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br GPR is a class
2021-10-01

GPR119 is a class A GPCR expressed on pancreatic β-cells and certain enteroendocrine lrrk2 which upon activation with an agonist, increases insulin secretion in response to rising glucose levels. Mechanistically, this insulinotropic effect is bifurcated involving both GPR119-mediated β-cell signa
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In summary through medicinal chemistry
2021-10-01

In summary, through medicinal chemistry design and computer-assisted conformational modeling, the initial lead was evolved into a series of dihydrobenzofuran derivatives, , as potent GPR119 agonists. Optimization of general structure at various regions of the molecule, including the substituent on
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Several investigators including ourselves have previously
2021-10-01

Several investigators including ourselves have previously shown, that allogeneic HLA-DPB1 class II-alleles are powerful leukemia rejection fluorescent probes for CD4 T-cell therapy following allogeneic hematopoietic stem cell transplantation (Herr et al., 2017, Rutten et al., 2008, Stevanovic et al
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In insects structural cuticular proteins CPs play important
2021-10-01

In insects, structural cuticular proteins (CPs) play important roles in determining the diverse physical properties of the cuticle, depending on developmental stages, as well as different body regions, as a result of interactions with other CPs and the structural biopolymer chitin [4]. Many studies
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Glutamate activates cationic glutamate gated channels i e
2021-10-01

Glutamate activates cationic glutamate-gated channels (i.e. ionotropic glutamate receptors) that mediate the fast excitatory actions of glutamate. It also activate G protein-coupled receptors, named metabotropic glutamate receptors (mGluRs) (Pin and Bettler, 2016). The eight subtypes of mGluRs are k
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The rapid actions of glucocorticoids
2021-10-01

The rapid actions of glucocorticoids range from the production of endocannabinoid as a retrograde messenger [9], to regulation of ion channels [10], [11], to inhibitory effects on immune AACOCF3 [12], [13], [14]. Many different kinase signaling pathways have been implicated in the rapid actions of
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Both preclinical and clinical studies have identified a
2021-10-01

Both preclinical and clinical studies have identified a distributed set of CNS nuclei that participate in cognitive control of feeding behavior. Preclinical studies that utilize restricted access feeding schedules (RFS) indicate that rodents learn to anticipate delivery of scheduled meals as indicat
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The second experiment investigated the possible
2021-10-01

The second experiment investigated the possible neuronal mechanism underlying the effect of acupuncture. The baseline level of methamphetamine consumption in each group was similar, as in the first experiment (Fig. 2A). Acupuncture at HT7 also significantly inhibited the methamphetamine self-adminis
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br Conclusions Histone acetylation deacetylation is a major
2021-09-30

Conclusions Histone acetylation/deacetylation is a major epigenetic mechanism implicated in the regulation of transcription and various biological processes such as development and gametogenesis from plants to vertebrates. However, despite being well characterized in zebrafish, acetyltransferase
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Although histamine can induce both
2021-09-30

Although histamine can induce both proliferation and differentiation in vitro (Molina-Hernandez and Velasco, 2008), the promotion of neurogenesis conferred by H3R antagonism here does not seem to be caused by either the proliferation or the reduction of apoptosis of NSCs (Figure S3). Furthermore, H3
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While the dogma of the mainstream considers
2021-09-30

While the dogma of the mainstream considers Hippo pathway as a series of size-controlling kinases, there were still some controversial data supporting that YAP, a vital oncoprotein of Hippo downstream, is antagonistic to regenerative proliferation [[20], [21], [22]]. Known for its expansion-driving
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Under normal physiological conditions the body has sufficien
2021-09-30

Under normal physiological conditions, the body has sufficient oxygen supply, so glucose can produce large amounts of ATP by aerobic oxidation and oxidative phosphorylation in cells. After SCI, hypoxia ischemia can occur in local tissue, leading to decreasing of intracellular oxygen partial pressure
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The isoenzyme hGSTP is an attractive
2021-09-30

The isoenzyme hGSTP1-1 is an attractive drug target due to its high levels of disease association (target validation) and druggability (target tractability) properties [5,6,[17], [18], [19], [20], [21]]. hGSTP1-1 functions as a homodimer protein [18]. Each monomer has two domains, an α/β domain (N-t
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Overall this study provides compelling evidence that overexp
2021-09-30

Overall, this study provides compelling evidence that overexpression of catalase coupled with an enriched diet of OM3 fatty acids are metabolically beneficial. This combination was shown to increase adipose tissue expression of the GPR120/FFAR4, which by interacting with the Nrf2 pathway, resulted i
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Alpha synuclein AS is a protein
2021-09-30

Alpha synuclein (AS) is a protein located in presynaptic terminals of neurons that functions in recycling and storage of neurotransmitters [17]. Under conditions of inflammation and oxidative stress, AS proteins misfold and accumulate into rvx [81], [90]. The aggregates of misfolded AS oligimorize i
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