Article
Surveying helix 12 dynamics within constitutively active estrogen receptors using bipartite tetracysteine display.
The Journal of biological chemistry - 1 Mar 2025
Sendanayake Lasantha R, Pokhrel Ranju, Holub Justin M
Abstract excerpt
Somatic Y537S and D538G mutations within the estrogen receptor alpha ligand-binding domain (ERα-LBD) have been linked to enhanced cell proliferation, survival, and metastases in ER-positive breast cancers. Such mutations are thought to confer ligand-independent receptor activation by increasing the flexibility of helix 12 (H12), a segment within the ERα-LBD that acts as a dynamic regulator of ERα activity. We...
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