ERpS294 is a biomarker of ligand or mutational ERα activation and a breast cancer target for CDK2 inhibition.
Oncotarget
Scott, Gary K GK; Chu, David D; Kaur, Ravneet R; Malato, Julia J; Rothschild, Daniel E DE; Frazier, Katya K; Eppenberger-Castori, Serenella S; Hann, Byron B; Park, Ben Ho BH; Benz, Christopher C CC
Posttranslationally modified progesterone receptors direct ligand-specific expression of breast cancer stem cell-associated gene programs.
Journal Of Hematology & Oncology
Knutson, Todd P TP; Truong, Thu H TH; Ma, Shihong S; Brady, Nicholas J NJ; Sullivan, Megan E ME; Raj, Ganesh G; Schwertfeger, Kathryn L KL; Lange, Carol A CA
p21-activated kinase group II small compound inhibitor GNE-2861 perturbs estrogen receptor alpha signaling and restores tamoxifen-sensitivity in breast cancer cells.
Ligand binding promotes CDK-dependent phosphorylation of ER-alpha on hinge serine 294 but inhibits ligand-independent phosphorylation of serine 305.
Molecular Cancer Research : Mcr
Held, Jason M JM; Britton, David J DJ; Scott, Gary K GK; Lee, Elbert L EL; Schilling, Birgit B; Baldwin, Michael A MA; Gibson, Bradford W BW; Benz, Christopher C CC