Supplementary Figures 1-13 and Supplementary Materials and Methods from The Dysregulated Pharmacology of Clinically Relevant ESR1 Mutants is Normalized by Ligand-activated WT Receptor
Year: 2023
Type: supplementary-materials
Abstract: Supplemental Figure 1: Structures of clinically relevant compounds used in this study. Supplemental Figure 2: Cells expressing both the ERWT and ERmuts have similar pharmacological responses to antiestrogens when compared to cells only expressing ERWT. Supplemental Figure 3: Albeit differences in clonal variability, there is indistinguishable differences in T47D proliferation in response to antiestrogens. Supplemental Figure 4: Downregulation of ER in MCF7B cells is unaffected by the presence of the mutant receptor. Supplemental Figure 5: Validation of ER mutation status in engineered cell lines. Supplemental Figure 6: Protein levels of transfected constructs in SKBR3 cells are consistent with MCF7 expression level. Supplemental Figure 7: ER expression in MCF7I cells is titratable with doxycycline treatment. Supplemental Figure 8: Overexpression of ERY537S or ERD538G, not ERWT, in MCF7I cells changes ligand potency. Supplemental Figure 9: Western blot validation of relative ER expression levels in SKBR3. Supplemental Figure 10: Agonist activation of relative expression levels of ERWT and ERmuts in SKBR3 cells. Supplemental Figure 11: In-Cell Western validation of ER expression levels for siRNA knockdown and cDNA overexpression in MCF7i. Supplemental Figure 12: Agonist activation of relative expression levels of ERWT and ERmuts in MCF7i cells. Supplemental Figure 13: The altered potency of fulvestrant against the ERmuts on endogenous ER target genes is only evident when expressed at a level higher than the WT receptor.
Language: English
Subfield: Genetics
Domain: Life Sciences
Open Access status: gold
OpenAlex ID: W4362490246