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https://www.readbyqxmd.com/read/28714043/effects-of-surgically-assisted-rapid-maxillary-expansion-on-mandibular-position-a-three-dimensional-study
#1
Talles Fernando Medeiros Oliveira, Valfrido Antônio Pereira-Filho, Mario Francisco Real Gabrielli, Eduardo Sanches Gonçales, Ary Santos-Pinto
BACKGROUND: This study aimed to evaluate three-dimensional changes in mandibular position after surgically assisted rapid maxillary expansion (SARME). METHODS: A retrospective study was carried out with tomographic records of 30 adult patients with maxillary transverse deficiency who underwent SARME. Cone beam computed tomography scans were obtained preoperatively (T1), after expansion (T2) and 6 months after expansion (T3). Mandibular landmarks were measured with respect to axial, sagittal, and coronal planes...
December 2017: Progress in Orthodontics
https://www.readbyqxmd.com/read/28696695/structure-based-approach-to-identify-5-4-hydroxyphenyl-pyrrole-2-carbonitrile-derivatives-as-potent-and-tissue-selective-androgen-receptor-modulators
#2
Ray Unwalla, James J Mousseau, Olugbeminiyi O Fadeyi, Chulho Choi, Kevin Parris, Baihua Hu, Thomas Kenney, Susan Chippari, Christopher McNally, Karthick Vishwanathan, Edward Kilbourne, Catherine Thompson, Sunil Nagpal, Jay Wrobel, Matthew Yudt, Carl A Morris, Dennis Powell, Adam M Gilbert, Eugene L Piatnitski Chekler
In an effort to find new and safer treatments for osteoporosis and frailty, we describe a novel series of selective androgen receptor modulators (SARMs). Using a structure-based approach, we identified compound 7, a potent AR (ARE EC50 = 0.34 nM) and selective (N/C interaction EC50 = 1206 nM) modulator. In vivo data, an AR LBD X-ray structure of 7, and further insights from modeling studies of ligand receptor interactions are also presented.
July 27, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28683272/axon-death-pathways-converge-on-axundead-to-promote-functional-and-structural-axon-disassembly
#3
Lukas J Neukomm, Thomas C Burdett, Andrew M Seeds, Stefanie Hampel, Jaeda C Coutinho-Budd, Jonathan E Farley, Jack Wong, Yonca B Karadeniz, Jeannette M Osterloh, Amy E Sheehan, Marc R Freeman
Axon degeneration is a hallmark of neurodegenerative disease and neural injury. Axotomy activates an intrinsic pro-degenerative axon death signaling cascade involving loss of the NAD(+) biosynthetic enzyme Nmnat/Nmnat2 in axons, activation of dSarm/Sarm1, and subsequent Sarm-dependent depletion of NAD(+). Here we identify Axundead (Axed) as a mediator of axon death. axed mutants suppress axon death in several types of axons for the lifespan of the fly and block the pro-degenerative effects of activated dSarm in vivo...
July 5, 2017: Neuron
https://www.readbyqxmd.com/read/28657313/novel-methods-for-prioritizing-close-in-analogs-from-structure-activity-relationship-matrices
#4
Liying Zhang, Kjell Johnson, Jeremy Starr, Jared Milbank, Andrew M Kuhn, Christopher Poss, Robert V Stanton, Veerabahu Shanmugasundaram
Here we describe the development of novel methods for compound evaluation and prioritization based on the structure-activity relationship matrix (SARM) framework. The SARM data structure allows automatic and exhaustive extraction of SAR patterns from data sets and their organization into a chemically intuitive scaffold/functional-group format. While SARMs have been used in the retrospective analysis of SAR discontinuity and identifying underexplored regions of chemistry space, there have been only a few attempts to apply SARMs prospectively in the prioritization of "close-in" analogs...
July 13, 2017: Journal of Chemical Information and Modeling
https://www.readbyqxmd.com/read/28624515/development-of-selective-androgen-receptor-modulators-sarms
#5
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
#6
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
#7
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...
July 2017: Infection Control and Hospital Epidemiology
https://www.readbyqxmd.com/read/28499507/nasolabial-changes-after-two-different-approaches-for-surgically-assisted-rapid-maxillary-expansion
#8
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
#9
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
#10
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
#11
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
#12
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
#13
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
#14
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
#15
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
#16
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
#17
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
#18
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
#19
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
#20
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
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