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br Results and discussion br Conclusions
2021-12-28
Results and discussion Conclusions TZDs represent a well-studied group of antidiabetic agents. Based on previous observations of the ability of some TZDs to activate FFAR1, we designed five scaffolds consisting of the TZD head, a linker, and a carefully selected privileged structure. For the p
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Herein we report the discovery
2021-12-28
Herein, we report the discovery of AM-3189 (). AM-3189 maintains the in vivo efficacy of AMG 837 while displaying a superior pharmacokinetic profile and minimal CNS exposure. As we reported previously, activity on the GPR40 receptor varies significantly with substitution at the β-carbon relative to
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Cx mimetic peptides short synthetic
2021-12-27
Cx mimetic peptides, short synthetic peptides corresponding to intracellular amino flumethasone sequences of diverse Cx have better specificity compared to traditional GJ blockers and openers. In particular, it was reported that Cx mimetic peptides reversibly inhibited GJ channel function in a conc
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Some clinical reports have suggested that
2021-12-27
Some clinical reports have suggested that galanin has a role in the neurobiology of mood disorders [[6], [7], [8], [9], [10]]. In behavioral studies, contradictory results have been reported [11,12]. For example, systemic administration of non-selective galanin receptor agonists, such as galmic [13]
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Liver is the house for a
2021-12-27
Liver is the house for a variety of xenobiotic-metabolizing Clindamycin HCl that produce reactive oxygen species as well as reactive metabolites (Johansson et al., 2009; Noh et al., 2017; Puntarulo and Cederbaum, 1998). When the enzymes act upon pre- or pro-haptens, the chemicals would be activated
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Following the discovery of diketo
2021-12-27
Following the discovery of β-diketo compounds S-1360 [31] and L-731988 [32] as anti-HIV integrase inhibitors, a group of researchers discovered a potent microcystin lr synthesis based derivative (1) as the inhibitor of HIV integrase functioning at the 3′-processing and strand transfer steps of HIV i
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Further investigation of the effects of this
2021-12-27
Further investigation of the effects of this inhibitor on histone acetylation revealed no HAT inhibitory effects at the level of global histone acetylation after 20h of incubation with C646. After 6h of incubation with C646, however, a slight increase in histone H3 acetylation was observed at lysine
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Although histamine can induce both proliferation and
2021-12-27
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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HCC is one of the most prevalent malignant tumors
2021-12-27
HCC is one of the most prevalent malignant tumors and a leading cause of cancer-related death, globally [[11], [12], [13]]. Hepatitis B virus (HBV) infection is closely related to the development of liver diseases [[14], [15], [16], [17]]. More than 350 million people are chronically infected with H
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Membrane based integrative treatment processes emerge as pot
2021-12-27
Membrane based integrative treatment processes emerge as potential solution compared to the conventional techniques. Gisi et al. (2009) presented a treatment scheme for tannery wastewater consisting of a biological pre-treatment and then a polymer as coagulant followed by reverse Thyroid Hormone Rec
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One of pathogenesis of COPD is oxidant antioxidant imbalance
2021-12-27
One of pathogenesis of COPD is oxidant/antioxidant imbalance. Indeed, it is well known that chronic tobacco smoking is a major risk factor for the development of COPD, and a defect in the detoxification of reactive species produced by cigarette smoke may predispose smokers to airflow obstruction and
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br Results and discussion br Conclusion In summary starting
2021-12-27
Results and discussion Conclusion In summary, starting from our previous lead Moniliformin sodium salt mg 1, we replaced the 5-nitropyrimidine core with pyrimidopyrimidine to obtain a series of novel compounds as drug candidates of GPR119 agonist for treatment of type 2 diabetes. Some derivat
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Considering the fact that OCL induced depletion of
2021-12-27
Considering the fact that OCL induced depletion of T ha 47 in non-stimulated cultures, the only possible explanation of this effect is the elevated mortality of these cells. It was found that OCL at the higher concentration induced the apoptosis of CD4+ and CD8+ T cells. These results strongly sugg
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Rapid action of E on
2021-12-27
Rapid action of E2 on GnRH neurons has been known for some time. E2 hyperpolarizes guinea pig GnRH neurons, alters cAMP production in GT1-cells and stimulates or inhibits [Ca2+]i oscillations within 15 min (Lagrange et al., 1995; Navarro et al., 2003; Temple et al., 2004; Romanò et al., 2008). Impor
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The two competitive bivalent GlxI inhibitors polyBHG nM and
2021-12-27
The two competitive bivalent GlxI inhibitors polyBHG2-62 (=1nM) and polyBHG2-54 (=0.3nM) () were designed based on the transition-state analog -(-bromophenyl--hydroxycarbamoyl) glutathione (BHG) by an examination of the X-ray crystal structure of human GlxI in complex with one CHG at each active sit
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