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Selective androgen receptor modulators

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https://www.readbyqxmd.com/read/28440570/mass-spectrometric-characterization-of-the-selective-androgen-receptor-modulator-sarm-yk-11-for-doping-control-purposes
#1
Mario Thevis, Thomas Piper, Josef Dib, Andreas Lagojda, Dirk Kuehne, Lars Packschies, Hans Geyer, Wilhelm Schaenzer
RATIONALE: Selective androgen receptor modulators (SARMs) represent an emerging class of therapeutics targeting inter alia conditions referred to as cachexia and sarcopenia. Due to their anabolic properties, the use of SARMs is prohibited in sports as regulated by the World Anti-Doping Agency (WADA), and doping control laboratories test for these anabolic agents in blood and urine. In order to accomplish and maintain comprehensive test methods, the characterization of new drug candidates is critical for efficient sports drug testing...
April 25, 2017: Rapid Communications in Mass Spectrometry: RCM
https://www.readbyqxmd.com/read/28428441/selective-glucocorticoid-receptor-modulators-sgrms-delay-castrate-resistant-prostate-cancer-growth
#2
Jacob Kach, Tiha M Long, Phillip Selman, Eva Y Tonsing-Carter, Maria A Bacalao, Ricardo R Lastra, Larischa de Wet, Shane Comiskey, Marc Gillard, Calvin VanOpstall, Diana C West, Wen-Ching Chan, Donald Vander Griend, Suzanne D Conzen, Russell Z Szmulewitz
Increased glucocorticoid receptor (GR) expression and activity following androgen blockade can contribute to castration-resistant prostate cancer (CRPC) progression. Therefore, we hypothesized that GR antagonism will have therapeutic benefit in CRPC. However, the FDA-approved nonselective, steroidal GR antagonist, mifepristone, lacks GR specificity, reducing its therapeutic potential. Here we report that two novel non-steroidal and highly selective GR modulators (SGRMs), CORT118335 and CORT108297, have the ability to block GR activity in prostate cancer (PC) and slow CRPC progression...
April 20, 2017: Molecular Cancer Therapeutics
https://www.readbyqxmd.com/read/28382513/rna-splicing-and-splicing-regulator-changes-in-prostate-cancer-pathology
#3
REVIEW
Jennifer Munkley, Karen Livermore, Prabhakar Rajan, David J Elliott
Changes in mRNA splice patterns have been associated with key pathological mechanisms in prostate cancer progression. The androgen receptor (abbreviated AR) transcription factor is a major driver of prostate cancer pathology and activated by androgen steroid hormones. Selection of alternative promoters by the activated AR can critically alter gene function by switching mRNA isoform production, including creating a pro-oncogenic isoform of the normally tumour suppressor gene TSC2. A number of androgen-regulated genes generate alternatively spliced mRNA isoforms, including a prostate-specific splice isoform of ST6GALNAC1 mRNA...
April 5, 2017: Human Genetics
https://www.readbyqxmd.com/read/28363748/synthesis-and-biological-evaluation-of-novel-selective-androgen-receptor-modulators-sarms-part-ii-optimization-of-4-pyrrolidin-1-yl-benzonitrile-derivatives
#4
Moriteru Asano, Takenori Hitaka, Takashi Imada, Masami Yamada, Megumi Morimoto, Hiromi Shinohara, Takahito Hara, Masuo Yamaoka, Takashi Santou, Masaharu Nakayama, Yumi Imai, Noriyuki Habuka, Jason Yano, Keith Wilson, Hisashi Fujita, Atsushi Hasuoka
We recently reported a class of novel tissue-selective androgen receptor modulators (SARMs), represented by a naphthalene derivative A. However, their pharmacokinetic (PK) profiles were poor due to low metabolic stability. To improve the PK profiles, we modified the hydroxypyrrolidine and benzonitrile substituents of 4-(pyrrolidin-1-yl)benzonitrile derivative B, which had a comparable potency as that of compound A. This optimization led us to further modifications, which improved metabolic stability while maintaining potent androgen agonistic activity...
May 1, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28345956/modulation-of-steroidogenesis-by-vitamin-d3-in-granulosa-cells-of-the-mouse-model-of-polycystic-ovarian-syndrome
#5
Shabnam Bakhshalizadeh, Fardin Amidi, Ashraf Alleyassin, Masoud Soleimani, Reza Shirazi, Maryam Shabani Nashtaei
Polycystic ovarian syndrome (PCOS) is the most common endocrine disorder of women of reproductive age characterized by polycystic ovarian morphology, anovulation or oligomenorrhea, and hyperandrogenism. It is shown that disruption in the steroidogenesis pathway caused by excess androgen in PCOS is a critical element of abnormal folliculogenesis and failure in dominant follicle selection. Vitamin D plays an important role in the regulation of ovulatory dysfunction and can influence genes involved in steroidogenesis in granulosa cells...
June 2017: Systems Biology in Reproductive Medicine
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
#6
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
#7
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
#8
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
#9
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
#10
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
#11
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
#12
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)...
March 1, 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
#13
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
#14
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
#15
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
#16
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
#17
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
#18
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
#19
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
#20
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
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