Co-repressor release but not ligand binding is a prerequisite for transcription activation by human retinoid acid receptor alpha ligand-binding domain.

Abstract excerpt

Nuclear hormone receptors coordinately regulate the activity of genetic networks through the recruitment of transcriptional co-regulators, including co-repressors and co-activators. Allosteric modulation of the ligand-binding domain by hormonal activators shifts the co-factor binding preference by defined structural changes in overlapping docking sites. We report here that mutations at conserved residues within...

Topics

• Amino Acid Sequence
• Animals
• Cell Line
• Crystallography, X-Ray
• Dimerization
• Dose-Response Relationship, Drug
• Escherichia coli
• Humans
• Ligands
• Models, Molecular
• Molecular Sequence Data