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https://www.readbyqxmd.com/read/27706103/in-vitro-metabolic-studies-of-rev-erb-agonists-sr9009-and-sr9011
#1
Lore Geldof, Koen Deventer, Kris Roels, Eva Tudela, Peter Van Eeno
SR9009 and SR9011 are attractive as performance-enhancing substances due to their REV-ERB agonist effects and thus circadian rhythm modulation activity. Although no pharmaceutical preparations are available yet, illicit use of SR9009 and SR9011 for doping purposes can be anticipated, especially since SR9009 is marketed in illicit products. Therefore, the aim was to identify potential diagnostic metabolites via in vitro metabolic studies to ensure effective (doping) control. The presence of SR9009 could be demonstrated in a black market product purchased over the Internet...
October 3, 2016: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/27603791/pharmacological-targeting-the-rev-erbs-in-sleep-wake-regulation
#2
Ariadna Amador, Salvador Huitron-Resendiz, Amanda J Roberts, Theodore M Kamenecka, Laura A Solt, Thomas P Burris
The circadian clock maintains appropriate timing for a wide range of behaviors and physiological processes. Circadian behaviors such as sleep and wakefulness are intrinsically dependent on the precise oscillation of the endogenous molecular machinery that regulates the circadian clock. The identical core clock machinery regulates myriad endocrine and metabolic functions providing a link between sleep and metabolic health. The REV-ERBs (REV-ERBα and REV-ERBβ) are nuclear receptors that are key regulators of the molecular clock and have been successfully targeted using small molecule ligands...
2016: PloS One
https://www.readbyqxmd.com/read/26963516/pharmacological-and-genetic-modulation-of-rev-erb-activity-and-expression-affects-orexigenic-gene-expression
#3
Ariadna Amador, Yongjun Wang, Subhashis Banerjee, Theodore M Kameneka, Laura A Solt, Thomas P Burris
The nuclear receptors REV-ERBα and REV-ERBβ are transcription factors that play pivotal roles in the regulation of the circadian rhythm and various metabolic processes. The circadian rhythm is an endogenous mechanism, which generates entrainable biological changes that follow a 24-hour period. It regulates a number of physiological processes, including sleep/wakeful cycles and feeding behaviors. We recently demonstrated that REV-ERB-specific small molecules affect sleep and anxiety. The orexinergic system also plays a significant role in mammalian physiology and behavior, including the regulation of sleep and food intake...
2016: PloS One
https://www.readbyqxmd.com/read/26842585/emerging-drugs-affecting-skeletal-muscle-function-and-mitochondrial-biogenesis-potential-implications-for-sports-drug-testing-programs
#4
Mario Thevis, Wilhelm Schänzer
RATIONALE: A plethora of compounds potentially leading to drug candidates that affect skeletal muscle function and, more specifically, mitochondrial biogenesis, has been under (pre)clinical investigation for rare as well as more common diseases. Some of these compounds could be the object of misuse by athletes aiming at artificial and/or illicit and drug-facilitated performance enhancement, necessitating preventive and proactive anti-doping measures. METHODS: Early warnings and the continuous retrieval and dissemination of information are crucial for sports drug testing laboratories as well as anti-doping authorities, as they assist in preparation of efficient doping control analytical strategies for potential future threats arising from new therapeutic developments...
March 15, 2016: Rapid Communications in Mass Spectrometry: RCM
https://www.readbyqxmd.com/read/26616049/stimulation-of-nuclear-receptor-rev-erbs-regulates-tumor-necrosis-factor-induced-expression-of-proinflammatory-molecules-in-c6-astroglial-cells
#5
Norimitsu Morioka, Mizuki Tomori, Fang Fang Zhang, Munenori Saeki, Kazue Hisaoka-Nakashima, Yoshihiro Nakata
Under physiological conditions, astrocytes maintain homeostasis in the CNS. Following inflammation and injury to the CNS, however, activated astrocytes produce neurotoxic molecules such as cytokines and chemokines, amplifying the initial molecular-cellular events evoked by inflammation and injury. Nuclear receptors REV-ERBα and REV-ERBβ (REV-ERBs) are crucial in the regulation of inflammation- and metabolism-related gene transcription. The current study sought to elucidate a role of REV-ERBs in rat C6 astroglial cells on the expression of inflammatory molecules following stimulation with the neuroinflammatory cytokine tumor necrosis factor (TNF)...
January 8, 2016: Biochemical and Biophysical Research Communications
https://www.readbyqxmd.com/read/25800870/suppression-of-atherosclerosis-by-synthetic-rev-erb-agonist
#6
Sadichha Sitaula, Cyrielle Billon, Theodore M Kamenecka, Laura A Solt, Thomas P Burris
The nuclear receptors for heme, REV-ERBα and REV-ERBβ, play important roles in the regulation of metabolism and inflammation. Recently it was demonstrated that reduced REV-ERBα expression in hematopoetic cells in LDL receptor null mice led to increased atherosclerosis. We sought to determine if synthetic REV-ERB agonists that we have developed might have the ability to suppress atherosclerosis in this model. A previously characterized synthetic REV-ERB agonist, SR9009, was used to determine if activation of REV-ERB activity would affect atherosclerosis in LDL receptor deficient mice...
May 8, 2015: Biochemical and Biophysical Research Communications
https://www.readbyqxmd.com/read/24355794/a-study-on-circadian-rhythm-disorder-of-rat-lung-tissue-caused-by-mechanical-ventilation-induced-lung-injury
#7
Huan Li, Chunxiao Wang, Jiaqi Hu, Junyuan Tan
Ventilator-induced lung injury (VILI), the most serious complication of mechanical ventilation therapy, is an excessive inflammatory response in lung tissue characterized by infiltration of inflammatory cells and overproduction of inflammatory mediators. The pathogenesis of VILI is very complex. It is becoming increasingly evident that disruption of circadian rhythm affects the immune response. Whether the pathogenesis of VILI is associated with circadian rhythm disruption has not been reported. In this study, we establish VILI model in SD rat by performing an endotracheal intubation and placing the rat on a mechanical ventilator (tidal volume of 40 ml/kg or 10 ml/kg without positive end-expiratory pressure)...
February 2014: International Immunopharmacology
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