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https://www.readbyqxmd.com/read/28624515/development-of-selective-androgen-receptor-modulators-sarms
#1
REVIEW
Ramesh Narayanan, Christopher C Coss, James T Dalton
The Androgen Receptor (AR), a member of the steroid hormone receptor family, plays important roles in the physiology and pathology of diverse tissues. AR ligands, which include circulating testosterone and locally synthesized dihydrotestosterone, bind to and activate the AR to elicit their effects. Ubiquitous expression of the AR, metabolism and cross reactivity with other receptors limit broad therapeutic utilization of steroidal androgens. However, the discovery of selective androgen receptor modulators (SARMs) and other tissue-selective nuclear hormone receptor modulators that activate their cognate receptors in a tissue-selective manner provides an opportunity to promote the beneficial effects of androgens and other hormones in target tissues with greatly reduced unwanted side-effects...
June 15, 2017: Molecular and Cellular Endocrinology
https://www.readbyqxmd.com/read/28621446/commentary-on-clark-et-al-the-long-and-winding-road-for-selective-androgen-receptor-modulators-sarms
#2
James T Dalton
No abstract text is available yet for this article.
June 16, 2017: British Journal of Clinical Pharmacology
https://www.readbyqxmd.com/read/28580894/hospital-acquired-methicillin-resistant-staphylococcus-aureus-bloodstream-infections-in-qu%C3%A3-bec-impact-of-guidelines
#3
Lynne Li, Elise Fortin, Claude Tremblay, Muleka Ngenda-Muadi, Christophe Garenc, Danielle Moisan, Jasmin Villeneuve, Caroline Quach
OBJECTIVE We examined the impact of methicillin-resistant Staphylococcus aureus (MRSA) guidelines in Québec adult hospitals from January 1, 2006, to March 31, 2015, by examining the incidence rate reduction (IRR) in healthcare-associated MRSA bloodstream infections (HA-MRSA), using central-line associated bloodstream infections (CLABSIs) as a comparator. METHODS In this study, we utilized a quasi-experimental design with Poisson segmented regression to model HA-MRSA and CLABSI incidence for successive 4-week surveillance segments, stratified by teaching status...
June 5, 2017: Infection Control and Hospital Epidemiology
https://www.readbyqxmd.com/read/28499507/nasolabial-changes-after-two-different-approaches-for-surgically-assisted-rapid-maxillary-expansion
#4
N Alves, T F M Oliveira, V A Pereira-Filho, E S Gonçales, M A C Gabrielli, L A Passeri
This retrospective study evaluated the nasolabial changes in patients who underwent surgically assisted rapid maxillary expansion (SARME) using two different approaches. Nineteen patients were included in the study, divided into two groups according to the kind of surgical approach performed: group 1 (n=9), SARME performed through the standard Le Fort I circumvestibular approach followed by the alar base cinch, and group 2 (n=10), SARME performed through a subtotal vestibular approach associated to a V-shaped incision at the maxillary midline in the labial frenulum region, without alar base cinch...
May 9, 2017: International Journal of Oral and Maxillofacial Surgery
https://www.readbyqxmd.com/read/28468164/effects-of-surgical-and-nonsurgical-rapid-maxillary-expansion-on-palatal-structures
#5
Gökmen Kurt, Ayşe Tuba Altuğ, Gökhan Türker, Banu Kiliç, Erdem Kiliç, Alper Alkan
AIM: The aim of the present study was to compare the effects of surgical and nonsurgical rapid maxillary expansion (RME) in skeletally mature patients. MATERIALS AND METHODS: Surgically assisted rapid maxillary expansion (SARME) was used in 18 patients (2 males, 16 females) with a mean age of 19.90 years. Two nonsurgical RME groups were constructed to compare the expansion changes of SARME. Eighteen patients in maximum pubertal peak (12 males, 6 females) with a mean age of 13...
May 2017: Journal of Craniofacial Surgery
https://www.readbyqxmd.com/read/28454849/synthesis-and-biological-evaluation-of-novel-selective-androgen-receptor-modulators-sarms-part-iii-discovery-of-4-5-oxopyrrolidine-1-yl-benzonitrile-derivative-2f-as-a-clinical-candidate
#6
Katsuji Aikawa, Moriteru Asano, Koji Ono, Noriyuki Habuka, Jason Yano, Keith Wilson, Hisashi Fujita, Hitoshi Kandori, Takahito Hara, Megumi Morimoto, Takashi Santou, Masuo Yamaoka, Masaharu Nakayama, Atsushi Hasuoka
We previously reported that 4-(pyrrolidin-1-yl)benzonitrile derivative 1b was a selective androgen receptor modulator (SARM) that exhibited anabolic effects on organs such as muscles and the central nervous system (CNS), but neutral effects on the prostate. From further modification, we identified that 4-(5-oxopyrrolidine-1-yl)benzonitrile derivative 2a showed strong AR binding affinity with improved metabolic stabilities. Based on these results, we tried to enhance the AR agonistic activities by modifying the substituents of the 5-oxopyrrolidine ring...
July 1, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/28453658/androgen-receptor-agonists-increase-lean-mass-improve-cardiopulmonary-functions-and-extend-survival-in-preclinical-models-of-duchenne-muscular-dystrophy
#7
Suriyan Ponnusamy, Ryan D Sullivan, Dahui You, Nadeem Zafar, Chuan He Yang, Thirumagal Thiyagarajan, Daniel L Johnson, Maron L Barrett, Nikki J Koehler, Mayra Star, Erin J Stephenson, Dave Bridges, Stephania A Cormier, Lawrence M Pfeffer, Ramesh Narayanan
Duchenne muscular dystrophy (DMD) is a neuromuscular disease that predominantly affects boys as a result of mutation(s) in the dystrophin gene. DMD is characterized by musculoskeletal and cardiopulmonary complications, resulting in shorter life-span. Boys afflicted by DMD typically exhibit symptoms within 3-5 years of age and declining physical functions before attaining puberty. We hypothesized that rapidly deteriorating health of pre-pubertal boys with DMD could be due to diminished anabolic actions of androgens in muscle, and that intervention with an androgen receptor (AR) agonist will reverse musculoskeletal complications and extend survival...
July 1, 2017: Human Molecular Genetics
https://www.readbyqxmd.com/read/28449232/safety-pharmacokinetics-and-pharmacologic-effects-of-the-selective-androgen-receptor-modulator-gsk2881078-in-healthy-men-and-postmenopausal-women
#8
Richard V Clark, Ann C Walker, Susan Andrews, Philip Turnbull, Jeffrey A Wald, Mindy H Magee
AIM: Selective androgen receptor modulators (SARMs) induce anabolic effects on muscle without the adverse effects of androgenic steroids. In this first-in-human study, we report safety, tolerability, pharmacokinetics (PK), and pharmacodynamics of the SARM GSK2881078. METHODS: In Part A, healthy young men (n = 10) received a single dose of study drug (0 mg, 0.05 mg, 0.1 mg, 0.2 mg GSK2881078 or matching-placebo). In Part B, repeat-dose cohorts in men (n = 65) were 0...
April 27, 2017: British Journal of Clinical Pharmacology
https://www.readbyqxmd.com/read/28440570/mass-spectrometric-characterization-of-the-selective-androgen-receptor-modulator-sarm-yk-11-for-doping-control-purposes
#9
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/28373203/three-tier-regulation-of-cell-number-plasticity-by-neurotrophins-and-tolls-in-drosophila
#10
Istvan Foldi, Niki Anthoney, Neale Harrison, Monique Gangloff, Brett Verstak, Mohanakarthik Ponnadai Nallasivan, Samaher AlAhmed, Bangfu Zhu, Mark Phizacklea, Maria Losada-Perez, Marta Moreira, Nicholas J Gay, Alicia Hidalgo
Cell number plasticity is coupled to circuitry in the nervous system, adjusting cell mass to functional requirements. In mammals, this is achieved by neurotrophin (NT) ligands, which promote cell survival via their Trk and p75(NTR) receptors and cell death via p75(NTR) and Sortilin. Drosophila NTs (DNTs) bind Toll receptors instead to promote neuronal survival, but whether they can also regulate cell death is unknown. In this study, we show that DNTs and Tolls can switch from promoting cell survival to death in the central nervous system (CNS) via a three-tier mechanism...
May 1, 2017: Journal of Cell Biology
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
#11
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/28137616/detection-of-sarms-in-doping-control-analysis
#12
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/28134645/effects-of-surgical-and-nonsurgical-rapid-maxillary-expansion-on-palatal-structures
#13
Gökmen Kurt, Ayşe Tuba Altuğ, Gökhan Türker, Banu Kiliç, Erdem Kiliç, Alper Alkan
AIM: The aim of the present study was to compare the effects of surgical and nonsurgical rapid maxillary expansion (RME) in skeletally mature patients. MATERIALS AND METHODS: Surgically assisted rapid maxillary expansion (SARME) was used in 18 patients (2 males, 16 females) with a mean age of 19.90 years. Two nonsurgical RME groups were constructed to compare the expansion changes of SARME. Eighteen patients in maximum pubertal peak (12 males, 6 females) with a mean age of 13...
January 27, 2017: Journal of Craniofacial Surgery
https://www.readbyqxmd.com/read/28049609/surgically-assisted-rapid-maxillary-expansion-sarme-with-or-without-intraoperative-releasing-of-the-nasal-septum
#14
Thomas Jensen, Maria Rodrigo-Domingo
OBJECTIVE: To assess nasal septum deviation after surgically assisted rapid maxillary expansion (SARME) with or without intraoperative releasing of the nasal septum. STUDY DESIGN: A total of 20 consecutive adult patients with transverse maxillary deficiency underwent SARME with intraoperative releasing (n = 10) or nonreleasing (n = 10) of the nasal septum. Cone beam computed tomography scans were obtained immediately after surgery (T1), after the end of distraction (T2), and 6 months after SARME (T3)...
March 2017: Oral Surgery, Oral Medicine, Oral Pathology and Oral Radiology
https://www.readbyqxmd.com/read/27979262/effects-and-detection-of-nandrosol-and-ractopamine-administration-in-veal-calves
#15
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/27876544/follow-up-of-surgically-assisted-rapid-maxillary-expansion-after-6-5-years-skeletal-and-dental-effects
#16
J P de Gijt, A Gül, S T H Tjoa, E B Wolvius, K G H van der Wal, M J Koudstaal
Surgically-assisted rapid maxillary expansion (SARME) is a technique used to widen the maxilla, and we present the results of our long-term follow up (6.5 years). Seventeen patients who had been treated with SARME and prospectively followed were invited for long-term follow up using dental casts and posteroanterior cephalograms. The following measurements were made on the dental casts: transverse distances at canine, premolar, and molar level, length of the arch, and width and depth of the palate at premolar and molar level...
January 2017: British Journal of Oral & Maxillofacial Surgery
https://www.readbyqxmd.com/read/27827563/analytical-strategies-to-detect-enobosarm-administration-in-bovines
#17
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/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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