CAL-39

G1 Acts through GPER1 in Vulvar Carcinoma Cells A431/CAL-39

GPER1 can act as either tumor-promoting or tumor-suppressive depending on cancer type, yet its role in vulvar carcinoma remains undefined. Loris et al. clarified whether GPER1 supports or suppresses vulvar cancer progression. First, they determined subcellular localization of GPER1 in vulvar carcinoma cell lines A431/CAL-39, scored expression in a vulvar-neoplasia tissue microarray (TMA), and finally evaluated proliferation, viability, migration, clonogenicity, and morphology after treatment with GPER1 agonist (G1) or antagonist (G36).

Immunofluorescence confirmed GPER1 localization to both the nucleus and cytoplasm with no statistical difference between A431 and CAL-39 vulvar carcinoma cells (Fig. 1D, E). Treatment cells were treated with G1 (1.25 µM) ± varying doses of GPER1 antagonist G36. G1 treatment alone significantly decreased proliferation of both A431 (37.39 ± 3.88% vs. control; p < 0.001; Fig. 2A) and CAL-39 (39.91 ± 3.39% vs. control; p < 0.01; Fig. 2B), and this suppression was reversed in a dose-dependent manner by G36. In A431 cells, proliferation rates rose to 72.34 ± 6.62% (p = 0.05) and 100.65 ± 12.64% (p = 0.001) treated with 2.5 µM and 5 µM G36, respectively. Similarly, CAL-39 proliferation rates showed a dose-dependent recovery to 67.44 ± 15.04% and 85.18 ± 10.71% (p < 0.05) treated with 2.5 and 5 µM G36, respectively.