fold | Malamas et al43 |
| DPN | ER-β | Agonist | ~70-fold | Meyers et al1 |
| FERb 033 | ER-β | Agonist | ~62-fold | Minutolo et al132 |
| WAY 200070 | ER-β | Agonist | ~68-fold | Compton et al76 |
| PHTPP | ER-β | Antagonist | ~36-fold | Compton et al76 |
| *(R,R)-THC | ER-β | Antagonist* | ~4-fold | Sun et al131 |
| *RU486 | ER-β | Antagonist* | ~5-fold | Fang et al133 |
Denotes ligand compounds with both known partial ER agonist and antagonist activities.
ER, estrogen receptor; N/A, not applicable; unknown or negligible binding selectivity or equal binding affinity for both ER-α and ER-β.
These are the systematic (IUPAC) names: 1. Estradiol-17β: (17β)-estra-1,3,5(10)-triene-3,17-diol; 2. ICI 182,780: 7α,17β-[9-[(4,4,5,5,5-Pentafluoropentyl) sulfinyl]nonyl]estra-1,3,5(10)-triene-3,17-diol; 3. 4-OH Tamoxifen: (Z)-2-[4-(1,2-diphenylbut-1-enyl)phenoxy]-N,N-dimethylethanamine; 4. ZK 164015: 2-(4-Hydroxyphenyl)-3-methyl-1-[10-(pentylsulfonyl)decyl]-1H-indol-5-ol; 5. PPT: 4,4',4''-(4-Propyl-[1H]-pyrazole-1,3,5-triyl)trisphenol; 6. Y 134: [6-Hydroxy-2-(4-hydroxyphenyl)benzo[b]thien-3-yl]-[4-[4-(1-methylethyl)-1-piperazinyl]phenyl]methanone; 7. (R,R)-THC: (R,R)-5,11-Diethyl-5,6,11,12-tetrahydro-2,8-chrysenediol; 8. MPP: 1,3-Bis(4-hydroxyphenyl)-4-methyl-5-[4-(2-piperidinylethoxy)phenol]-1H-pyrazole dihydrochloride; 9. DPN: 2,3-bis(4-Hydroxyphenyl)-propionitrile. Alternative name: Diarylpropionitrile; 10. FERb 033: 2-Chloro-3′-fluoro-3,4'-dihydroxy-[1,1-biphenyl]-4-carboxaldehyde oxime; 11. WAY 200070: 7-Bromo-2-(4-hydroxyphenyl)-1,3-benzoxazol-5-ol; 12. PHTPP: 4-[2-Phenyl-5,7-bis(trifluoromethyl)pyrazolo [1,5-a]pyrimidin-3-yl]phenol; 13. RU486: 11β-[p-(Dimethylamino)phenyl]-17β-hydroxy-17-(1-propynyl)estra-4,9-dien-3-one.