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Article
Open AccessDiscovery of small molecule agonists of the Relaxin Family Peptide Receptor 2
The relaxin/insulin-like family peptide receptor 2 (RXFP2) belongs to the family of class A G-protein coupled receptors (GPCRs) and it is the only known target for the insulin-like factor 3 peptide (INSL3). Th...
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Article
Open AccessINPP4B protects from metabolic syndrome and associated disorders
A high fat diet and obesity have been linked to the development of metabolic dysfunction and the promotion of multiple cancers. The causative cellular signals are multifactorial and not yet completely understo...
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Article
Open AccessAndrogen Receptor and Poly(ADP-ribose) Glycohydrolase Inhibition Increases Efficiency of Androgen Ablation in Prostate Cancer Cells
There is mounting evidence of androgen receptor signaling inducing genome instability and changing DNA repair capacity in prostate cancer cells. Expression of genes associated with base excision repair (BER) i...
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Article
Inositol polyphosphate 4-phosphatase type II regulation of androgen receptor activity
Activation and transcriptional reprogramming of AR in advanced prostate cancer frequently coincides with the loss of two tumor suppressors, INPP4B and PTEN, which are highly expressed in human and mouse prosta...
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Protocol
Techniques for Evaluation of AR Transcriptional Output and Recruitment to DNA
Steroid receptors are ligand activated transcription factors whose promoter specificity is regulated by a broad set of coregulators and pioneer factors. Corepressors and coactivators determine receptors’ recru...
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Article
Open AccessINPP4B suppresses prostate cancer cell invasion
INPP4B and PTEN dual specificity phosphatases are frequently lost during progression of prostate cancer to metastatic disease. We and others have previously shown that loss of INPP4B expression correlates with...
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Article
Identification and optimization of small-molecule agonists of the human relaxin hormone receptor RXFP1
The anti-fibrotic, vasodilatory and pro-angiogenic therapeutic properties of recombinant relaxin peptide hormone have been investigated in several diseases, and recent clinical trial data has shown benefit in ...
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Chapter
Roles of Androgen Receptor Coregulators and Cell Signaling in the Regulation of Androgen-Responsive Genes
Androgen receptor (AR) is a member of the ligand activated transcription factor family. Its function is regulated by a complex network of coregulatory proteins and cell signaling pathways. AR is a key transcri...
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Article
Open AccessAndrogen receptor footprint on the way to prostate cancer progression
The prostate gland is exquisitely sensitive to androgen receptor (AR) signaling. AR signaling is obligatory for prostate development and changes in AR levels, its ligands or shifts in AR mode of action are ref...
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Chapter
Coregulators and the Regulation of Androgen Receptor Action in Prostate Cancer
The importance of androgen receptors in primary prostate cancer is well established and some form of androgen blockade is the primary treatment for metastatic prostate cancer. There is increasing evidence that...
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Chapter
Androgen Receptor Coactivators and Prostate Cancer
Among USA men, prostate cancer (PC) is the second most common cause of death from cancer. Thus, the etiology, prevention, and treatment of the disease are a major health concern. Development and differentiatio...
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Article
A transgenic insertion upstream of Sox9 is associated with dominant XX sex reversal in the mouse
In most mammals, male development is triggered by the transient expression of the Y-chromosome gene, Sry, which initiates a cascade of gene interactions ultimately leading to the formation of a testis from the in...
