Reasoning
PS3 is met at strong strength. The exact ESR1 p.Asp538Gly (D538G), corresponding to NM_000125.4:c.1613A>G, has been evaluated in multiple independent functional systems with appropriate wild-type comparisons and orthogonal readouts. In HEK293T, SKBR3, MCF7, and other breast-cancer-cell assays, D538G produced ligand-independent estrogen-receptor transcriptional activity, increased ER target-gene signaling, coactivator recruitment, proliferation or tumor growth after estrogen withdrawal, and reduced sensitivity to tamoxifen and fulvestrant. The strongest quantitative support includes SRC3 coactivator binding without estradiol in purified-protein assays (Kd 151 +/- 20 nM for D538G versus no detectable wild-type binding), altered ligand-binding affinities, and ERE-luciferase and xenograft results reproduced across several papers. These are biologically relevant assays for ESR1 activation and endocrine resistance and consistently support an altered, activating functional effect. The evidence is not described as validated and reproducible in a clinical diagnostic laboratory, so the most stringent validation note is not independently satisfied; nevertheless, the generic PS3 definition is satisfied by the convergent well-established in vitro and in vivo functional evidence.
Rule
Well-established in vitro or in vivo functional studies supportive of a damaging effect on the gene or gene product.
Evidence considered
- PMID:24185510: In an estrogen-response-element luciferase assay in HEK293T cells, exact p.Asp538Gly showed strong constitutive activity without estrogen, with 4-hydroxytamoxifen and fulvestrant IC50 values two- to fourfold higher than wild type.
- PMID:24185512: Exact Asp538Gly showed high estrogen-independent ER transcriptional activity, increased ER target-gene expression and Ser118 phosphorylation, increased AIB1 association, and increased tumor growth in an MCF7 xenograft model after estrogen withdrawal; higher tamoxifen and fulvestrant concentrations were required for near-complete inhibition.
- PMID:24217577: Exact A1613G/D538G showed ligand-independent transcriptional activity, SRC-1 interaction, increased ER-regulated gene expression, proliferation and migration, and relative resistance to 4-hydroxytamoxifen and fulvestrant.
- PMID:24398047: Exact c.1613A>G/p.D538G was tested in ERE-luciferase assays and showed constitutive estrogen-receptor transcriptional activity, reduced antiestrogen response, and relative resistance to estrogen deprivation.
- PMID:26836308: In purified ERalpha ligand-binding-domain assays, D538G bound SRC3 without estradiol at Kd 151 +/- 20 nM while wild-type ERalpha showed no detectable binding; D538G also showed altered estradiol and 4-hydroxytamoxifen binding affinities and conformational changes by orthogonal biophysical and structural methods.
Still missing
- The reviewed studies are research assays rather than validated, reproducible clinical diagnostic-laboratory assays.
Sources