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Selective androgen receptor modulators

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https://www.readbyqxmd.com/read/29785666/evaluation-of-ostarine-as-a-selective-androgen-receptor-modulator-in-a-rat-model-of-postmenopausal-osteoporosis
#1
D B Hoffmann, M Komrakova, S Pflug, M von Oertzen, D Saul, L Weiser, T A Walde, M Wassmann, A F Schilling, W Lehmann, S Sehmisch
Selective androgen receptor modulators (SARMs) have shown beneficial effects on muscle wasting, general physical function and bone properties in male mammals. However, data on the effects of SARMs in postmenopausal osteoporotic bone are scarce. We evaluated the effects of the SARM drug ostarine on postmenopausal osteoporotic bone in a rat osteoporosis model. Ovariectomy was performed on 46 of 56 3-month-old female Sprague-Dawley rats. Eight weeks after ovariectomy, ostarine was orally administered daily for 5 weeks in dosages of 0...
May 21, 2018: Journal of Bone and Mineral Metabolism
https://www.readbyqxmd.com/read/29763383/eb-2017-article-soy-protein-isolate-feeding-does-not-result-in-reproductive-toxicity-in-the-pre-pubertal-rat-testis
#2
Martin Jj Ronis, Horacio Gomez-Acevedo, Kartik Shankar, Neha Sharma, Michael Blackburn, Rohit Singhal, Kelly E Mercer, Thomas M Badger
The isoflavone phytoestrogens found in the soy protein isolate used in soy infant formulas have been shown to have estrogenic actions in the developing male reproductive tract resulting in reproductive toxicity. However, few studies have examined potential estrogenicity of soy protein isolate as opposed to that of pure isoflavones. In this study, we fed weanling male Sprague-Dawley rats a semi-purified diet with casein or soy protein isolate as the sole protein source from postnatal day 21 to 33. Additional groups were fed casein or soy protein isolate and treated s...
May 2018: Experimental Biology and Medicine
https://www.readbyqxmd.com/read/29727260/in-house-validation-of-a-liquid-chromatography-tandem-mass-spectrometry-method-for-the-determination-of-selective-androgen-receptor-modulators-sarms-in-bovine-urine
#3
Kathrin S Schmidt, Joachim Mankertz
A sensitive and robust liquid chromatography - tandem mass spectrometry (LC-MS/MS) method allowing the rapid screening and confirmation of selective androgen receptor modulators (SARMS) in bovine urine was developed and successfully validated according to Commission Decision 2002/657/EC, chapter 3.1.3 "alternative validation", by applying a matrix-comprehensive in-house validation concept. The confirmation of the analytes in the validation samples was achieved both on the basis of the multiple reaction monitoring (MRM) ion ratios as laid down in Commission Decision 2002/657/EC and by comparison of their EPI spectra with a reference mass spectral library by making use of the QTRAP technology...
May 4, 2018: Food Additives & Contaminants. Part A, Chemistry, Analysis, Control, Exposure & Risk Assessment
https://www.readbyqxmd.com/read/29722624/cross-talk-between-androgen-and-wnt-signaling-potentially-contributes-to-age-related-skeletal-muscle-atrophy-in-rats
#4
Petey W Mumford, Matthew A Romero, Xuansong Mao, C Brooks Mobley, Wesley C Kephart, Cody T Haun, Paul A Roberson, Kaelin C Young, Jeffrey S Martin, Joshua F Yarrow, Darren T Beck, Michael D Roberts
We sought to determine whether age-related gastrocnemius muscle mass loss was associated with parallel decrements in androgen receptor (AR) or select Wnt signaling markers. To test this hypothesis, serum free and total testosterone (TEST) as well as gastrocnemius AR and Wnt signaling markers were analyzed in male Fischer 344 rats that were 3/6/12/18 and 24 months (mo) old (n=9 per group). Free and total TEST were greatest in 6 mo rats, and AR protein and Wnt5 protein levels linearly declined with aging. There were associations between Wnt5 protein levels and relative gastrocnemius mass (r=0...
May 3, 2018: Journal of Applied Physiology
https://www.readbyqxmd.com/read/29720561/androgen-receptor-signaling-reduces-radiosensitivity-in-bladder-cancer
#5
Hiroki Ide, Satoshi Inoue, Taichi Mizushima, Guiyang Jiang, Kuang-Hsiang Chuang, Mototsugu Oya, Hiroshi Miyamoto
Although radiotherapy often with chemotherapy has been shown to offer a survival benefit comparable to that of radical cystectomy in select patients with bladder cancer, the development of radiosensitization strategies may significantly enhance its application. Notably, emerging preclinical evidence has indicated the involvement of androgen receptor (AR) signaling in urothelial cancer progression. We here assessed whether AR signals could contribute to modulating radiosensitivity in bladder cancer cells. Ionizing radiation reduced the numbers of viable cells or colonies of AR-negative lines more significantly than those of AR-positive lines...
May 2, 2018: Molecular Cancer Therapeutics
https://www.readbyqxmd.com/read/29704771/new-approach-based-on-immunochemical-techniques-for-monitoring-of-selective-estrogen-receptor-modulators-serms-in-human-urine
#6
J-Pablo Salvador, Ester Vila-Roca, Núria Monfort, Rosa Ventura, M-Pilar Marco
Antiestrogenic compounds such as tamoxifen, toremifen and chlomifen are used illegally by athletes to minimize physical impacts such as gynecomastia resulting from the secondary effects of anabolic androgenic steroids, used to increase athletic efficiency unlawfully. The use of these compounds is banned by the World Anti-Doping Agency (WADA) and controls are made through analytical methodologies such as HPLC-MS/MS, which do not fulfil the sample throughput requirements. Moreover, compounds such as tamoxifen are also used to treat hormone receptor-positive breast cancer (ER + )...
April 22, 2018: Journal of Pharmaceutical and Biomedical Analysis
https://www.readbyqxmd.com/read/29683475/pharmacological-interventions-for-the-prevention-of-insufficiency-fractures-and-avascular-necrosis-associated-with-pelvic-radiotherapy-in-adults
#7
REVIEW
Qurrat U van den Blink, Kate Garcez, Caroline C Henson, Susan E Davidson, Claire E Higham
BACKGROUND: Pelvic radiotherapy is a treatment delivered to an estimated 150,000 to 300,000 people annually across high-income countries. Fractures due to normal stresses on weakened bone due to radiotherapy are termed insufficiency fractures. Pelvic radiotherapy-related interruption of the blood supply to the hip is termed avascular necrosis and is another recognised complication. The reported incidences of insufficiency fractures are 2.7% to 89% and risk of developing avascular necrosis is 0...
April 23, 2018: Cochrane Database of Systematic Reviews
https://www.readbyqxmd.com/read/29666640/investigating-the-interactive-effects-of-sex-steroid-hormones-and-brain-derived-neurotrophic-factor-during-adolescence-on-hippocampal-nmda-receptor-expression
#8
Cushla R McCarthny, Xin Du, YeeWen Candace Wu, Rachel A Hill
Sex steroid hormones have neuroprotective properties which may be mediated by brain-derived neurotrophic factor (BDNF). This study sought to determine the interactive effects of preadolescent hormone manipulation and BDNF heterozygosity (+/- ) on hippocampal NMDA-R expression. Wild-type and BDNF+/- mice were gonadectomised, and females received either 17 β -estradiol or progesterone treatment, while males received either testosterone or dihydrotestosterone (DHT) treatment. Dorsal (DHP) and ventral hippocampus (VHP) were dissected, and protein expression of GluN1, GluN2A, GluN2B, and PSD-95 was assessed by Western blot analysis...
2018: International Journal of Endocrinology
https://www.readbyqxmd.com/read/29649433/repurposing-sex-steroids-and-related-drugs-as-potential-treatment-for-parkinson-s-disease
#9
REVIEW
Mélanie Bourque, Marc Morissette, Thérèse Di Paolo
Parkinson's disease (PD) is a neurodegenerative disorder for which a greater prevalence and incidence is described in men. This suggests a protective effect of sex hormones in the brain. Therefore, steroids and drugs to treat endocrine conditions could have additional application for PD. Here, we review the protective effect of sex hormones, particularly estrogens, progesterone, androgens and dehydroepiandrosterone, in animal models of PD and also in human studies. Data also support that drugs affecting estrogen neurotransmission such as selective estrogen receptor modulators or affecting steroid metabolism with 5α-reductase inhibitors could be repositioned for treatment of PD...
April 9, 2018: Neuropharmacology
https://www.readbyqxmd.com/read/29621580/use-of-nutritional-supplements-contaminated-with-banned-doping-substances-by-recreational-adolescent-athletes-in-athens-greece
#10
Konstantinos Tsarouhas, Nassia Kioukia-Fougia, Petros Papalexis, Aristidis Tsatsakis, Dimitrios Kouretas, Flora Bacopoulou, Christina Tsitsimpikou
Although the use of nutritional supplements by adult athletes has been extensively studied, information on supplements consumption by adolescent athletes is still limited. The present study reports on the use of nutritional supplements contaminated with banned doping substances among 170 recreational adolescent athletes from eleven, randomly selected, gym centres, in Athens, Greece. Nutritional supplements consumption was reported by almost 60% of the study population, with proteins/amino acids and vitamins being the most popular...
April 2, 2018: Food and Chemical Toxicology
https://www.readbyqxmd.com/read/29605576/effects-of-maternal-dietary-selenium-se-enriched-yeast-on-testis-development-testosterone-level-and-testicular-steroidogenesis-related-gene-expression-of-their-male-kids-in-taihang-black-goats
#11
Lei Shi, Ruigao Song, Xiaolei Yao, Yunli Duan, Youshe Ren, Chunxiang Zhang, Wenbin Yue, Fulin Lei
To investigate the effects of maternal dietary selenium (Se-enriched yeast) on testis development, testosterone level and steroidogenesis-related gene expression in testis of their male kids, selected pregnant Taihang Black Goats were randomly allotted to four treatment groups. They were fed the basal gestation and lactation diets supplemented with 0 (control), 0.5, 2.0 and 4.0 mg of Se/kg DM. Thirty days after weaning, testes were collected from the kids. After the morphological development status of testis was examined, tissue samples were collected for analyzing testosterone concentration and histological parameters...
March 26, 2018: Theriogenology
https://www.readbyqxmd.com/read/29578828/the-cellular-and-molecular-effects-of-the-androgen-receptor-agonist-cl-4as-1-on-breast-cancer-cells
#12
Mamoun Ahram, Ebtihal Mustafa, Shatha Abu Hammad, Mariam Alhudhud, Randa Bawadi, Lubna Tahtamouni, Faisal Khatib, Malek Zihlif
PURPOSE: The androgen receptor (AR) has attracted attention in the treatment of breast cancer. Due to the undesirable side effects of AR agonists, attempts have been undertaken to develop selective AR modulators. One of these compounds is Cl-4AS-1. This study examined this compound more closely at the cellular and molecular levels. METHODS: Three different breast cancer cell lines were utilized, namely the luminal MCF-7 cells, the molecular apocrine MDA-MB-453 cells, and the triple negative, basal MDA-MB-231 cells...
March 26, 2018: Endocrine Research
https://www.readbyqxmd.com/read/29572126/bone-health-during-endocrine-therapy-for-cancer
#13
REVIEW
Tilman D Rachner, Robert Coleman, Peyman Hadji, Lorenz C Hofbauer
Preservation of bone health remains a long-term clinical challenge in patients with breast and prostate cancer. Osteoporosis, defined by a loss of bone mass and microarchitecture, often results in fragility fractures that are typically associated with a high socioeconomic burden. Endocrine therapy, a mainstay treatment in the management of patients with hormone-sensitive breast and prostate cancer in the adjuvant setting, commonly exerts adverse effects on the musculoskeletal system and is associated with an increased risk of osteoporosis and fractures...
March 20, 2018: Lancet Diabetes & Endocrinology
https://www.readbyqxmd.com/read/29560112/systematic-identification-of-functionally-relevant-risk-alleles-to-stratify-aggressive-versus-indolent-prostate-cancer
#14
Salpie Nowinski, Aida Santaolalla, Ben O'Leary, Massimo Loda, Ayesha Mirchandani, Mark Emberton, Mieke Van Hemelrijck, Anita Grigoriadis
Novel approaches for classification, including molecular features, are needed to direct therapy for men with low-grade prostate cancer (PCa), especially men on active surveillance. Risk alleles identified from genome-wide association studies (GWAS) could improve prognostication. Those risk alleles that coincided with genes and somatic copy number aberrations associated with progression of PCa were selected as the most relevant for prognostication. In a systematic literature review, a total of 698 studies were collated...
February 27, 2018: Oncotarget
https://www.readbyqxmd.com/read/29556396/longer-trinucleotide-repeats-of-androgen-receptor-are-associated-with-higher-testosterone-and-low-oxytocin-levels-in-diabetic-premature-ejaculatory-dysfunction-patients
#15
Haroon Latif Khan, Shahzad Bhatti, Sana Abbas, Yousaf Latif Khan, Rosa Maria Marquez Gonzalez, Muhammad Aslamkhan, Gerardo Rodriguez Gonzalez, Hikmet Hakan Aydin
Background: Despite its worldwide high occurrence, the obscurity regarding the description, epidemiology and management of premature ejaculation remains provocative. It is well established that male premature ejaculatory dysfunction is an increasing problem due to spontaneous ejaculation across a variety of general and clinical subjects. The main goal of this study was to determine the relationships between trinucleotide repeats of the androgen receptor (AR), sex steroids, and pituitary hormones with sexual function in men with type 2 diabetes mellitus (DM) and reported with acquired premature ejaculation (PE)...
2018: Basic and Clinical Andrology
https://www.readbyqxmd.com/read/29527831/development-of-a-selective-androgen-receptor-modulator-for-transdermal-use-in-hypogonadal-patients
#16
V Krishnan, N J Patel, J G Mackrell, S A Sweetana, H Bullock, Y L Ma, T H Waterhouse, B C Yaden, J Henck, Q Q Zeng, K Gavardinas, P Jadhav, A Saeed, P Garcia-Losada, D A Robins, C T Benson
We have identified a non-steroidal selective androgen receptor modulator (SARM), termed LY305, that is bioavailable through a transdermal route of administration while highly cleared via hepatic metabolism to limit parent compound exposure in the liver. Selection of this compound and its transdermal formulation was based on the optimization of skin absorption properties using both in vitro and in vivo skin models that supported PBPK modeling for human PK predictions. This molecule is an agonist in perineal muscle while being a weak partial agonist in the androgenic tissues such as prostate...
March 12, 2018: Andrology
https://www.readbyqxmd.com/read/29518658/in-vitro-profiling-of-toxic-effects-of-prominent-environmental-lower-chlorinated-pcb-congeners-linked-with-endocrine-disruption-and-tumor-promotion
#17
Kateřina Pěnčíková, Lucie Svržková, Simona Strapáčová, Jiří Neča, Iveta Bartoňková, Zdeněk Dvořák, Martina Hýžďalová, Jakub Pivnička, Lenka Pálková, Hans-Joachim Lehmler, Xueshu Li, Jan Vondráček, Miroslav Machala
The mechanisms contributing to toxic effects of airborne lower-chlorinated PCB congeners (LC-PCBs) remain poorly characterized. We evaluated in vitro toxicities of environmental LC-PCBs found in both indoor and outdoor air (PCB 4, 8, 11, 18, 28 and 31), and selected hydroxylated metabolites of PCB 8, 11 and 18, using reporter gene assays, as well as other functional cellular bioassays. We focused on processes linked with endocrine disruption, tumor promotion and/or regulation of transcription factors controlling metabolism of both endogenous compounds and xenobiotics...
June 2018: Environmental Pollution
https://www.readbyqxmd.com/read/29508640/the-use-of-selective-estrogen-receptor-modulators-on-bone-health-in-men
#18
Sok Kuan Wong, Nur-Vaizura Mohamad, Putri Ayu Jayusman, Ahmad Nazrun Shuid, Soelaiman Ima-Nirwana, Kok-Yong Chin
Selective estrogen receptor modulators (SERMs) represent a class of drugs that act as agonist or antagonist for estrogen receptor in a tissue-specific manner. The SERMs drugs are initially used for the prevention and treatment of osteoporosis in postmenopausal women. Bone health in prostate cancer patients has become a significant concern, whereby patients undergo androgen deprivation therapy is often associated with deleterious effects on bone. Previous preclinical and epidemiological findings showed that estrogens play a dominant role in improving bone health as compared to testosterone in men...
March 6, 2018: Aging Male: the Official Journal of the International Society for the Study of the Aging Male
https://www.readbyqxmd.com/read/29505030/selective-modulation-of-the-androgen-receptor-af2-domain-rescues-degeneration-in-spinal-bulbar-muscular-atrophy
#19
Nisha M Badders, Ane Korff, Helen C Miranda, Pradeep K Vuppala, Rebecca B Smith, Brett J Winborn, Emmanuelle R Quemin, Bryce L Sopher, Jennifer Dearman, James Messing, Nam Chul Kim, Jennifer Moore, Brian D Freibaum, Anderson P Kanagaraj, Baochang Fan, Heather Tillman, Ping-Chung Chen, Yingzhe Wang, Burgess B Freeman, Yimei Li, Hong Joo Kim, Albert R La Spada, J Paul Taylor
Spinal bulbar muscular atrophy (SBMA) is a motor neuron disease caused by toxic gain of function of the androgen receptor (AR). Previously, we found that co-regulator binding through the activation function-2 (AF2) domain of AR is essential for pathogenesis, suggesting that AF2 may be a potential drug target for selective modulation of toxic AR activity. We screened previously identified AF2 modulators for their ability to rescue toxicity in a Drosophila model of SBMA. We identified two compounds, tolfenamic acid (TA) and 1-[2-(4-methylphenoxy)ethyl]-2-[(2-phenoxyethyl)sulfanyl]-1H-benzimidazole (MEPB), as top candidates for rescuing lethality, locomotor function and neuromuscular junction defects in SBMA flies...
May 2018: Nature Medicine
https://www.readbyqxmd.com/read/29491216/selective-androgen-receptor-modulator-yk11-up-regulates-osteoblastic-proliferation-and-differentiation-in-mc3t3-e1-cells
#20
Tomofumi Yatsu, Taichi Kusakabe, Keisuke Kato, Yoshio Inouye, Kiyomitsu Nemoto, Yuichiro Kanno
Androgens are key regulators that play a critical role in the male reproductive system and have anabolic effects on bone mineral density and skeletal muscle mass. We have previously reported that YK11 is a novel selective androgen receptor modulator (SARM) and induces myogenic differentiation and selective gene regulation. In this study, we show that treatment of YK11 and dihydrotestosterone (DHT) accelerated cell proliferation and mineralization in MC3T3-E1 mouse osteoblast cells. Further, YK11-treated cells increased osteoblast specific differentiation markers, such as osteoprotegerin and osteocalcin, compared to untreated cells...
2018: Biological & Pharmaceutical Bulletin
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