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Selective androgen receptor modulators

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https://www.readbyqxmd.com/read/28315012/chlorinated-biphenyls-effect-on-estrogen-related-receptor-expression-steroid-secretion-mitochondria-ultrastructure-but-not-on-mitochondrial-membrane-potential-in-leydig-cells
#1
Agnieszka Milon, Malgorzata Opydo-Chanek, Waclaw Tworzydlo, Jerzy Galas, Laura Pardyak, Alicja Kaminska, Anna Ptak, Malgorzata Kotula-Balak
To characterize polychlorinated biphenyls (PCBs) action on Leydig cells, PCBs congeners, low-chlorinated (delor 103; d103) and high-chlorinated ones (delor 106; d106) were selected. The cells were treated according to PCBs dose (d103 or d106 0.2 ng/ml in low doses:, or 2 ng/ml in high doses) and type (d103 + d106 in low doses or 103 + 106 in high doses). After 24 h treatment with PCBs, a distinct increase in estrogen-related receptors (ERRs type α, β and γ) expression was revealed. However, the dose- and type-dependent PCBs effect was mostly exerted on ERRα expression...
March 18, 2017: Cell and Tissue Research
https://www.readbyqxmd.com/read/28275030/selective-androgen-receptor-modulator-in-a-patient-with-hormone-positive-metastatic-breast-cancer
#2
Namratha Vontela, Vamsi Koduri, Lee S Schwartzberg, Gregory A Vidal
Androgen receptors (ARs) are highly coexpressed in estrogen receptor (ER)-positive breast cancers. Their role in breast tumorigenesis has been postulated, but the mechanism is not yet well-characterized. Steroidal androgens were previously used as an anticancer strategy but fell out of favor because of toxicity and the discovery of alternative therapies. Recent attempts to modulate androgen pathway signaling have focused on AR inhibitors. This report discusses a case using a well-tolerated selective AR modulator to treat a highly pretreated patient with ER-positive breast cancer, which resulted in a durable partial response...
March 2017: Journal of the National Comprehensive Cancer Network: JNCCN
https://www.readbyqxmd.com/read/28235766/sigma1-targeting-to-suppress-aberrant-androgen-receptor-signaling-in-prostate-cancer
#3
Jeffrey D Thomas, Charles G Longen, Halley M Oyer, Nan Chen, Christina M Maher, Joseph M Salvino, Blase Kania, Kelsey N Anderson, William F Ostrander, Karen E Knudsen, Felix J Kim
Suppression of androgen receptor (AR) activity in prostate cancer by androgen depletion or direct AR antagonist treatment, although initially effective, leads to incurable castration resistant prostate cancer (CRPC) via compensatory mechanisms including resurgence of AR and AR splice variant (ARV) signaling. Emerging evidence suggests that Sigma1 (also known as sigma-1 receptor) is a unique chaperone or scaffolding protein that contributes to cellular protein homeostasis. We reported previously that some Sigma1-selective small molecules can be used to pharmacologically modulate protein homeostasis pathways...
February 24, 2017: Cancer Research
https://www.readbyqxmd.com/read/28228232/hormone-receptor-expression-profile-of-low-grade-serous-ovarian-cancers
#4
Marianna Buttarelli, Floriana Mascilini, Gian Franco Zannoni, Alessandra Ciucci, Enrica Martinelli, Flavia Filippetti, Giovanni Scambia, Gabriella Ferrandina, Daniela Gallo
OBJECTIVE: Low-grade serous ovarian carcinomas (LGSOCs) are a histological subtype of epithelial ovarian tumors, accounting for fewer than 5% of all cases of ovarian carcinoma. Due to the chemoresistant nature of this subtype a search for more effective systemic therapies is actively ongoing, hormonal therapy showing some degree of activity in this clinical setting. The present study ought to investigate the hormone receptor status of LGSOCs, as a strategy to provide molecular support for patient-tailored hormonal treatments...
February 20, 2017: Gynecologic Oncology
https://www.readbyqxmd.com/read/28149506/treatment-of-hypogonadism-current-and-future-therapies
#5
REVIEW
Arthi Thirumalai, Kathryn E Berkseth, John K Amory
The treatment of hypogonadism in men is of great interest to both patients and providers. There are a number of testosterone formulations currently available and several additional formulations under development. In addition, there are some lesser-used alternative therapies for the management of male hypogonadism, which may have advantages for certain patient groups. The future of hypogonadism therapy may lie in the development of selective androgen receptor modulators that allow the benefits of androgens whilst minimizing unwanted side effects...
2017: F1000Research
https://www.readbyqxmd.com/read/28137616/detection-of-sarms-in-doping-control-analysis
#6
Mario Thevis, Wilhelm Schänzer
The class of selective androgen receptor modulators (SARMs) has been the subject of intense and dedicated clinical research over the past two decades. Potential therapeutic applications of SARMs are manifold and focus particularly on the treatment of conditions manifesting in muscle loss such as general sarcopenia, cancer-associated cachexia, muscular dystrophy, etc. Consequently, based on the substantial muscle- and bone-anabolic properties of SARMs, these agents constitute substances with significant potential for misuse in sport and have therefore been added to the Word Anti-Doping Agency's (WADA's) Prohibited List in 2008...
January 27, 2017: Molecular and Cellular Endocrinology
https://www.readbyqxmd.com/read/28130434/selective-progesterone-receptor-modulator-sprm-ulipristal-acetate-upa-and-its-effects-on-the-human-endometrium
#7
L H R Whitaker, A A Murray, R Matthews, G Shaw, A R W Williams, P T K Saunders, H O D Critchley
STUDY QUESTION: What is the impact of administration of the selective progesterone receptor modulator (SPRM), ulipristal acetate (UPA) on the endometrium of women with fibroids? SUMMARY ANSWER: UPA administration altered expression of sex-steroid receptors and progesterone-regulated genes and was associated with low levels of glandular and stromal cell proliferation. WHAT IS KNOWN ALREADY: Administration of all SPRM class members results in PAEC (progesterone receptor modulator associated endometrial changes)...
January 26, 2017: Human Reproduction
https://www.readbyqxmd.com/read/28054434/in-vitro-phase-i-metabolism-of-selective-estrogen-receptor-modulators-in-horse-using-ultra-high-performance-liquid-chromatography-high-resolution-mass-spectrometry
#8
Karen Y Kwok, George H M Chan, Wai Him Kwok, Jenny K Y Wong, Terence S M Wan
Selective estrogen receptor modulators (SERMs) are chemicals that possess the anti-oestrogenic activities that are banned "in" and "out" of competition by the World Anti-Doping Agency (WADA) in human sports, and by the International Federation of Horseracing Authorities (IFHA) in horseracing. SERMs can be used as performance enhancing drugs to boost the level of androgens or to compensate for the adverse effects as a result of extensive use of androgenic anabolic steroids (AASs). SERMs have indeed been abused in human sports; hence, a similar threat can be envisaged in horseracing...
January 5, 2017: Drug Testing and Analysis
https://www.readbyqxmd.com/read/28013033/differential-sensitivity-to-estrogen-induced-opsin-expression-in-two-poeciliid-freshwater-fish-species
#9
Caitlin N Friesen, Mary E Ramsey, Molly E Cummings
The sensory system shapes an individual's perception of the world, including social interactions with conspecifics, habitat selection, predator detection, and foraging behavior. Sensory signaling can be modulated by steroid hormones, making these processes particularly vulnerable to environmental perturbations. Here we examine the influence of exogenous estrogen manipulation on the visual physiology of female western mosquitofish (Gambusia affinis) and sailfin mollies (Poecilia latipinna), two poeciliid species that inhabit freshwater environments across the southern United States...
December 21, 2016: General and Comparative Endocrinology
https://www.readbyqxmd.com/read/28002850/medical-management-of-endometriosis-in-patients-with-chronic-pelvic-pain
#10
Mohamed A Bedaiwy, Catherine Allaire, Paul Yong, Sukinah Alfaraj
Endometriosis is a common cause of pelvic pain in women of reproductive age. Traditional medical therapies are hormonal in nature, including estrogen-progestin contraceptives, progestins, and gonadotropin-releasing hormone (GnRH) agonists. Other hormonal options are androgens and aromatase inhibitors, with research also suggesting a possible role for GnRH antagonists and selective progesterone receptor modulators. Other than nonsteroidal anti-inflammatories, further work is required for nonhormonal therapies such as antiangiogenic and immune-modulating drugs...
January 2017: Seminars in Reproductive Medicine
https://www.readbyqxmd.com/read/27994732/development-of-n-4-phenoxyphenyl-benzenesulfonamide-derivatives-as-novel-nonsteroidal-progesterone-receptor-antagonists
#11
Ayumi Yamada, Yuko Kazui, Hiromasa Yoshioka, Aya Tanatani, Shuichi Mori, Hiroyuki Kagechika, Shinya Fujii
We report here development of N-(4-phenoxyphenyl)benzenesulfonamide derivatives as a novel class of nonsteroidal progesterone receptor (PR) antagonists. PR plays key roles in various physiological systems, including the female reproductive system, and PR antagonists are candidates for clinical treatment of multiple diseases, including uterine leiomyoma, endometriosis, breast cancer, and some psychiatric disorders. We found that the benzenesulfonanilide skeleton functions as a novel scaffold for PR antagonists, and we adopted 3-chlorobenzenesulfonyl derivative 20a as a lead compound for structural development...
December 8, 2016: ACS Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/27979262/effects-and-detection-of-nandrosol-and-ractopamine-administration-in-veal-calves
#12
Sara Divari, Enrica Berio, Paola Pregel, Alessandra Sereno, Luca Chiesa, Radmila Pavlovic, Sara Panseri, Toine F H Bovee, Bartolomeo Biolatti, Francesca T Cannizzo
The present study describes different effects of the selective androgen receptor modulator (SARM) nandrolone phenylpropionate (Nandrosol) and the β-agonist ractopamine administration in veal calves, and it investigates different strategies applied to trace these molecules. Morphological changes of gonads and accessory glands attributed to androgen effects, such as testicular atrophy, seminiferous tubule diameter reduction and hyperplasia of prostate epithelium, were detected, although SARMs are not described to cause these lesions...
April 15, 2017: Food Chemistry
https://www.readbyqxmd.com/read/27974229/selective-estrogen-receptor-modulators-and-the-vitamin-d-analogue-eldecalcitol-block-bone-loss-in-male-osteoporosis
#13
Yuiko Sato, Toshimi Tando, Mayu Morita, Kana Miyamoto, Tami Kobayashi, Ryuichi Watanabe, Takatsugu Oike, Morio Matsumoto, Masaya Nakamura, Takeshi Miyamoto
Rapid increases in the number of elderly people have dramatically increased the number of female and male osteoporosis patients. Osteoporosis often causes bone fragility fractures, and males exhibit particularly poor prognosis after these fractures, indicating that control of osteoporosis is crucial to maintain quality of men's lives. However, osteoporosis therapies available for men have lagged behind advances available for women. Here, we show that three selective estrogen receptor modulators (SERMs), namely, raloxifene, bazedoxifene, and tamoxifen, plus the vitamin D analogue ED71, also called eldecalcitol, completely block orchiectomy-induced, testosterone-depleted bone loss in male mice in vivo...
January 22, 2017: Biochemical and Biophysical Research Communications
https://www.readbyqxmd.com/read/27890446/efficacy-of-therapies-after-galeterone-in-patients-with-castration-resistant-prostate-cancer
#14
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
#15
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...
January 2017: Cell Death and Differentiation
https://www.readbyqxmd.com/read/27827563/analytical-strategies-to-detect-enobosarm-administration-in-bovines
#16
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 for consumers with food from animal origin that it is free from any residues of such compounds, analytical strategies are required to ensure safe food and also to enable fair trade between producers...
April 2017: Food Additives & Contaminants. Part A, Chemistry, Analysis, Control, Exposure & Risk Assessment
https://www.readbyqxmd.com/read/27729416/pushing-estrogen-receptor-around-in-breast-cancer
#17
REVIEW
Elgene Lim, Gerard Tarulli, Neil Portman, Theresa E 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...
December 2016: Endocrine-related Cancer
https://www.readbyqxmd.com/read/27726308/selective-androgen-receptor-modulators-comparative-excretion-study-of-bicalutamide-in-bovine-urine-and-faeces
#18
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
#19
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
#20
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
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