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Selective androgen receptor modulators

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https://www.readbyqxmd.com/read/27890446/efficacy-of-therapies-after-galeterone-in-patients-with-castration-resistant-prostate-cancer
#1
Rana R McKay, Lillian Werner, Matthew Fiorillo, Jennifer Roberts, Elisabeth I Heath, Glenn J Bubley, Robert Bruce Montgomery, Mary-Ellen Taplin
BACKGROUND: Galeterone is a multi-targeted agent with activity as a CYP17 inhibitor, androgen receptor antagonist, and also causes androgen receptor degradation. It has shown meaningful anti-tumor activity with a well-tolerated safety profile in patients with castration-resistant prostate cancer (CRPC) in phase I and II studies; however, the efficacy of currently approved CRPC therapies after treatment with galeterone is unknown. In this study, we evaluate prostate specific antigen (PSA) response of non-protocol therapies following galeterone in a subset of patients treated on the Androgen Receptor Modulation Optimized for Response (ARMOR) 2 study...
October 27, 2016: Clinical Genitourinary Cancer
https://www.readbyqxmd.com/read/27858941/block-one-unleash-a-hundred-mechanisms-of-dab2ip-inactivation-in-cancer
#2
REVIEW
Arianna Bellazzo, Giulio Di Minin, Licio Collavin
One of the most defining features of cancer is aberrant cell communication; therefore, a molecular understanding of the intricate network established among tumor cells and their microenvironment could significantly improve comprehension and clinical management of cancer. The tumor suppressor DAB2IP (Disabled homolog 2 interacting protein), also known as AIP1 (ASK1 interacting protein), has an important role in this context, as it modulates signal transduction by multiple inflammatory cytokines and growth factors...
November 18, 2016: Cell Death and Differentiation
https://www.readbyqxmd.com/read/27827563/analytical-strategies-to-detect-enobosarm-administration-in-bovines
#3
Nora Cesbron, Alexandre Sydor, Mylène Penot, Stéphanie Prevost, Bruno Le Bizec, Gaud Dervilly-Pinel
Selective androgen receptor modulators (SARMs) are a novel class of androgen receptor ligands. They are intended to exhibit the same kind of effects as androgenic drugs, like anabolic steroids, but be much more selective in their action, targeting particular tissues without any undesirable effects on others. While the main applications of these synthetic substances are for therapeutic purposes, they also have a high potential for misuse in veterinary practice and the sporting world. In order to guarantee the consumers with food from animal origin free from any residues of such compounds, analytical strategies are required to ensure safe food and also enable fair trade between producers...
November 9, 2016: Food Additives & Contaminants. Part A, Chemistry, Analysis, Control, Exposure & Risk Assessment
https://www.readbyqxmd.com/read/27729416/pushing-estrogen-receptor-around-in-breast-cancer
#4
Elgene Lim, Gerard Tarulli, Neil Portman, Theresa Hickey, Wayne D Tilley, Carlo Palmieri
The estrogen receptor-α (herein called ER) is a nuclear sex steroid receptor (SSR) that is expressed in approximately 75% of breast cancers. Therapies that modulate ER action have substantially improved the survival of patients with ER-positive breast cancer, but resistance to treatment still remains a major clinical problem. Treating resistant breast cancer requires co-targeting of ER and alternate signalling pathways that contribute to resistance to improve the efficacy and benefit of currently available treatments...
October 11, 2016: Endocrine-related Cancer
https://www.readbyqxmd.com/read/27726308/selective-androgen-receptor-modulators-comparative-excretion-study-of-bicalutamide-in-bovine-urine-and-faeces
#5
Dante Rojas, Gaud Dervilly-Pinel, Nora Cesbron, Mylène Penot, Alexandre Sydor, Stéphanie Prévost, Bruno Le Bizec
Besides their development for therapeutic purposes, non-steroidal selective androgen receptor modulators (non-steroidal SARMs) are also known to impact growth-associated pathways as ligands of androgenic receptors (AR). They present a potential for abuse in sports and food-producing animals as an interesting alternative to anabolic androgenic steroids (AAS). These compounds are easily available and could therefore be (mis)used in livestock production as growth promoters. To prevent such practices, dedicated analytical strategies should be developed for specific and sensitive detection of these compounds in biological matrices...
October 11, 2016: Drug Testing and Analysis
https://www.readbyqxmd.com/read/27693991/simplifying-and-expanding-analytical-capabilities-for-various-classes-of-doping-agents-by-means-of-direct-urine-injection-high-performance-liquid-chromatography-high-resolution-high-accuracy-mass-spectrometry
#6
Christian Görgens, Sven Guddat, Andreas Thomas, Philipp Wachsmuth, Anne-Katrin Orlovius, Gerd Sigmund, Mario Thevis, Wilhelm Schänzer
So far, in sports drug testing compounds of different classes are processed and measured using different screening procedures. The constantly increasing number of samples in doping analysis, as well as the large number of substances with doping related, pharmacological effects require the development of even more powerful assays than those already employed in sports drug testing, indispensably with reduced sample preparation procedures. The analysis of native urine samples after direct injection provides a promising analytical approach, which thereby possesses a broad applicability to many different compounds and their metabolites, without a time-consuming sample preparation...
November 30, 2016: Journal of Pharmaceutical and Biomedical Analysis
https://www.readbyqxmd.com/read/27681158/tissue-selective-androgen-receptor-modulators-sarms-increase-pelvic-floor-muscle-mass-in-ovariectomized-mice
#7
Suriyan Ponnusamy, Ryan D Sullivan, Thirumagal Thiyagarajan, Heather Tillmann, Robert H Getzenberg, Ramesh Narayanan
Stress urinary incontinence (SUI), a prevalent condition, is represented by an involuntary leakage of urine that results, at least in part, from weakened or damaged pelvic floor muscles and is triggered by physical stress. Current treatment options are limited with no oral therapies available. The pelvic floor is rich in androgen receptor and molecules with anabolic activity including selective androgen receptor modulators (SARMs) may serve as therapeutic options for individuals with SUI. In this study, two SARMs (GTx-024 and GTx-027) were evaluated in a post-menopausal animal model in order to determine their effect on pelvic floor muscles...
September 28, 2016: Journal of Cellular Biochemistry
https://www.readbyqxmd.com/read/27660402/circadian-rhythmicity-and-the-influence-of-clock-genes-on-prostate-cancer
#8
Zsofia Kiss, Paramita M Ghosh
The androgen receptor (AR) plays a key role in the development and progression of prostate cancer (CaP). Since the mid-1990s, reports in the literature pointed out higher incidences of CaP in some select groups, such as airline pilots and night shift workers in comparison to those working regular hours. The common finding in these 'high-risk' groups was that they all experienced a deregulation of the body's internal circadian rhythm. Here we discuss how the circadian rhythm affects androgen levels and modulates CaP development and progression...
September 22, 2016: Endocrine-related Cancer
https://www.readbyqxmd.com/read/27606620/reconfiguring-the-ar-tif2-protein-protein-interaction-hcs-assay-in-prostate-cancer-cells-and-characterizing-the-hits-from-a-lopac-screen
#9
Ashley T Fancher, Yun Hua, Daniel P Camarco, David A Close, Christopher J Strock, Paul A Johnston
The continued activation of androgen receptor (AR) transcription and elevated expression of AR and transcriptional intermediary factor 2 (TIF2) coactivator observed in prostate cancer (CaP) recurrence and the development of castration-resistant CaP (CRPC) support a screening strategy for small-molecule inhibitors of AR-TIF2 protein-protein interactions (PPIs) to find new drug candidates. Small molecules can elicit tissue selective effects, because the cells of distinct tissues express different levels and cohorts of coregulatory proteins...
October 2016: Assay and Drug Development Technologies
https://www.readbyqxmd.com/read/27586511/opioid-induced-androgen-deficiency-opiad-diagnosis-management-and-literature-review
#10
REVIEW
Timothy K O'Rourke, Matthew S Wosnitzer
Opioid-induced androgen deficiency (OPIAD) was initially recognized as a possible consequence of opioid use roughly four decades ago. Long-acting opioid use carries risks of addiction, tolerance, and systemic side effects including hypogonadotropic hypogonadism with consequent testosterone depletion leading to multiple central and peripheral effects. Hypogonadism is induced through direct inhibitory action of opioids on receptors within the hypothalamic-pituitary-gonadal (HPG) and hypothalamic-pituitary-adrenal (HPA) axes as well as testosterone production within the testes...
October 2016: Current Urology Reports
https://www.readbyqxmd.com/read/27552127/emerging-medication-for-the-treatment-of-male-hypogonadism
#11
Aydogan Aydogdu, Ronald S Swerdloff
INTRODUCTION: Male hypogonadism is characterized by inadequate production of Testosterone (T) (hypoandrogenism) and deficiencies in spermatogenesis. The main treatment of male hypogonadism is T replacement therapy (TRT), but for some of the patients, alternative drugs may be more suitable. AREAS COVERED: The available literature of T and alternative treatments for male hypogonadism are discussed. EXPERT OPINION: Transdermal application of T gels are the most commonly used route of T administration...
September 2016: Expert Opinion on Emerging Drugs
https://www.readbyqxmd.com/read/27535042/novel-uses-for-the-anabolic-androgenic-steroids-nandrolone-and-oxandrolone-in-the-management-of-male-health
#12
REVIEW
Christopher Wu, Jason R Kovac
There has recently been renewed interest in novel clinical applications of the anabolic-androgenic steroid (AAS) testosterone and its synthetic derivatives, particularly given with the rising popularity of testosterone supplementation therapy (TST) for the treatment of male hypogonadism. In this manuscript, we provide a brief review of the history of AAS and discuss clinical applications of two of the more well-known AAS: nandrolone and oxandrolone. Both agents exhibit favorable myotrophic/androgenic ratios and have been investigated for effectiveness in numerous disease states...
October 2016: Current Urology Reports
https://www.readbyqxmd.com/read/27499010/epigenetic-modulation-of-ar-gene-expression-in-prostate-cancer-du145-cells-with-the-combination-of-sodium-butyrate-and-5-aza-2-deoxycytidine
#13
Barbora Fialova, Petra Luzna, Jan Gursky, Katerina Langova, Zdenek Kolar, Katerina Smesny Trtkova
The androgen receptor (AR) plays an essential role in the development and progression of prostate cancer. Castration-resistant prostate cancer (CRPC) is a consequence of androgen deprivation therapy. Unchecked CRPC followed by metastasis is lethal. Some CRPCs show decreased AR gene expression due to epigenetic mechanisms such as DNA methylation and histone deacetylation. The aim of this study was to epigenetically modulate the methylated state of the AR gene leading to targeted demethylation and AR gene expression in androgen-independent human prostate cancer DU145 cell line, representing the CRPC model with very low or undetectable AR levels...
October 2016: Oncology Reports
https://www.readbyqxmd.com/read/27484626/evolving-novel-chemical-entities-for-management-of-benign-prostatic-hyperplasia
#14
Vishnu Lal Sharma, Sonal Gupta, Gopal Gupta
Proliferation of the smooth muscle and epithelial cells within the prostatic transition zone in older men leads to benign prostatic hyperplasia (BPH) which is hallmarked by the troublesome lower urinary tract symptoms. The affair responsible for the initiation and promotion of disease is still unresolved. Alpha blockers and 5α-reductase inhibitors are used as management options for relief of the dynamic and static components respectively. Combination therapy including both the alpha blocker and 5α-reductase inhibitors is emerging as inclusive parcel for treatment...
June 30, 2016: Mini Reviews in Medicinal Chemistry
https://www.readbyqxmd.com/read/27431683/identification-of-nr0b1-as-a-novel-androgen-receptor-co-repressor-in-mouse-sertoli-cells
#15
Yu-Chi Li, Man-Ling Luo, Huan Guo, Tian-Tian Wang, Shou-Ren Lin, Jian-Bo Chen, Qian Ma, Yan-Li Gu, Zhi-Mao Jiang, Yao-Ting Gui
Nuclear receptor subfamily 0 group B member 1 (Nr0b1) is an atypical member of the nuclear receptor family that is predominantly expressed in mouse Sertoli cells (SCs). Mutations of NR0B1 in humans cause adrenal failure and hypogonadotropic hypogonadism. The targeted mutagenesis of Nr0b1 in mice has revealed a primary gonadal defect characterized by the overexpression of aromatase and cellular obstruction of the seminiferous tubules and efferent ductules, leading to germ cell death and infertility. The transgenic expression of Nr0b1 under the control of the Müllerian-inhibiting substance promoter (MIS-Nr0b1), which is selectively expressed in SCs, improves fertility...
September 2016: International Journal of Molecular Medicine
https://www.readbyqxmd.com/read/27419898/identification-of-selected-in-vitro-generated-phase-i-metabolites-of-the-steroidal-selective-androgen-receptor-modulator-mk-0773-for-doping-control-purposes
#16
Andreas Lagojda, Dirk Kuehne, Oliver Krug, Andreas Thomas, Tina Wigger, Uwe Karst, Wilhelm Schänzer, Mario Thevis
Research into developing anabolic agents for various therapeutic purposes has been pursued for decades. As the clinical utility of anabolic-androgenic steroids has been found to be limited because of their lack of tissue selectivity and associated off-target effects, alternative drug entities have been designed and are commonly referred to as selective androgen receptor modulators (SARMs). While most of these SARMs are of nonsteroidal structure, the drug candidate MK-0773 comprises a 4-aza-steroidal nucleus...
2016: European Journal of Mass Spectrometry
https://www.readbyqxmd.com/read/27402268/ba321-a-novel-carborane-analog-that-binds-to-androgen-and-estrogen-receptors-acts-as-a-new-selective-androgen-receptor-modulator-of-bone-in-male-mice
#17
Kenta Watanabe, Michiko Hirata, Tsukasa Tominari, Chiho Matsumoto, Yasuyuki Endo, Gillian Murphy, Hideaki Nagase, Masaki Inada, Chisato Miyaura
Carboranes are a class of carbon-containing polyhedral boron cluster compounds with globular geometry and hydrophobic surface that interact with hormone receptors such as estrogen receptor (ER) and androgen receptor (AR). We have synthesized BA321, a novel carborane compound, which binds to AR. We found here that it also binds to ERs, ERα and ERβ. In orchidectomized (ORX) mice, femoral bone mass was markedly reduced due to androgen deficiency and BA321 restored bone loss in the male, whilst the decreased weight of seminal vesicle in ORX mice was not recovered by administration of BA321...
September 9, 2016: Biochemical and Biophysical Research Communications
https://www.readbyqxmd.com/read/27393623/a-novel-approach-to-breast-cancer-prevention-reducing-excessive-ovarian-androgen-production-in-elderly-women
#18
Giorgio Secreto, Sabina Sieri, Claudia Agnoli, Sara Grioni, Paola Muti, Barnett Zumoff, Milena Sant, Elisabetta Meneghini, Vittorio Krogh
Minimizing endogenous estrogen production and activity in women at high risk for breast cancer is a prominent approach to prevention of the disease. A number of clinical trials have shown that the administration of selective-estrogen receptor modulators or aromatase inhibitors significantly reduces the incidence of breast cancer in healthy women. Unfortunately, these drugs often produce adverse effects on the quality of life and are, therefore, poorly accepted by many women, even those who are at high risk for breast cancer...
August 2016: Breast Cancer Research and Treatment
https://www.readbyqxmd.com/read/27382931/novel-therapeutic-options-for-cachexia-and-sarcopenia
#19
Alessio Molfino, Maria Ida Amabile, Filippo Rossi Fanelli, Maurizio Muscaritoli
INTRODUCTION: Cachexia and sarcopenia are conditions phenotypically characterized by muscle loss and represent a factor of poor prognosis, increasing patients' morbidity and mortality. Cachectic and sarcopenic patients often suffer from low quality of life, presenting lower muscle strength and appetite loss, which makes research on novel treatment strategies to ameliorate clinical response including patient's symptoms, the objective of scientific interest. AREAS COVERED: This article covers recent developments in the area of cachexia and sarcopenia treatment and therapeutic interventions, targeting central nervous system involvement, key inflammatory and muscle-specific metabolic pathways...
October 2016: Expert Opinion on Biological Therapy
https://www.readbyqxmd.com/read/27364545/steroid-hormone-receptors-and-prostate-cancer-role-of-structural-dynamics-in-therapeutic-targeting
#20
REVIEW
Raj Kumar
Steroid hormone receptors (SHRs) act in cell type- and gene-specific manner through interactions with coregulatory proteins to regulate numerous physiological and pathological processes at the level of gene regulation. Binding of steroid receptor modulator (SRM) ligand leads to allosteric changes in SHR to exert positive or negative effects on the expression of target genes. Due, in part, to the fact that current SRMs generally target ligand binding domain (LBD)/AF2 and neglect intrinsically disordered (ID) N-terminal domain (NTD)/AF1, clinically relevant SRMs lack selectivity and are also prone to the development of resistance over time...
September 2016: Asian Journal of Andrology
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