Table 2.
Dex-mesylate (Dex-Mes) and selective glucocorticoid receptor agonist (SEGRA) compounds 1217 and 1218 but not GSK866 or Dex covalently bind glucocorticoid receptor ligand-binding domain (GR-LBD)-specific cysteines.
| Sample | Modifications |
|---|---|
| Ctrl | – |
| Dex | – |
| Dex-Mes | Peptide 615–633 → C622 |
| GSK866 | – |
| 1217 | Peptide 615–633 → C622 |
| 1218 | Peptide 615–633 → C622 |
MassspecMass spectrometry-based identification of GR-LBD cysteine-containing peptides which bind covalently to SEGRAs GSK866, 1217, or 1218. The position of the LBD peptide in hGR is indicated by the residue numbers of the first and last amino acid of the peptide (according to the SwissProt database). The modified residue is described by the official amino acid acronym and its position in hGR.