Y0001591

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High-content positional biosensor screening assay for compounds to prevent or disrupt androgen receptor and transcriptional intermediary factor 2 protein-protein interactions.

Yun Hua et al.

Assay and drug development technologies, 12(7), 395-418 (2014-09-03)

The androgen receptor-transcriptional intermediary factor 2 (AR-TIF2) positional protein-protein interaction (PPI) biosensor assay described herein combines physiologically relevant cell-based assays with the specificity of binding assays by incorporating structural information of AR and TIF2 functional domains along with intracellular targeting

[Acute flutamide-induced hepatitis].

D Nicolás et al.

Gastroenterologia y hepatologia, 22(5), 262-263 (1999-07-09)

Inhibition of SGK1 enhances mAR-induced apoptosis in MCF-7 breast cancer cells.

Guilai Liu et al.

Cancer biology & therapy, 16(1), 52-59 (2014-11-27)

Functional membrane androgen receptors (mAR) have previously been described in MCF-7 breast cancer cells. Their stimulation by specific testosterone albumin conjugates (TAC) activate rapidly non-genomic FAK/PI3K/Rac1/Cdc42 signaling, trigger actin reorganization and inhibit cell motility. PI3K stimulates serum and glucocorticoid inducible

Activated androgen receptor promotes bladder cancer metastasis via Slug mediated epithelial-mesenchymal transition.

Yifeng Jing et al.

Cancer letters, 348(1-2), 135-145 (2014-03-26)

Androgen receptor (AR) has been indicated to be involved in bladder cancer progression. We showed androgen induced epithelial-mesenchymal transition (EMT) in AR-positive bladder cancer cells and promoted tumor metastasis in xenograft models. We subsequently identified that Slug was the mediator

Glucocorticoid-like activity of propylparaben, butylparaben, diethylhexyl phthalate and tetramethrin mixtures studied in the MDA-kb2 cell line.

Ivana Klopčič et al.

Toxicology letters, 232(2), 376-383 (2014-12-03)

Endocrine-disrupting compounds can interfere with the endocrine organs or hormone system and cause tumors, birth defects and developmental disorders in humans. The estrogen-like activity of compounds has been widely studied but little is known concerning their possible modulation of the

Prenatal influence of an androgen agonist and antagonist on the differentiation of the ovine sexually dimorphic nucleus in male and female lamb fetuses.

Charles E Roselli et al.

Endocrinology, 155(12), 5000-5010 (2014-09-13)

The ovine sexually dimorphic nucleus (oSDN) is 2 times larger in rams than in ewes. Sexual differentiation of the oSDN is produced by testosterone exposure during the critical period occurring between gestational day (GD)60 and GD90 (term, 147 d). We

[Hepatotoxicity due to flutamide].

E Caballería et al.

Medicina clinica, 102(11), 434-434 (1994-03-26)

Acute and fulminant hepatitis induced by flutamide: case series report and review of the literature.

Javier Brahm et al.

Annals of hepatology, 10(1), 93-98 (2011-02-09)

Flutamide is a non-steroidal anti-androgenic drug, commonly used in the treatment of advanced prostate cancer, acne and hirsutism. This drug may induce various degrees of liver injury, including acute liver failure (ALF), with further need for liver transplantation. Here, we

Assessment of estrogenic and anti-androgenic activities of the mycotoxin zearalenone and its metabolites using in vitro receptor-specific bioassays.

José-Manuel Molina-Molina et al.

Food and chemical toxicology : an international journal published for the British Industrial Biological Research Association, 74, 233-239 (2014-12-03)

Zearalenone (ZEN) is a well-known mycotoxin present in numerous agricultural products. Humans and animals are therefore at a risk of exposure to zearalenone through consumption of contaminated food. After intake, ZEN is reduced to α- and β-zearalenol (α-ZEL and β-ZEL)

Aromatase (Cyp19a1b) in the pituitary is dynamically involved in the upregulation of lhb but not fshb in the vitellogenic female ricefield eel Monopterus albus.

Shen Zhang et al.

Endocrinology, 155(11), 4531-4541 (2014-08-12)

Aromatase, encoded by Cyp19a1, is expressed in the pituitary of vertebrates; however, its physiological relevance remains poorly defined. In teleosts, the duplicated cyp19a1b is preferentially expressed in the pituitary where LH and FSH are synthesized in distinct gonadotropes. Our present

Expression of sex hormone receptors in juvenile angiofibromas and antiproliferative effects of receptor modulators.

Bernhard Schick et al.

Head & neck, 36(11), 1596-1603 (2013-09-03)

Predilection of juvenile angiofibromas in adolescent boys has prompted the hypothesis of hormone-dependent tumor growth. However, knowledge on expression and function of sex hormone receptors in juvenile angiofibromas is still sparse and inconsistent. Transcript and protein expression of sex hormone

Leuprolide with flutamide for complete androgen ablation: therapeutic alternative for advanced prostatic cancer (stage D2).

E Chime-Udeh

Connecticut medicine, 55(9), 526-528 (1991-09-01)

Peritubular myoid cells participate in male mouse spermatogonial stem cell maintenance.

Liang-Yu Chen et al.

Endocrinology, 155(12), 4964-4974 (2014-09-03)

Peritubular myoid (PM) cells surround the seminiferous tubule and together with Sertoli cells form the cellular boundary of the spermatogonial stem cell (SSC) niche. However, it remains unclear what role PM cells have in determining the microenvironment in the niche

Testosterone increases renal anti-aging klotho gene expression via the androgen receptor-mediated pathway.

Shih-Che Hsu et al.

The Biochemical journal, 464(2), 221-229 (2014-08-28)

Gender is known to be associated with longevity and oestrogen administration induced longevity-associated gene expression is one of the potential mechanisms underlying the benefits of oestrogen on lifespan, whereas the role of testosterone in the regulation of longevity-associated gene expressions

[Toxic hepatitis and liver failure under therapy with flutamide].

C Lübbert et al.

Der Internist, 45(3), 333-340 (2004-03-05)

Flutamide is an antiandrogen and frequently used for the treatment of prostatic cancer. Severe hepatotoxicity occurs in few patients but may be fatal. We report on two patients with prostatic cancer who received a therapy with flutamide. They showed different

Alterations in luteal production of androstenedione, testosterone, and estrone, but not estradiol, during mid- and late pregnancy in pigs: effects of androgen deficiency.

Malgorzata Grzesiak et al.

Theriogenology, 82(5), 720-733 (2014-07-12)

Recently, we have found that flutamide-induced androgen deficiency altered progesterone production in the porcine corpus luteum (CL) during mid- and late pregnancy. Herein, we tested whether flutamide administration subsequently influences androgen and estrogen metabolism in the CL of pregnancy. Pregnant

[The hepatotoxicity of flutamide].

A P Pogromov et al.

Klinicheskaia meditsina, 76(7), 56-58 (1998-09-22)

KLF9, a transcription factor induced in flutamide-caused cell apoptosis, inhibits AKT activation and suppresses tumor growth of prostate cancer cells.

Pengliang Shen et al.

The Prostate, 74(9), 946-958 (2014-04-17)

Kruppel-like factors (KLFs) are involved in various biological processes; emerging studies have indicated that KLF9 plays a critical role in regulating tumorigenesis. The role of KLF9 in prostate cancer (PCa), however, has not yet been investigated. The expression of KLF

Flutamide induced methemoglobinemia.

A M Khan et al.

The Journal of urology, 157(4), 1363-1363 (1997-04-01)

Coagulation factor VII is regulated by androgen receptor in breast cancer.

Ali Naderi

Experimental cell research, 331(1), 239-250 (2014-12-03)

Androgen receptor (AR) is widely expressed in breast cancer; however, there is limited information on the key molecular functions and gene targets of AR in this disease. In this study, gene expression data from a cohort of 52 breast cancer

[Fulminant liver failure with a fatal outcome due to flutamide].

C M Fernández Peña et al.

Medicina clinica, 108(6), 237-238 (1997-02-15)

Flutamide. A preliminary review of its pharmacodynamic and pharmacokinetic properties, and therapeutic efficacy in advanced prostatic cancer.

R N Brogden et al.

Drugs, 38(2), 185-203 (1989-08-01)

Flutamide is a non-steroidal antiandrogenic drug devoid of hormonal agonist activity. Flutamide appears to be a specific antiandrogen only at androgen-dependent accessory genital organs. Its pharmacological activity is due substantially to the principal metabolite, 2-hydroxyflutamide. In comparative trials involving small

Flutamide monotherapy as primary treatment in advanced prostatic carcinoma.

K P Delaere et al.

Seminars in oncology, 18(5 Suppl 6), 13-18 (1991-10-01)

Little is known about the efficacy of flutamide monotherapy in previously untreated patients with prostatic carcinoma. In this study, 40 patients with advanced disease were treated with 250 mg flutamide, three times daily. The mean follow-up was 7 months. After

Review of the histological effects of the anti-androgen, flutamide, on mouse testis.

Reiko Anahara et al.

Reproductive toxicology (Elmsford, N.Y.), 25(2), 139-143 (2008-02-05)

This is a mini-review summarizing recent findings on the effect of flutamide (FLUT), an anti-androgenic toxicant, on the mouse testis, particularly on the ectoplasmic specialization (ES) in the testis. FLUT induces a reduction in the weight of male reproductive tissues

Pharmacology and pharmacokinetics of flutamide.

R Neri

Urology, 34(4 Suppl), 19-21 (1989-10-01)

Flutamide is rapidly metabolized by hydroxylation of the side chain to SCH 16423 (alpha, alpha, alpha-trifluoro-2-methyl-4'-nitro-m-lactotoluidide), the major metabolic product in all species studied, which is biologically active in vivo and in vitro studies. Flutamide exhibits its antiandrogenic activity by

Ketoconazole and Flutamide in the treatment of disseminated intravascular clotting from prostate cancer: a case report and review.

S Chakrapee-Sirisuk et al.

Journal of the Medical Association of Thailand = Chotmaihet thangphaet, 84(10), 1495-1501 (2002-01-24)

Disseminated intravascular clotting (DIC) is a well-recognized complication of malignancy. Prostatic cancer can produce chronic DIC as well as acute severe DIC. Treatment of DIC are general supportive measures including heparin, transfusion of blood, platelets and clotting factors, but the

Screening of bisphenol A, triclosan and paraben analogues as modulators of the glucocorticoid and androgen receptor activities.

Katra Kolšek et al.

Toxicology in vitro : an international journal published in association with BIBRA, 29(1), 8-15 (2014-09-07)

A homeostasis of the glucocorticoid and androgen endocrine system is essential to human health. Their disturbance can lead to various diseases, for example cardiovascular, inflammatory and autoimmune diseases, infertility, cancer. Fifteen widely used industrial chemicals that disrupt endocrine activity were

[Basic and clinical characteristics of flutamide].

K Suzuki et al.

Nihon rinsho. Japanese journal of clinical medicine, 58 Suppl, 211-215 (2000-10-07)

Antiandrogen flutamide protects male mice from androgen-dependent toxicity in three models of spinal bulbar muscular atrophy.

Kayla J Renier et al.

Endocrinology, 155(7), 2624-2634 (2014-04-20)

Spinal and bulbar muscular atrophy (SBMA) is a late-onset, progressive neurodegenerative disease linked to a polyglutamine (polyQ) expansion in the androgen receptor (AR). Men affected by SBMA show marked muscle weakness and atrophy, typically emerging midlife. Given the androgen-dependent nature

Examining the role of testosterone in mediating short-term aggressive responses to social stimuli in a lizard.

Jo McEvoy et al.

PloS one, 10(4), e0125015-e0125015 (2015-04-24)

Hormones have been suggested as a key proximate mechanism that organize and maintain consistent individual differences in behavioural traits such as aggression. The steroid hormone testosterone in particular has an important activational role in mediating short-term aggressive responses to social

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