Overview of HNF-4 repressors and antagonistic ligands and their functions
| Substance | HNF-4 Domain | Mode of Action | References | |
|---|---|---|---|---|
| Antagonistic ligands | ω-3 and ω-6 polyunsaturated fatty acyl-CoAs | Unknown | Hertz et al., 1998 | |
| (C18:3, ω-3)-CoA | Lowers affinity of the HNF-4α dimer to its cognate enhancer | |||
| Saturated (C18:0)-CoA | Lowers affinity of the HNF-4α dimer to its cognate enhancer | |||
| Leads to decreased HNF-4α dimerization | ||||
| Repressors | SHP | AF-2 | Competition with coactivators for the AF-2 binding domain | Lee et al., 2000 |
| AF-2 | Direct inhibition after binding to the AF-2 domain through a SHP repressor domain (unknown mechanism) | |||
| COUP-TFs | No | Competition with HNF-4α for binding to cis-acting DNA sites of many regulatory regions | Kimura et al., 1993; Ktistaki and Talianidis, 1997 | |
| HNF-1α | AF-2 | Binding to the AF-2 domain, probably competing with coactivators |