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Prostate cancer that recurs after androgen deprivation therapy is the second leading cause of cancer-related death in North American men. Clinical and experimental evidences indicate that the development of recurrent prostate cancer is dependent on re-activation of the androgen ...

Evaluating endocrine activities of environmental chemicals or screening for new small molecule modulators of the androgen receptor (AR) transcription activity requires standardized and reliable assay procedures. Scintillation proximity assays (SPA) are sensitive and ...

Androgen receptor (AR) acts as a ligand-regulated transcription factor that conveys the message of both natural and synthetic androgens directly to the level of gene programs. Reporter gene assays provide a convenient and quantitative way to measure the transcriptional activity of AR ...

The androgen receptor (AR) is the central component of a dynamic conformational and interaction cascade initiated by androgenic hormones. AR function can be modified by cellular inputs not examined in test tube studies of AR action. Thus, there is a need to measure AR conformation and biochemi ...

The androgen receptor (AR) has a DNA-binding domain that consists of two zinc coordinating modules. While residues of the first module make most of the sequence-specific contacts, the second module functions as a homodimerization interface (1). This explains why the androgen response el ...

The androgen receptor (AR) plays a pivotal role in the progression of prostate cancer from the androgen-dependent to the castration-resistant state, making it a potential target for therapy. In this chapter, we describe the preparation and use of sublines of LNCaP and C4-2 human prostate canc ...

High-affinity binding of testosterone or dihydrotestosterone to the androgen receptor (AR) triggers the androgen-dependent AR NH2- and carboxyl-terminal (N/C) interaction between the AR NH2-terminal FXXLF motif and the activation function 2 (AF2) hydrophobic binding surfa ...

The recruitment of co-repressors to the androgen receptor is an important mechanism for reducing androgen-mediated gene activation. Importantly, co-repressors play a major role in the treatment of hormone-dependent growing tissue, such as prostate cancer and breast cancer. In line ...

Androgen receptor (AR) is a ligand-controlled transcription factor that is deregulated and therefore targeted in prostate cancer. In addition to androgens, AR is regulated by post-translational modifications (PTMs). SUMOylation, conjugation of small ubiquitin-related mo ...

Acetylation is an essential post-translational modification in which an acetyl group is covalently conjugated to a protein substrate. Histone acetylation was first proposed nearly half a century ago by Dr. Vincent Allfrey. Subsequent studies have shown that acetylated core histon ...

Systems-level approaches have emerged that rely on analytical, microscopy-based technology for the discovery of novel drug targets and the mechanisms driving AR signaling, transcriptional activity, and ligand independence. Single cell behavior can be quantified by high-thr ...

Understanding the biology of prostate cancer and the roles of androgen receptor in prostate cancer progression is essential to the development of novel therapeutic strategies to effectively attack and eradicate this disease. Preclinical, in vivo, studies are critical to further ev ...

Androgen acting through the androgen receptor (AR) is known to be essential for male sexual differentiation and development. Using Cre-lox technology, we have generated the floxed AR mice, which have been bred with general or tissue-specific Cre expressing transgenic mice to knock out the AR ...

Chromatin immunoprecipitation (ChIP) is an invaluable tool in the study of transcriptional regulation. ChIP methods require both a priori knowledge of the transcriptional regulators which are important for a given biological system and high-quality specific antibodies for th ...

The human androgen receptor (AR) is expressed in nearly all prostate cancers (PCa) and is known to participate in tumor progression through the expression of genes involved in the proliferation and differentiation of PCa. It is suggested that different types of ligands induce a distinct AR co ...

Fusion between androgen-regulated TMPRSS2 and ETS transcription factor gene ERG is the most frequent genetic alteration that occurs in 40–70% of prostate cancers. Not only ERG but also other ETS transcription factor genes are involved in gene fusions. ETV1, ETV4, and ETV5 have all several fus ...

The balance between proliferation and cell death is often disrupted in cancer leading to tumor growth. In prostate cancer, these events are regulated, at least in part, through androgen signaling. Prostate cancer is dependent on androgens for growth in the initial stages where apoptosis is s ...

Increased metabolic activity is a hallmark of proliferating cancer cells. One common deregulated metabolic pathway in prostate cancer is de novo lipogenesis which is highly increased in prostate cancer and is linked to poor prognosis and metastasis. Male sex hormones play an essential r ...

Much evidence indicates that, with few exceptions, non-genomic actions of steroids are mediated by receptors universally known as nuclear receptors. Steroid receptors do not exhibit intrinsic tyrosine kinase activity. Nevertheless, they stimulate different signaling path ...

Androgen receptor (AR) is a ligand-dependent transcription factor that belongs to the nuclear receptor superfamily. In the presence of its specific ligands, AR translocates into the nucleus, interacts with chromatin at hormone response elements (HREs) and recruits a variety of coreg ...