Progesterone receptor activation regulates seizure susceptibility

Activation (transformation) of the chick oviduct progesterone receptor was found to be induced at 0 degrees C by heparin free in solution as well as by chromatography on a column of heparin linked to acrylamide/agarose. The transformed molecule displayed properties of the activated form of [3H]progesterone-receptor complex obtained by heat treatment or by high ionic strength: smaller size (s20,w = 3.9 S, Stokes radius = 5.2 nm), lower rate of dissociation (t 1/2 approx. 50 h at 0 degrees C compared with approx. 20 h for the ‘native’ form) and increased binding to phosphocellulose. In all cases, molybdate was an effective inhibitor of transformation and stabilized a large ‘native’ form (s20,w = 7.9 S, Stokes radius = 7.6 nm). Transformation by neither KCl nor heparin depended on the presence of ligand bound to the receptor, and the properties of the receptor molecule produced by treatment of ligand-free receptor with high ionic strength or with heparin were identical with those of the activated progesterone-receptor complex, demonstrating that receptor activation can be obtained experimentally in the absence of hormone. Our data are compatible with a model in which activation implies separation of the 4 S units, which compose the approx. 8 S ‘native’ form.

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Progesterone Receptor Activation of Extranuclear Signaling Pathways in Regulating p53 Expression in Vascular Endothelial Cells

Molecular Endocrinology ◽

10.1210/me.2010-0424 ◽

2011 ◽

Vol 25 (3) ◽

pp. 421-432 ◽

Cited By ~ 20

Author(s):

Sung-Po Hsu ◽

Wen-Sen Lee

Keyword(s):

Endothelial Cells ◽

Progesterone Receptor ◽

Signaling Pathways ◽

Vascular Endothelial Cells ◽

Receptor Activation ◽

Vascular Endothelial ◽

P53 Expression ◽

Extranuclear Signaling

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Cyclic GMP May Potentiate Lordosis Behaviour By Progesterone Receptor Activation

Journal of Neuroendocrinology ◽

10.1046/j.1365-2826.1999.00298.x ◽

1999 ◽

Vol 11 (2) ◽

pp. 107 ◽

Cited By ~ 42

Author(s):

H.-P. Chu

Keyword(s):

Progesterone Receptor ◽

Cyclic Gmp ◽

Receptor Activation ◽

Lordosis Behaviour

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LPA1 Receptor Promotes Progesterone Receptor Phosphorylation through PKCα in Human Glioblastoma Cells

Cells ◽

10.3390/cells10040807 ◽

2021 ◽

Vol 10 (4) ◽

pp. 807

Author(s):

Silvia Anahi Valdés-Rives ◽

Denisse Arcos-Montoya ◽

Marisol de la Fuente-Granada ◽

Carmen J. Zamora-Sánchez ◽

Luis Enrique Arias-Romero ◽

...

Keyword(s):

Progesterone Receptor ◽

Transcriptional Activity ◽

Receptor Activation ◽

Protein Protein Interaction ◽

Downstream Target ◽

Cellular Processes ◽

High Grade Astrocytoma ◽

Wide Range ◽

Lpa1 Receptor ◽

Human Gbm

Lysophosphatidic acid (LPA) induces a wide range of cellular processes and its signaling is increased in several cancers including glioblastoma (GBM), a high-grade astrocytoma, which is the most common malignant brain tumor. LPA1 receptor is expressed in GBM cells and its signaling pathways activate protein kinases C (PKCs). A downstream target of PKC, involved in GBM progression, is the intracellular progesterone receptor (PR), which can be phosphorylated by this enzyme, increasing its transcriptional activity. Interestingly, in GBM cells, PKCα isotype translocates to the nucleus after LPA stimulation, resulting in an increase in PR phosphorylation. In this study, we determined that LPA1 receptor activation induces protein-protein interaction between PKCα and PR in human GBM cells; this interaction increased PR phosphorylation in serine400. Moreover, LPA treatment augmented VEGF transcription, a known PR target. This effect was blocked by the PR selective modulator RU486; also, the activation of LPA1/PR signaling promoted migration of GBM cells. Interestingly, using TCGA data base, we found that mRNA expression of LPAR1 increases according to tumor malignancy and correlates with a lower survival in grade III astrocytomas. These results suggest that LPA1/PR pathway regulates GBM progression.

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