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As part of our discovery efforts searching for small molecul
2021-11-24
As part of our discovery efforts searching for small molecule GPR119 agonists, we analyzed active pharmacophores of known agonists from the literature, and found that -methylsulfonylphenyl and substituted 4-hydroxyl piperidine are common fragments. In our initial efforts, we linked these two fragme
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With these cyclopropene glutamate derivatives in
2021-11-24
With these cyclopropene-glutamate derivatives in hand, we tested their ability to ligate with popular bioorthogonal reagents (Fig 3). First, we tested their ability to ligate with a tetrazine (3,6-Di-2-pyridyl-1,2,4,5-tetrazine) via an inverse electron demand Diels-Alder reaction by monitoring the c
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Rare mutations can impair the molecular
2021-11-24
Rare mutations can impair the molecular function of GR and alter tissue sensitivity to GCs in humans, resulting in primary generalized GC resistance (PGGR) and hypersensitivity (PGGH) [14]. Familial and sporadic PGGR, or Chrousos Syndrome, is characterized by general and partial insensitivity of tis
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Ghsr may have therapeutic value in
2021-11-24
Ghsr may have therapeutic value in disorders associated with impairments in AHN. As anxiety disorders and enhanced fear responses observed in PTSD are linked with overgeneralization of similar but distinct memories (i.e poor discrimination), we suggest that acyl-ghrelin’s anti-anxiety effect (Lutter
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br Results br Discussion secretase
2021-11-24
Results Discussion γ-secretase-mediated proteolysis of integral membrane proteins is required for diverse biological processes (Lal and Caplan, 2011). One γ-secretase target of particular interest is Notch, as recent work has shown Notch activity to be increased in obesity and associated metab
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Notwithstanding the functioning of galaninergic system may b
2021-11-24
Notwithstanding, the functioning of galaninergic system may be even more complex (Fuxe et al., 2012). Some studies present evidence that GAL2 receptors might form heteroreceptor complexes with neuropeptide Y1 receptors in tlr signaling of amygdala (Narváez et al., 2015a), DRN (Díaz-Cabiale et al.,
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br Conclusion br Acknowledgements br Introduction Aminobutyr
2021-11-24
Conclusion Acknowledgements Introduction γ- Aminobutyric neurokinin receptor (GABA) is the main inhibitory neurotransmitter in the adult central nervous system. GABA receptors are divided into two classes, GABAA and GABAB. GABAA is an ionotropic receptor that mediates fast GABA responses b
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br Materials and methods This is a retrospective case
2021-11-24
Materials and methods This is a retrospective case-controlled study. The cases were selected based on the presence or absence of preeclampsia. Women enrolled in the study delivered singleton pregnancies at our institution from June 2003 to July 2004. Preeclampsia is defined as elevated blood pres
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br The inhibitory effect of ATP B knockdown on lysosomal
2021-11-24
The inhibitory effect of ATP7B knockdown on lysosomal exocytosis is likely mediated by the resulting oxidative stress induced by Cu, as exposure to oxidative stress induced by tert-Butyl hydroperoxide (TBHP) inhibited β-hex exocytosis as well, indicating that oxidative stress inhibits lysosomal ex
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As the presence of HPV specific antibodies at time
2021-11-24
As the presence of HPV-specific FIPI at time of vaccination is related to antibody response to vaccination [28], we evaluated its influence on the antibody responses among HIV+ and HIV− individuals at Months 7 and 18. Despite the small numbers, we observed that HIV+ men with detectable serum HPV ant
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In addition JMJ proteins respond to biotic stress and abioti
2021-11-24
In addition, JMJ proteins respond to biotic stress and abiotic stress in plants. Rice genes OsJMJ704 and OsJMJ705, which have demethylase activities of H3K27me2/3 and H3K4me2/3, respectively, regulate defense-related genes and affect the defense ability of rice against bacterial pathogen Xoo (Li et
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The proposed contributory role of endogenous histamine via a
2021-11-24
The proposed contributory role of endogenous histamine via activation of H1 receptor in the locomotor sensitization induced by caffeine was further ratified by H1 receptor antagonism during the induction phase and subsequently its effect on expression to locomotor sensitization induced by caffeine.
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br S Nitrosoglutathione reductase GSNOR also
2021-11-23
S-Nitrosoglutathione reductase (GSNOR) also identified as glutathione-dependent formaldehyde dehydrogenase (FDH), is a zinc-dependent dehydrogenase. It is a member of the alcohol dehydrogenase (ADH) family and is called class III alcohol dehydrogenase that regulates the levels of S-nitrosothiols (
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GT cells were treated in two ways
2021-11-23
GT1-7 GSK2194069 were treated in two ways; specifically, they were either dosed or transfected with VP, reflecting the extracellular and intracellular actions of VP, respectively. A dose of 200 pg/ml VP in culture supernatants was effective in stimulating GnRH in the supernatant and cell extracts;
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corticotropin-releasing factor In the course of our syntheti
2021-11-23
In the course of our synthetic studies, we also discovered an unprecedented application of Burgess reagent. Instead of generating an olefin by an intramolecular syn-elimination, the product resulting from the treatment of spirocyclic alcohols 11 and 12 with Burgess reagent led to the expansion of th
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